Volatile Imidazoles and Group 2 Imidazole Based Metal Precursors

Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion. Synthesis of the novel compounds and their use to form BST films is also contemplated

BENZIMIDAZOLE DERIVATIVES USEFUL AS TRPM8 CHANNEL MODULATORS

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: 18-. (canceled)11. A method as in claim 10 , wherein the inflammatory pain is due to inflammatory bowel disease claim 10 , visceral pain claim 10 , migraine claim 10 , post operative pain claim 10 , osteoarthritis claim 10 , rheumatoid arthritis claim 10 , back pain claim 10 , lower back pain claim 10 , joint pain claim 10 , abdominal pain claim 10 , chest pain claim 10 , labor claim 10 , musculoskeletal diseases claim 10 , skin diseases claim 10 , toothache claim 10 , pyresis claim 10 , burn claim 10 , sunburn claim 10 , snake bite claim 10 , venomous snake bite claim 10 , spider bite claim 10 , insect sting claim 10 , neurogenic bladder claim 10 , interstitial cystitis claim 10 , urinary tract infection claim 10 , rhinitis claim 10 , contact dermatitis/hypersensitivity claim 10 , itch claim 10 , eczema claim 10 , pharyngitis claim 10 , mucositis claim 10 , enteritis claim 10 , irritable bowel syndrome claim 10 , cholecystitis claim 10 , pancreatitis claim 10 , postmastectomy pain syndrome claim 10 , menstrual pain claim 10 , endometriosis claim 10 , sinus headache claim 10 , tension headache claim 10 , or arachnoiditis.12. A method as in claim 10 , wherein the inflammatory pain is inflammatory hyperalgesia.13. A method as in claim 12 , wherein the inflammatory hyperalgesia is inflammatory somatic hyperalgesia or inflammatory visceral hyperalgesia.14. A method as in claim 12 , wherein the inflammatory hyperalgesia is due to inflammation claim 12 , osteoarthritis claim 12 , rheumatoid arthritis claim 12 , back pain claim 12 , joint pain claim 12 , abdominal pain claim 12 , musculoskeletal diseases claim 12 , skin diseases claim 12 , post operative pain claim 12 , headaches claim 12 , fibromyalgia claim 12 , toothache claim 12 , burn claim 12 , sunburn claim 12 , insect sting ...

Photoredox-Catalyzed Direct C-H Functionalization of Arenes

The invention generally relates to methods of making substituted arenes via direct C—H amination. More specifically, methods of making para- and ortho-substituted arenes via direct C—H amination are disclosed. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 2. The method of claim 1 , wherein the electron donating group is selected from —OH claim 1 , —SH claim 1 , —NH claim 1 , C1-C8 alkyl claim 1 , C1-C8 alkoxy claim 1 , C1-C8 thioalkoxy claim 1 , C1-C8 alkylamino claim 1 , (C1-C8)(C1-C8) dialkylamino claim 1 , —OC(═O)R claim 1 , —NHC(═O)R claim 1 , and Ar;{'sup': 6', '7, 'wherein each of Rand Ris independently selected from C1-C8 alkyl; and'}{'sup': '2', 'wherein Aris selected from aryl and heteroaryl and substituted with 0, 1, 2, or 3 groups independently selected from halogen and C1-C8 alkyl.'}3. The method of claim 1 , wherein Z is F.48-. (canceled)12. (canceled)13. The method of claim 1 , wherein the fluoride is selected from ammonium fluoride claim 1 , cesium fluoride claim 1 , and triethylamine hydrofluoride.1415-. (canceled)16. The method of claim 1 , wherein the oxidant is molecular oxygen.17. The method of claim 1 , wherein the oxidant is 2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethyl-1-piperidinyloxy radical (TEMPO).1820-. (canceled)21. The method of claim 1 , wherein Z is —CN.29. The method of claim 1 , wherein the compound is isotopically-labeled.30. The method of claim 25 , wherein the compound contains a radioactive isotope.31. The method of claim 1 , wherein the compound is not isotopically-labeled. This application is a continuation of U.S. application Ser. No. 15/826,092, filed Nov. 29, 2017, which is a continuation of International Application No. PCT/US2016/035549 with an international filing date of Jun. 2, 2016, which claims priority to U.S. Provisional Application No. 62/170,632 filed on Jun. 3, 2015, the contents of which are incorporated ...

HIGH MOLECULAR WEIGHT POLYLACTIC ACID SYNTHESIZED VIA POLYCONDENSATION CATALYZED BY BIONIC CREATININE GUANIDININIUM CHLORIDE

Disclosed is a high molecular weight polylactic acid synthesized by using a method for synthesizing and catalytically-polycondensing bionic creatinine-guanidinium chloride. Creatinine is used as the material in a reaction with aqueous hydrochloric acid to synthesize a bionic creatinine-guanidinium salt catalyst, creatinine-guanidinium chloride (CR.Cl). The creatinine-guanidinium chloride synthesized is used as a catalyst, an industrial grade lactic acid (LA, 85% to 90%, aqueous solution) is used as a monomer, a solvent-free two-step polycondensation method is used to synthesize and afford metal-free and toxic residue-free polylactic acid featuring high biological safety and high molecular weight. 13-. (canceled)6. The method according to claim 5 , wherein the high molecular weight polylactic acid has a weight average molecular weight (Mw) of from about 1.4×10to about 2.5×10. The present invention belongs to the field of biodegradable medical materials, relating to a process for synthesizing polylactic acid featuring a high biological safety and a high molecular weight via polycondensation, wherein a bionic organic guanidinium salt, creatinine-guanidinium chloride, is used as catalyst.In recent years, along with the rapid development of medicine, pharmacy and biological tissue engineering, the demand for materials featuring good biocompatibility, biological safety and biodegradability is rapidly growing throughout the world. Biodegradable polylactic acid has been extensively applied in modern pharmaceutical science (controlled-released and targeted drug carriers), biological tissue engineering science (surgical sutures, bone screws, fracture splints, meniscus-repairing materials and devices, cells and bioactive species scaffold materials) and the like. It is required that the polymers used in the field of pharmacy and medicine should not contain any metal and toxic ingredient. Currently, the production of commercially available polylactic acid is mainly performed as ...

Compounds and Methods for Treating Cancer and Diseases of the Central Nervous System

Disclosed are compounds of the general formula (I): 132-. (canceled)3436-. (canceled)37. The method of claim 33 , wherein D is 1 claim 33 ,3-imidazolyl.38. The method of claim 33 , wherein n is 3 to 4.39. The method of claim 33 , wherein n is 4.40. The method of claim 33 , wherein T is substituted with perfluoroalkyl.41. The method of claim 33 , wherein T is selected from the group consisting of: 4-chlorophenyl claim 33 , 3-methoxyphenyl claim 33 , 2-amino-4-chlorophenyl claim 33 , 4-methoxyphenyl claim 33 , phenyl claim 33 , 4 fluorophenyl claim 33 , 4-bromophenyl claim 33 , 4-iodophenyl claim 33 , 2-hydroxyphenyl claim 33 , 4-nitrophenyl claim 33 , biphenyl-4-yl claim 33 , 3 claim 33 ,4-dichlorophenyl claim 33 , 4-isopropylphenyl claim 33 , 4-tert-butylphenyl claim 33 , 4-hydroxyphenyl claim 33 , 4-(trifluoromethyl)phenyl) claim 33 , and 4-benzoylphenyl.42. (canceled)43. The method of claim 33 , wherein said compound is selected from the group consisting of: 4-(4-chlorophenyl)-1-(1H-imidazol-1-yl)butane hydrochloride (QC-105); 1-(3-Phenyl-propyl)-1H-imidazole hydrochloride (QC-172); 1-[4-(4-Bromo-phenyl)-butyl]1H-imidazole hydrochloride (QC-199); 1-[4-(4-(Trifluoromethyl)phenyl)butyl]-1H-imidazole hydrochloride (QC-234); and pharmaceutically acceptable salts thereof.44. The method of claim 33 , wherein said compound is 1-[4-(4 Bromo-phenyl)-butyl]-1H-imidazole hydrochloride (QC-199); or pharmaceutically acceptable salts thereof.45. The method according to claim 33 , wherein the disease is Alzheimer's disease.4689-. (canceled)90. The method according to claim 33 , wherein the disease is Parkinson's disease.91. The method of claim 40 , wherein T is substituted with Br.92. The method of claim 40 , wherein T is substituted with Cl. This invention is in the field of pharmaceuticals, and relates to compounds and compositions for treating/mitigating cancer and for suppressing tumor growth. The invention also relates to compounds, compositions and methods for the ...

PREPARATION AND USE OF SILVER SULFADIAZINE-IMMOBILIZED FILLERS

Silver sulfadiazine-immobilized inorganic fillers are described, and their synthesis is presented. The fillers are believed to have utility in dental composites and dental adhesives to achieve potent, long-term, and none-leaching antimicrobial effects. 1. A composition of matter , comprising:a particulate substrate comprising an inorganic filler;an amine-terminated hydrocarbon molecule moiety covalently bonded by way of a carbon atom of said hydrocarbon molecule moiety to said inorganic filler;a cyanuric chloride molecule moiety bonded to an amine group of said amine-terminated hydrocarbon molecule moiety;a sulfadiazine molecule moiety bonded to said cyanuric chloride molecule moiety; anda silver metal ion incorporated in said sulfadiazine moiety.2. The composition of matter of claim 1 , wherein a second sulfadiazine molecule moiety is bonded to said cyanuric chloride molecule moiety.3. The composition of matter of claim 2 , wherein said second sulfadiazine molecule moiety has a second silver metal ion incorporated therein.4. The composition of matter of claim 1 , wherein said particulate substrate comprising an inorganic filler is a particulate glass substrate.5. The composition of matter of claim 4 , wherein said particulate glass substrate comprises a glass containing BaO.6. The composition of matter of claim 1 , wherein said amine-terminated hydrocarbon molecule moiety is (3-aminopropyl)trimethoxysilane.7. A method of producing a composition of matter claim 1 , comprising the steps of:providing a particulate substrate comprising an inorganic filler;reacting said inorganic filler with an amine-terminated hydrocarbon molecule moiety to covalently bond said hydrocarbon molecule moiety by way of a carbon atom thereof to said inorganic filler to produce an amine modified substrate;reacting said amine modified substrate with a cyanuric chloride molecule moiety to bond said cyanuric chloride molecule moiety to an amine group of said amine-terminated hydrocarbon ...

CETP INHIBITORS

Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: 3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': '1', 'Y is —(CRR)—;'}{'sup': '6', 'sub': 1', '5', '1', '5, 'R and Rare each independently selected from the group consisting of H and —C-Calkyl, wherein —C-Calkyl is optionally substituted with 1-11 halogens;'}{'sup': 1', '2, 'sub': 1', '5', '2', 'n', '1', '5, 'Ris selected from the group consisting of H, —C-Calkyl, and —(C(R))A, wherein —C-Calkyl is optionally substituted with 1-11 halogens;'}{'sup': 2', '1', '1', '2', '2', '2', '1', '2, 'sub': 2', 'n, 'Wherein one of B and Ris A; and one of B, R, and Ris Aor —(C(R))A; so that the compound of Formula I comprises one group Aand one group A;'}{'sup': '3', 'claim-text': (a) an aromatic ring selected from phenyl and naphthyl;', {'sup': 3', '3, '(b) a 5-6-membered heterocyclic ring having 1-4 heteroatoms independently selected from N, S, O, and —N(O)—, and optionally also comprising 1-3 double bonds and a carbonyl group, wherein the point of attachment of Ato the phenyl ring to which Ais attached is a carbon atom; and'}, {'sub': 'x', 'sup': 3', '3, '(c) a benzoheterocyclic ring comprising a phenyl ring fused to a 5-6-membered heterocyclic ring having 1-2 heteroatoms independently selected from O, N, and —S(O)— and optionally 1-2 double bonds, wherein the point of attachment of Ato the phenyl ring to which Ais attached is a carbon atom;'}], 'Ais selected from the group consisting of{'sup': '2', 'claim-text': (a) an aromatic ring selected from phenyl and naphthyl;', '(b) a 5-6-membered heterocyclic ring having 1-4 heteroatoms independently selected from N, S, O, and —N(O)—, and optionally also comprising 1-3 double bonds and a carbonyl group;', '(c) a benzoheterocyclic ring ...

PHOTOREDOX-CATALYZED DIRECT C-H FUNCTIONALIZATION OF ARENES

The invention generally relates to methods of making substituted arenes via direct C—H amination. More specifically, methods of making para- and ortho-substituted arenes via direct C—H amination are disclosed. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 2. The method of claim 1 , wherein the electron donating group is selected from —OH claim 1 , —SH claim 1 , —NH claim 1 , C1-C8 alkyl claim 1 , C1-C8 alkoxy claim 1 , C1-C8 thioalkoxy claim 1 , C1-C8 alkylamino claim 1 , (C1-C8)(C1-C8) dialkylamino claim 1 , —OC(═O)R claim 1 , —NHC(═O)R claim 1 , and Ar;{'sup': 6', '7, 'wherein each of Rand Ris independently selected from C1-C8 alkyl; and'}{'sup': '2', 'wherein Aris selected from aryl and heteroaryl and substituted with 0, 1, 2, or 3 groups independently selected from halogen and C1-C8 alkyl.'}3. The method of claim 1 , wherein Z is a halogen.4. The method of claim 3 , wherein the halogen is selected from fluorine and chlorine.5. The method of claim 1 , wherein Z is selected from C1-C4 alkylamino claim 1 , C1-C4 dialkylamino claim 1 , arylamino claim 1 , diarylamino claim 1 , and C1-C4 alkarylamino.6. The method of claim 1 , wherein Z is —NH.7. The method of claim 1 , wherein Z is Ar.8. The method of claim 7 , wherein Aris selected from pyrazole claim 7 , 1 claim 7 ,2 claim 7 ,3-triazole claim 7 , 1 claim 7 , 2 claim 7 , 4-triazole claim 7 , benzotriazole claim 7 , imidazole claim 7 , and benzimidazole.12. The method of claim 1 , wherein the nucleophile is a halide.13. The method of claim 12 , wherein the halide is selected from ammonium fluoride claim 12 , cesium fluoride claim 12 , lithium chloride claim 12 , triethylamine hydrochloride claim 12 , and triethylamine hydrofluoride.14. The method of claim 1 , wherein the nucleophile is an amine.15. The method of claim 14 , wherein the amine is ammonium bicarbonate.16. The method of claim 1 , wherein the ...

Electronic Device and Compound

The invention relates to an electronic device comprising a compound having Formula (1): AB(1), wherein A is a structural moiety that consists of at least two atoms and comprises a conjugated system of delocalized electrons, each B is independently selected from an imine functional group (1a), wherein R, R, R, Rare independently selected from C-Calkyl, C-Calkenyl, C-Calkinyl, C-Ccycloalkyl, C-Caryl, C-Cheteroaryl, C-Carylalkyl, C-Cheteroarylalkyl, the wave line represents a covalent bond to the imine nitrogen atom, G is in each group (1a) independently selected from a quarternary carbon atom and from a cyclopropenylidene structural moiety, x is an integer equal one or higher, preferably equal two or higher, and the lone electron pair of the imine nitrogen atom and/or the pi-electrons of the imine double bond of at least one group B is conjugated with the conjugated system of delocalized electrons comprised in the structural moiety A, with the proviso that two or more of the substituents R, R, R, Rmay be connected to form a ring that may contain also unsaturation and, if any of the substituents R, R, R, Rcomprises two or more carbon atoms, up to one third of the overall count of the carbon atoms in the substituent or in any ring formed by two connected substituents can be replaced with heteroatoms independently selected from O, S, N and B as well as to an electrically semiconducting material and a compound for use in the electronic device. 2. Electronic device according to claim 1 , wherein x is an integer selected from 2 claim 1 , 3 and 4 and the lone electron pairs of the imine nitrogen atoms and/or the pi-electrons of the imine double bonds of at least two groups B are conjugated with the conjugated system of delocalized electrons comprised in the structural moiety A.3. Electronic device according to claim 1 , wherein A is a C-Carene or C-Cheteroarene structural moiety that contains one conjugated system of delocalized electrons.4. Electronic device according to ...

A Manufacturing Process for 2-Nitroimino Heterocyclic Compounds

The present invention relates to a process for manufacture of 2-nitroimino heterocyclic compounds and intermediates thereof. More particularly, the present invention relates to a convenient manufacturing process for preparation of 2-nitroimino imidazolidine compounds. 2. The process as claimed in claim 1 , wherein said nitroimino heterocyclic compound of Formula B is prepared using a diamine of Formula III wherein n is 2.3. The process as claimed in claim 1 , wherein said nitroimino heterocyclic compound of Formula B is prepared using a diamine of Formula III wherein n is 3.5. The process as claimed in claim 1 , wherein said acid is sulfuric acid.6. The process as claimed in claim 1 , wherein the reaction proceeds without isolation of compound of Formula II.7. The process as claimed in claim 1 , wherein the reaction is carried out at a temperature in the range of about of 5° C. to about 50° C. The present invention relates to a process for manufacture of 2-nitroimino heterocyclic compounds and intermediates thereof. More particularly, the present invention relates to a convenient manufacturing process for preparation of 2-nitroimino imidazolidine compounds.Nitroimino heterocyclic compounds of general Formula A are useful intermediates for certain insecticides and for products with certain medicinal applications. Imidacloprid is one such widely used insecticide.wherein R, Rand Rare the same or different and represent hydrogen or a lower alkyl of 1 to 4 carbon atoms, optionally substituted with a heterocyclic ring wherein one of the ring atoms comprises nitrogen, and wherein said ring is being optionally substituted with halogen or lower alkyl of 1 to 4 carbon atoms, and n is 2, 3 or 4.Imidacloprid is a systemic insecticide with translaminar activity and with contact and stomach action. It is widely used for controlling of sucking insects, including rice-, leaf- and plant hoppers, aphids, thrips and whitefly. It is also found to be effective against soil insects, ...

HYDROGEN SULFIDE DONOR IN ORGANIC SALT FORM AND PREPARATION METHOD THEREFOR

A hydrogen sulfide donor in an organic salt form and a preparation method thereof. The hydrogen sulfide donor exists as a salt formed by organic compounds with an alkaline motif and hydrogen sulfide with weak acidity. The hydrogen sulfide donor features with a simple structure, and an easy preparation method. Moreover, hydrogen sulfide donors in different forms can be prepared according to research and development needs. After the hydrogen sulfide donor enters an organism, the process of in vivo dissociation and hydrogen sulfide supply is simple, rapid, and effective, and there is no requirement for enzyme or any other complicated condition, and thus, the hydrogen sulfide donor has a great application prospect and value. 1. A hydrogen sulfide donor in organic salt form , characterized in that the donor is a salt structure formed by organic compounds with basic moiety and hydrogen sulfide.2. The hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are those pharmacological compounds possessing physiological and/or pharmacological activities.3. The hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are those with the structures selected from the group consisting of guanidines claim 1 , amidines claim 1 , hydrazines.4. The hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are those amino acid compounds such as arginine claim 1 , lysine claim 1 , etc.5. The hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are alkaloids.6. A preparative method for hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are dissolved in the solvent claim 1 , to which is added hydrogen sulfide ...

Hydrazinyl Lipidoids and Uses Thereof

The present disclosure is directed to hydrazinyl lipidoids, formulations thereof further comprising at least one active agent, as well as methods of delivering the at least one active agent to a target organism. 130-. (canceled)32. The compound of claim 31 , wherein Ris a group of formula (XII).33. The compound of claim 32 , wherein Ris hydrogen and Ris selected from the group consisting of an optionally substituted aliphatic group claim 32 , an optionally substituted heteroaliphatic group claim 32 , an optionally substituted aryl group claim 32 , an optionally substituted heteroaryl group claim 32 , an optionally substituted cycloalkyl group claim 32 , and an optionally substituted heterocycloalkyl group.34. The compound of claim 33 , wherein Ris selected from the group consisting of methyl claim 33 , 2-hydroxyethyl claim 33 , optionally substituted phenyl claim 33 , optionally substituted pyridyl claim 33 , and optionally substituted 2 claim 33 ,5-dihydro-1H-imidazole.35. The compound of claim 32 , wherein Ris hydrogen and Ris a group of formula (XII).36. The compound of claim 32 , wherein Ris a group of formula (XII) and Ris selected from the group consisting of an optionally substituted aliphatic group claim 32 , an optionally substituted heteroaliphatic group claim 32 , an optionally substituted aryl group claim 32 , an optionally substituted heteroaryl group claim 32 , an optionally substituted cycloalkyl group claim 32 , and an optionally substituted heterocycloalkyl group.37. The compound of claim 36 , wherein Ris selected from the group consisting of methyl claim 36 , 2-hydroxyethyl claim 36 , optionally substituted phenyl claim 36 , optionally substituted pyridyl claim 36 , and optionally substituted 2 claim 36 ,5-dihydro-1H-imidazole.38. The compound of claim 32 , wherein Rand Rare each a group of formula (XII).39. The compound of claim 31 , wherein Ris hydrogen and Ris selected from the group consisting of an optionally substituted aliphatic group claim ...

Process for Preparing Asymmetrical Imidazolium Salts

The invention relates to a process for preparing an asymmetrical imidazolium salt of formula (1A), in which R1 is an aromatic group, R2 is chosen from a cyclic secondary aliphatic alkyl group and a heteroalkyl group, R3 and R4 are chosen, independently of one another, from the group consisting of hydrogen, a halide and an alkyl group, and A″ is an anion. The process comprises a fast substep of forming a reaction mixture by bringing one equivalent of an aniline into contact with one equivalent of a compound bearing an amine group, in the presence of at least four point five equivalents of a Brønsted acid. The process also comprises a second substep of forming a solution comprising one equivalent of a dicarbonyl, one equivalent of formaldehyde, and at least four point five equivalents of the Brønsted acid, and adding thereto the reaction mixture formed in the first substep. The mixture is left to stir for a predetermined time at a predetermined temperature. The intermediate asymmetrical imidazolium salt 1A is then isolated.

BORATE-BASED BASE GENERATOR, AND BASE-REACTIVE COMPOSITION COMPRISING SUCH BASE GENERATOR

An object of the present invention is to provide a compound which is capable of attaining a composition having high storage stability without reacting with a base-reactive compound, even in the case of storage for a long period of time in a mixed state with the base-reactive compound, such as an epoxy-based compound, as well as capable of generating a strong base (guanidines, biguanides, phosphazenes or phosphoniums) by irradiation of light (active energy rays) or heating; a base generator comprising the compound; and a base-reactive composition comprising the base generator and the base-reactive compound. 3. The compound according to claim 1 , wherein Rin the general formula (A) is an alkyl group having 1 to 12 carbon atoms claim 1 , or a phenylethynyl group which may be substituted with a halogen atom claim 1 , an alkyl group having 1 to 6 carbon atoms claim 1 , an alkoxy group having 1 to 6 carbon atoms claim 1 , or an alkylthio group having 1 to 6 carbon atoms claim 1 , and all of Rto Rare the same phenyl group which may be substituted with a halogen atom claim 1 , an alkyl group having 1 to 6 carbon atoms claim 1 , an alkoxy group having 1 to 6 carbon atoms claim 1 , or an alkylthio group having 1 to 6 carbon atoms.4. The compound according to claim 2 , wherein the ammonium cation having the guanidinium group claim 2 , the biguanidium group or the phosphazenium group claim 2 , or the phosphonium cation represented by Z in the general formula (A) is the ammonium cation having the guanidinium group represented by the general formula (B) claim 2 , the ammonium cation having the biguanidium group represented by the general formula (B) claim 2 , or the phosphonium cation represented by the general formula (B).5. The compound according to claim 4 , wherein claim 4 , in the compound represented by the general formula (B) claim 4 , Rtogether with Rand Rtogether with Rform an alkylene group having 2 to 4 carbon atoms claim 4 , Ris a hydrogen atom claim 4 , and Ris a ...

THERAPEUTIC COMPOUNDS

The invention provides methods for producing analgesia in an animal comprising administering to the animal a compound of the formula Ia′, Ib′, Ic′, and Id′:

METHOD OF PREPARING A HIGH PURITY IMIDAZOLIUM SALT

The present invention encompasses a novel method for synthesizing highly pure salts of the general formula QA, wherein Q is: 2. The process of claim 1 , wherein R=R=R=hydrogen and wherein each of R claim 1 , R claim 1 , R claim 1 , Rare independently methyl or ethyl.3. The process of claim 2 , wherein R=R=R=hydrogen claim 2 , R=methyl and wherein each of R claim 2 , R claim 2 , Rare independently methyl or ethyl.4. The process of claim 1 , wherein step a) is carried out in the absence of a solvent.5. The process of claim 1 , wherein step a) is carried out in the presence of a solvent.6. The process of claim 5 , wherein the solvent is at least partially removed between steps a) and b).7. The process of claim 1 , wherein claim 1 , in step b) claim 1 , water is added in an amount of at least 1 weight-% based on the amount of compounds (II) and (III) used in step a).8. The process of claim 1 , wherein “partial removal” in step c) means removal of at least 50% of the water added in step b).9. The process of claim 1 , wherein pressure pis lower than the saturated vapour pressure of compound (III) at the temperature Tand higher than the saturated vapour pressure of (I) at the temperature T.10. The process of claim 1 , wherein steps b) and c) are carried out at least twice claim 1 , and wherein step b) is carried out with the high purity compound of formula (I) obtained in directly antecedent step c).11. The process of claim 2 , wherein said process is carried out in the absence of an organic solvent.12. The process of claim 11 , wherein in step b) water is added in an amount of at least 1 weight-% based on the amount of compounds (II) and (III) used in step a).13. The process of claim 12 , wherein “partial removal” in step c) means removal of at least 50% of the water added in step b).14. The process of claim 13 , wherein pressure pis lower than the saturated vapour pressure of compound (III) at the temperature Tand higher than the saturated vapour pressure of (I) at the ...

ELUXADOLINE CRYSTALLINE FORMS AND PROCESSES FOR THEIR PREPARATION

Novel crystalline forms of Eluxadoline, having the formula (I), are described. Also described are the processes for the preparation of said crystalline forms. 1. A polymorphically and chemically stable crystalline form α′ of 5-({[(2S)-2-amino-3-(4-carbamoyl-2 ,6-dimethylphenyl)propanoyl][(1S)-1-(4-phenyl-1H-imidazol-2-yl)ethyl]-amino}methyl)-2-methoxybenzoic acid having an X-ray powder diffraction pattern that , when collected with Kα radiation of copper (λ=1.5418 Å) comprises main peaks at 7.98° , 13.94° , 14.28° , 14.66° , and 19.04° 2θ±0.1° 2θ.3. A solvate form of 5-({[(2S)-2-amino-3-(4-carbamoyl-2 ,6-dimethylphenyl)propanoyl][(1S)-1-(4-phenyl-1H-imidazol-2-yl)ethyl]amino}methyl)-2-methoxybenzoic acid with a ketone selected from the group consisting of acetone , 2-butanone , 3-pentanone and mixtures thereof.4. The solvate form according to claim 3 , wherein the solvate form is an acetone solvate having unit cell parameters equal to the following cell dimensions: a=24.18 ű0.01 Å; b=17.10 ű0.01 Å claim 3 , c=9.62 ű0.01 Å; α=90 degrees claim 3 , β=90 degrees; γ=90 degrees.5. The solvate form according to claim 4 , wherein the solvate form in an X-ray powder diffraction pattern collected with Kα radiation of copper (λ=1.5418 Å) comprises main peaks at 6.33° claim 4 , 8.92° claim 4 , 9.86° claim 4 , 12.80° claim 4 , and 18.04°+0.1° 2θ.6. The solvate form according to claim 5 , wherein the X-ray powder diffraction pattern further comprises peaks at 7.280 claim 5 , 8.92° claim 5 , 13.82° claim 5 , and 15.06°+0.1° 2θ.7. The solvate form according to claim 4 , wherein the solvate form in a DSC thermogram performed with a heating ramp of 10° C./min comprises a first feature with maximum at 122.9° C.±4.0° C. claim 4 , an event with maximum at 173.7° C.±4.0° C. claim 4 , and a second feature with maximum at 196.6° C.±4.0° C.8. The solvate form according to claim 4 , wherein the solvate form in a TGA thermogram shows a weight loss step between 25° C. and 120° C. of up to ...

Derivatives of N-alkyl imidazoles

Compounds of the formula ##STR1## wherein R is lower alkyl; R 1 is substituted or unsubstituted phenyl or phenyl straight chain lower alkyl; R 2 is substituted or unsubstituted phenyl, phenyl straight chain lower alkyl or phenyl straight chain lower alkenyl; and wherein said substitution, solely in the phenyl ring of the aforesaid groups, comprises one or more substituents independently selected from the group consisting of lower alkyl, lower alkoxy, halo and trifluoromethyl; X is oxygen or sulfur; n is an integer of from 1 to 4 with the proviso that n cannot be 1 when X is oxygen and R 1 is phenyl or substituted phenyl; and the antimicrobial acid addition salts thereof are useful as antifungal antibacterial and antiprotozoal agents.

GROUP 8-10 TRANSITION METAL CATALYST FOR THE POLYMERIZATION OF OLEFINS

Organic sulfates as ionic liquids

The invention relates to novel ionic liquids of general formula [cation] [R'-SO4], wherein R' represents a branched or linear, saturated or unsaturated, aliphatic or alicyclic, functionalised or unfunctionalised hydrocarbon chain having between 3 and 36 carbon atoms. Said novel ionic liquids can, for example, be used as solvents or solvent additives in chemical reactions, as extracting agents or as heat transfer media.

Halogenide-free preparation of ionic fluids

Preparation of ionic liquids (I) involves alkylating an amine, phosphine, imidazole, pyridine, triazole or pyrazole corresponding to the cation of (I) with a sulfate diester (II), then replacing the sulfate anion by the anion of (I). Preparation of ionic liquids of formula (I) involves alkylating the amine, phosphine, imidazole, pyridine, triazole or pyrazole, corresponding to the cation A<+>, with a sulfate diester of formula (II), then replacing the sulfate anion R4SO4<-> or R5SO4<-> by the anion Yn-. (An)<+>.(Yn-) (I) R4SO2R5 (II) n = 1 or 2; Yn- = BF4<->, BCl4<->, PF6<->, SbF6<->, AsF6<->, AlCl4<->, ZnCl3<->, CuCl2<->, SO4<2->, CO3<2->, R'COO<->, R'SO3<-> or (R'SO2)2N<->; R' = 1-12C linear, branched or cyclic alkyl, 5-18C aryl, (5-18C) aryl-(1-6C) alkyl or (1-6C) alkyl-(5-18C) aryl (all optionally halo-substituted); A<-> = N<+>R1R2R3R or P<+>R1R2R3R; or 1-(R)-3-(R1)-imidazolium, (R1)-substituted 1-(R)-pyridinium, 1-(R)-2-(R1)-pyrazolium or 1-(R)-1,3,5-triazolium (all optionally ring-substituted by one or more of 1-6C alkyl, 1-6C alkoxy, 1-6C aminoalkyl, 5-12C aryl or (5-12C) aryl-(1-6C) alkyl); R1-R3 = H; 1-20C linear, branched or cyclic alkyl; Het or Het-(1-6C) alkyl; or Ar or Ar-(1-6C) alkyl; R, R4, R5 = 1-24C linear, branched or cyclic alkyl; Het-(1-6C) alkyl; or Ar'-(1-6C) alkyl; Het = heteroaryl containing 3-8C and at least one of N, O and S (optionally substituted by one or more of 1-6C alkyl and halo); Ar = 5-12C aryl (optionally substituted by one or more of 1-6C alkyl and halo); and Ar' = 5-24C aryl (optionally substituted by one or more of 1-6C alkyl and halo).

Group 8-10 transition metal olefin polymerization catalysts

Provided are certain transition metal complexes which are useful as catalysts in the polymerization of olefinic monomers. In particular, the invention provides complexes of certain bidentate ligands bonded to Ni, Pd, Co, or Fe, and optionally, one or more neutral Lewis acids, and their use in the polymerization of olefins. Suitable complexes include those of the following structure: wherein M represents the transition metal, and Q, T, L, W, Z, R 1 ,R 2 and R 10 represent functional groups.

Catalyst compositions for the polymerization of olefins

The present invention provides catalyst systems useful in the polymerization of olefins comprising a transition metal component and a ligand component comprising a Nitrogen atom and/or functional groups comprising a Nitrogen atom, generally in the form of an imine functional group. In certain embodiments, the ligand component may further comprise a phosphorous atom. Preferred ligand components are bidentate (bind to the transition metal at two or more sites) and include a nitrogen-transition metal bond from two imine groups. The transition metal-ligand complex is generally cationic and associated with a weakly coordinating anion. In a preferred embodiment, the catalyst system of the present invention further comprises a Lewis or Bronsted acid complexed with the ligand component of the transition metal-ligand complex.

Catalyst compositions for the polymerization of olefins

The present invention includes novel ligands which may be utilized as part of a catalyst system. A catalyst system of the present invention is a transition metal-ligand complex. In particular, the catalyst system includes a transition metal component and a ligand component comprising a Nitrogen atom and/or functional groups comprising a Nitrogen atom, generally in the form of an imine functional group. In certain embodiments, the ligand component may further comprise a phosphorous atom. Preferred ligand components are bidentate (bind to the transition metal at two or more sites) and include a nitrogen-transition metal bond. The transition metal-ligand complex is generally cationic and associated with a weakly coordinating anion. A catalyst system of the present invention may further comprise a Lewis or Bronsted acid. The Lewis or Bronsted acid may be complexed with the ligand component of the transition metal-ligand complex.,

Group 8-10 transition metal olefin polymerization catalysts

A composition comprising a boron or aluminum containing neutral Lewis acid and a compound of formula I or Ia: wherein R 1 and R 2 are each independently hydrocarbyl, substituted hydrocarbyl, or silyl; Q is (i) C—R 4 , where R 4 is hydrocarbyl, substituted hydrocarbyl, heteroatom connected hydrocarbyl, or heteroatom connected substituted hydrocarbyl, (ii) P(NH 2 ) 2 , or (iii) S(NH)(NH 2 ) or S(O)(OH); L is a monoolefin or a neutral Lewis base that can be displaced by a monoolefin; T is hydrogen, hydrocarbyl or substituted hydrocarbyl, or with L forms a π-allyl group; and M is Ni(II), Pd(II), Co(II) or Fe(II). The composition is useful as an olefin polymerization catalyst. Also described is a process for preparing a supported catalyst.

Microbicide

Novel 1-phenoxyphenyl-2-triazolylethanol ethers of the formula I <IMAGE> in which R1 is halogen, R2 is halogen or methyl and R3 is C1-C4-alkyl, C1-C4-haloalkyl, C2-C6-alkoxyalkyl, C3-C6-alkenyl, C3-C6-alkynyl or cyclopropyl and their phytophysiologically acceptable acid addition salts have outstanding microbicidal, in particular phytofungicidal, properties. They can be used for the control and/or preventive protection of crop plants against infections by microorganisms. The preparation of these active substances and compositions containing them are described.

CARBAMOILOXIALQUILAZOLES SUBSTITUTED BY N.

Un compuesto de la fórmula (III); (III), en donde, R1, es hidrógeno o alquilo, R2, es hidrógeno, alquilo, alquilcarboniloxialquilo, acoxicarbonilo, alquilcarbonilo, mono- ó dialquilminoalquil- carboniloxialquilo; R4 y R6, se seleccionan, de una forma independiente, de entre el grupo consistente en hidrógeno, halógeno, alquilo, alcoxi, alquiltio, alquilsulfinilo, alquilsulfonilo, carboxi, alcoxicarbonilo, ciano, trifluorometilo, trifluorometoxi, nitro, aminosulfonilo, o sulfo; R6, es hidroxi, alcoxicarbonilalquilamino, alcoxi- carbonilamino, amino, alquilamino, alquilcarboniloxi, alcoxicarbonilalquilamino-alquilcarboniloxi, alcoxicarbonil- amino-alquilcarboniloxi, alquilaminoalquilcarboniloxi, amino- alquilcarboniloxi, alquilcarbonilamino, alquilcarbonilalquil- amino, aciloxi, acilamino, acilalquilamino; el grupo es fenilo o piridini-2-ílo; X- es X- y, X-, es un anión farmacéutcimente aceptable, en donde, ¿acilo¿, se refiere a un residuo representado por la fórmula R7CO- ó (R8O)2PO-, en donde, R7, es hidrógeno, alcoxi, alquilo, el cual puede estar opcionalmente sustituido por carboxi, amino, alquilamino, dialquilamino, o fenilo, y R8, es hidrógeno o alquilo, ¿alquilo¿, se refiere a un radical hidrocarburo, saturado o insaturado, que tiene de 1 a 6 átomos de carbono, ¿alcoxi¿, se refiere a una cadena de -O-alquilo, lineal o ramificada, que tiene de 1 a 5 átomos de carbono, ¿halógeno¿, significa flúor, cloro o bromo y, ¿alquiltio¿, se refiere a un cadena de -S-alquilo, lineal o ramificada, que tiene de 1 a 4 átomos de carbono, así como sales, hidratos o solvatos, farmacéuticamente aceptables, de la fórmula (III). A compound of the formula (III); (III), wherein R1 is hydrogen or alkyl, R2 is hydrogen, alkyl, alkylcarbonyloxyalkyl, acoxycarbonyl, alkylcarbonyl, mono- or dialkyl aminoalkylcarbonyloxyalkyl; R4 and R6 are independently selected from the group consisting of hydrogen, halogen, alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, carboxy, alkoxycarbonyl, ...

Imidazolylalkylamine derivative and pharmaceutical composition thereof

An imidazolylalkylamine derivative represented by general formula (I) useful as a steroid 17-20 lyase, a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as the active ingredient, wherein R1 represents hydrogen or lower alkyl; A1 represents optionally branched lower alkylene; A2 represents optionally bonded or branched lower alkylene; R2 represents (un)substituted phenyl, (un)substituted bi- or tricyclic hydrocarbon ring having fused benzene ring(s); or (un)substituted bi- or tricyclic fused hetero ring having fused benzene ring(s) and a hetero ring containing oxygen and/or sulfur and/or nitrogen as the hetero atom(s); R3 represents alkyl, lower alkenyl, lower alkynyl, cycloalkyl, -A3-R4, halogen-substituted lower alkyl, cyano-substituted lower alkyl, or (un)substituted hetero ring containing nitrogen as the hetero atom(s); A3 represents optionally branched lower alkylene or carbonyl; and R4 represents (un)substituted cycloalkyl, (un)substituted phenyl, or (un)substituted hetero ring containing nitrogen as the hetero atom(s); provided (1) -A?2-R2 and -R3¿ may be combined with the adjacent nitrogen atom to form (un)substituted tri- or tetracyclic fused hetero ring, and (2) when -A2-R2 represent (un)substituted phenyl or benzyl, (a) is bonded to the 4- or 5- position of the imidazole ring.

Isocyanates blocked with 1-amino-alkyl imidazoles as epoxy curing agents

Novel curing agents for heat-curable single package epoxy resins, the agents being adducts of aminoalkyl imidazoles with isocyanates. Cures are effected on heating the epoxy resin for times as short as 5 seconds.

Catalyst compositions for the polymerization of olefins

The present invention includes novel ligands which may be utilized as part of a catalyst system. A catalyst system of the present invention is a transition metal-ligand complex. In particular, the catalyst system includes a transition metal component and a ligand component comprising a Nitrogen atom and/or functional groups comprising a Nitrogen atom, generally in the form of an imine functional group. In certain embodiments, the ligand component may further comprise a phosphorous atom. Preferred ligand components are bidentate (bind to the transition metal at two or more sites) and include a nitrogen-transition metal bond. The transition metal-ligand complex is generally cationic and associated with a weakly coordinating anion. A catalyst system of the present invention may further comprise a Lewis or Bronsted acid. The Lewis or Bronsted acid may be complexed with the ligand component of the transition metal-ligand complex.

Catalyst compositions for the polymerization of olefins

The present invention provides catalyst systems useful in the polymerization of olefins comprising a transition metal component and a ligand component comprising a Nitrogen atom and/or functional groups comprising a Nitrogen atom, generally in the form of an imine functional group. In certain embodiments, the ligand component may further comprise a phosphorous atom. Preferred ligand components are bidentate (bind to the transition metal at two or more sites) and include a nitrogen-transition metal bond. The transition metal-ligand complex is generally cationic and associated with a weakly coordinating anion. In a preferred embodiment, the catalyst system of the present invention further comprises a Lewis or Bronsted acid complexed with the ligand component of the transition metal-ligand complex.

Processo para preparação de 2,4-oxazolidinadionas e intermediário

CATALYST COMPOSITIONS FOR THE POLYMERIZATION OF OLEFINS

Indan- und tetralinderivate

Compound process for preparing same composition containing same and method of inhibiting mould

Derivatives of thienyl- and furyl-substituted N-butyl and N-phenyl imidazoles

The compounds of the present invention are represented by the formula ##STR1## wherein R 1 and R 2 are the same or different and are optionally substituted furyl or thienyl the substituents independently selected from the group halo, C 1 to C 6 alkyl and C 1 to C 6 alkoxy or optionally substituted phenyl the substituents independently selected from the group halo, C 1 to C 4 alkyl, C 1 to C 4 alkoxy and trifluoromethyl; X is oxygen or sulfur; m is the integer 0; and n is the integer 2 or 3; and the antimicrobial acid addition salts thereof, with the proviso that when either R 1 or R 2 is said optionally substituted phenyl the other R 1 or R 2 is said optionally substituted furyl or thienyl. The compounds are useful for combatting fungi, bacteria and protozoa. They also have spermatocidal and spermatostatic activity.

Microbicidal triazolyl-ethyl-ethers

Novel substituted azolyl-ethyl ethers of the general formula I <IMAGE> wherein R1 is phenyl, phenyl mono- to trisubstituted by halogen, C1-C3- haloalkyl, nitro, C1-C3-alkoxy, C1-C8-alkyl and/or cyano, or phenyl substituted by phenyl or phenoxy, naphthyl, or naphthyl mono- or -disubstituted by halogen, nitro and/or C1-C3-alkyl, benzyl, or benzyl mono- or disubstituted by halogen, nitro and/or C1-C3-alkyl; R2 is phenyl, phenyl mono- to trisubstituted by halogen, C1-C3-haloalkyl, nitro, C1-C3-alkoxy, C1-C8-alkyl and/or cyano, or phenyl substituted by phenyl or phenoxy, or it is C1-C10-alkyl, C3-C8-cycloalkyl or C3-C8- cycloalkyl-(C1-C4-alkyl); R3 is C1-C12-alkyl, C2-C4-alkenyl, C3-C4-alkynyl, benzyl, or benzyl mono- or disubstituted by halogen, nitro and/or C1-C3-alkyl; and R4 is an azolyl group; including acid addition salts thereof, quaternary azolium salts and metal complexes, are used in agrochemical compositions for the preventive and curative combating of harmful microorganisms.

Ether derivatives from substituted 1-hydroxyalkyl azoles, process for their preparation as well as their use as fungicides and plant-growth regulators

Die Erfindung betrifft neue Ether-Derivate von substituierten 1-Hydroxyalkyl-azolen, ein Verfahren zu ihrer Herstellung sowie ihre Verwendung als Fungizide und Pflanzenwachstumsregulatoren. Die Verbindungen der allgemeinen Formel <IMAGE> in welcher A, B, R¹, R², Z und m die in der Beschreibung angegebene Bedeutung besitzen, werden erhalten, wenn man Alkoholate von 1-Hydroxylalkyl-azolen mit einem Halogenid R² - Hal in Gegenwart eines Verdünnungsmittels umsetzt, und gegebenenfalls anschließend an die so erhaltenen Verbindungen der Formel (I) eine Säure oder ein Metallsalz addiert. Die Wirkstoffe sind für den Gebrauch als Pflanzenschutzmittel geeignet und können mit besonders gutem Erfolg zur Bekämpfung solcher Pilze eingesetzt werden, die echte Mehltauerkrankungen hervorrufen. Die Wirkstoffe greifen ferner in den Metabolismus der Pflanzen ein und können deshalb als Wachstumsregulatoren eingesetzt werden. The invention relates to new ether derivatives of substituted 1-hydroxyalkyl-azoles, a process for their preparation and their use as fungicides and plant growth regulators. The compounds of the general formula <IMAGE> in which A, B, R¹, R², Z and m have the meaning given in the description are obtained if alcoholates of 1-hydroxylalkyl-azoles with a halide R² - Hal in the presence of a Reacts diluent, and then optionally adds an acid or a metal salt to the compounds of formula (I) thus obtained. The active ingredients are suitable for use as crop protection agents and can be used with particularly good success to combat those fungi which cause real mildew diseases. The active substances also interfere with the metabolism of the plants and can therefore be used as growth regulators.

Antimycosic agent

1. Antimycotic agent, characterised in that it contains at least one ether derivative of a substituted 1-hydroxyalkyl-azolyl derivative of the general formula : see diagramm : EP0085843,P11,F1 in which B represents oxygen, sulphur or the CH2 group ; R**1 represents the groupings : see diagramm : EP0085843,P11,F2 and see diagramm : EP0085843,P11,F3 or represents cycloalkyl which has 3 to 7 carbon atoms and is optionally substituted by alkyl with 1 to 2 carbon atoms, and optionally substituted phenyl, the following being mentioned as substituents : halogen, alkyl with 1 to 4 carbon atoms and halogenoalkyl with 1 to 2 carbon atoms and 1 to 5 identical or different halogen atoms ; X**1 represents hydrogen or halogen, X**2 represents halogen ; Y represents alkyl, alkoxy, alkylthio, halogeno-alkoxy, halogenoalkylthio, alkenyl with up to 6 carbon atoms, alkoxycarbonyl with 1 to 4 carbon atoms in the alkyl part, cyano and optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy with 1 to 4 carbon atoms in the alkyl part and phenylalkylthio with 1 to 4 carbon atoms in the alkyl part, the following being mentioned as phenyl substituents in each case : halogen, alkyl with 1 to 4 carbon atoms ; alkoxy and alkylthio with in each case 1 to 2 carbon atoms ; halogenoalkyl, halogenoalkoxy and halogenoalkylthio with in each case 1 to 2 carbon atoms and 1 to 5 identical or different halogen atoms, cyclohexyl, dialkylamino with 1 to 4 carbon atoms in each alkyl part, nitro, cyano and alkoxycarbonyl with 1 to 4 carbon atoms in the alkyl part ; n represents the numbers 0, 1 or 2 ; Z represents halogen, alkyl with 1 to 4 carbon atoms, cycloalkyl with 5 to 7 carbon atoms, alkoxy and alkylthio with in each case 1 to 4 carbon atoms, halogenoalkyl and halogenoalkoxy and halogenoalkylthio with in each case 1 to 2 carbon atoms and 1 to 5 identical or different halogen atoms, and phenyl, phenoxy and phenylalkyl and phenylalkoxy with 1 to 2 carbon atoms in the alkyl part or in the alkoxy ...

Fungicidally active 3-substituted 1-azolyl-3-methyl-1-phenoxy-butan-2-ones and -ols

New 3-substituted 1-azolyl-3-methyl-1-phenoxy-butan-2-ones and -ols of the general formula ##STR1## in which Az represents 1,2,4-triazol-1-yl, 1,2,4-triazol-4-yl or imidazol-1-yl, B represents the keto group or the CH(OH) group, Y represents oxygen or sulphur, R represents halogenoalkyl, optionally substituted phenyl or optionally substituted benzyl, or provided Y represents sulphur, may represent alkyl and X 1 , X 2 and X 3 are selected independently and each represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, alkylthio, alkylsulphonyl, nitro, cyano, alkoxycarbonyl or optionally substituted phenyl, are obtained if halogenoether ketones are reacted with 1,2,4-triazole or imidazole in the presence of a diluent and of an acid-binding agent, and, if appropriate, the keto derivatives thus obtained are reduced. The compounds, as such or as their acid-addition salts or metal-salt complexes, have fungicidal activity, for example against those fungi which cause powdery mildew diseases or cause rice diseases.

1-(beta-aryl-beta-(r-oxy)-ethyl)-imidazoles

THE COMPOUNDS ARE OF THE CLASS OF 1(B-ARYL-B-(R-OXY)ETHYL)-IMIDAZOLES, WHEREIN R IS ALKYL, ALKENYL, PHENYLALKENYL, HALOPHENYL ALKENYL OR ALKYNYL, USEFUL FOR THEIR ANTI-FUNGAL AND ANTI-BACTERIAL ACTIVITY.

1-{8 {62 -(1-adamantyloxy)halophenethyl{9 {0 imidazoles and congeners

Preparation of 1-( (3-(1-adamantyloxy)phenethyl)imidazoles and congeners- for example, 1-( Beta -(1-adamantyloxy)-4chlorophenethyl)imidazole oxalate- and 3-(1-adamantyl)-1-( ( Beta -hydroxyl)halophenethyl) imidazolium bromide by-products, together with biological properties thereof including antibacterial, antiprotozoal, anthelmintic, antifungal, and antialgal activities, are disclosed.

1-(beta-aryl)ethyl-imidazole derivatives

THE COMPOUNDS ARE OF THE CLASS OF 1-(B-ARYL)ETHYLIMIDAZOLE ETHERS AND AMINES USEFUL FOR THEIR ANTI-FUNGAL AND ANTI-BACTERIAL ACTIVITY.

Phenyl-imidazolylalkanyl derivatives

PHENYL-IMIDAZOLYLALKANYL DERIVATIVES ARE ANTIMYCOTIC AGENTS. THEY ARE PREPARED BY A NUMBER OF PROCESSES INCLUDING ACYLATION OR SULFONYLATION OF A PHENYL-IMIDAZOLYLALKANOL, TREATMENT OF A PHENYL-ALKANYL-CARBINOL WITH A DIIMIDAZOLLYL SULFONE, OXIDATION OF A PHENYL-IMIDAZOLYLALKYLMERCAPTAN OR REDUCTION OF A PHENYL-IMIDAZOLYLALKYLANOTE OR ALKANONITRILE. A TYPICAL EMBODIMENT IS 1-(1,1-DIPHENYL-2-ACETOXYETHYL) IMIDAZOLE.

Suebstitueye azolil-etil-eter ve bunlarin asit ilavesi tuzlari,kuaterner azolium tuz lari ve metal kompleksleri bun larin hazirlanisini ve mikrobisid madde olarak kullanilmasi

Ether derivatives of substituted 1-hydroxyalkyl- azoles as fungicides and plant growth regulators

Compounds which are ether derivatives of substituted 1-hydroxyalkyl-azoles, of the general formula ##STR1## in which A represents a nitrogen atom or a CH group, B represents oxygen, sulphur or a CH 2 group, R 1 represents a substituted alkyl, optionally substituted cycloalkyl or optionally substituted phenyl radical or, if either A represents a nitrogen atom, or if A represents the CH group and at the same B represents oxygen or sulphur, R 1 also represents an unsubstituted alkyl radical, R 2 represents an alkyl, alkenyl, alkinyl, optionally substituted phenyl or optionally substituted benzyl radical, Z represents a halogen atom or an alkyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, optionally substituted phenoxy, optionally substituted phenylalkyl or optionally substituted phenylalkoxy radical and m is 0, 1, 2 or 3, and acid addition salts and metal salt complexes thereof, are novel, are prepared as described, and find use as fungicides and as agents for regulating plant growth.

Ether derivatives from substituted 1-hydroxyalkyl azoles, process for their preparation as well as their use as fungicides and plant-growth regulators

Ether derivatives of substituted 1-hydroxyalkyl-azoles as fungicides and plant growth regulators

Compounds which are ether derivatives of substituted 1-hydroxyalkyl-azoles, of the general formula ##STR1## in which A represents a nitrogen atom or a CH group, B represents oxygen, sulphur or a CH 2 group, R 1 represents a substituted alkyl, optionally substituted cycloalkyl or optionally substituted phenyl radical or, if either A represents a nitrogen atom, or if A represents the CH group and at the same B represents oxygen or sulphur, R 1 also represents an unsubstituted alkyl radical, R 2 represents an alkyl, alkenyl, alkinyl, optionally substituted phenyl or optionally substituted benzyl radical, Z represents a halogen atom or an alkyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, optionally substituted phenoxy, optionally substituted phenylalkyl or optionally substituted phenylalkoxy radical and m is 0, 1, 2 or 3, and acid addition salts and metal salt complexes thereof, are novel, are prepared as described, and fine use as fungicides and as agents for regulating plant growth.

Substituted diazolylalkyl or triazolylalkyl carbinols, process for their preparation and their use as antimycotic compounds

1. Substituted di- or triazolylalkyl-carbinols of the general formula see diagramm : EP0120276,P20,F1 in which A represents a nitrogen atom or the CH group ; B represents a nitrogen atom or the CH group ; X represents hydrogen and straight-chain or branched alkyl with 1 to 6 carbon atoms ; Y represents straight-chain or branched alkyl with 1 to 6 carbon atoms ; and, if X represents hydrogen, also straight-chain or branched alkenyl and alkinyl with in each case 3 to 6 carbon atoms and benzyl which is optionally mono- to trisubstituted in the phenyl part by identical or different substituents, substituents which may mentioned being : halogen, alkyl with 1 to 4 carbon atoms, alkoxy and alkylthio with in each case 1 to 4 carbon atoms, halogenoalkyl, halogenoalkoxy and halogenoalkylthio with in each case 1 to 2 carbon and 1 to 5 identical or different halogen atoms, such as preferably fluorine and chlorine atoms, nitro and cyano ; R represents phenyl which is optionally mono- to tri-substituted by identical or different substituents, preferred substituents which may be mentioned being : halogen, alkyl with 1 to 4 carbon atoms, alkoxy and alkylthio with in each case 1 to 4 carbon atoms, halogenoalkyl, halogenoalkoxy and halogenoalkylthio with in each case 1 to 2 carbon and 1 to 5 identical or different halogen atoms, such as preferably fluorine and chlorine atoms, nitro, cyano, hydroxyl, hydroxycarbonyl with 1 to 4 carbon atoms in the alkyl part, hydroximinoalkyl with 1 to 4 carbon atoms, alkoximinoalkyl with 1 to 4 carbon atoms in each alkyl part, and phenyl, phenoxy, benzyl and benzyloxy, each of which is optionally substituted by halogen and/or alkyl with 1 to 2 carbon atoms ; R furthermore preferably represents the grouping see diagramm : EP0120276,P20,F2 wherein Alk**1 represents straight-chain or branched alkyl with 1 to 4 carbon atoms ; Alk**2 represents straight-chain or branched alkyl with 1 to 4 carbon atoms ; Alk**1 and Alk**2, together with the carbon atom to ...

Imidazolyl vinyl ethers having fungicidal and bactericidal activity

Aryl-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: <IMAGE> Ar in the formula represents a substituted or unsubstituted aryl or heterocyclic radical; R represents hydrogen or a C1-C12 alkyl or cycloalkyl (saturated or unsaturated) or Ar as above; Im represents a 1-H-imidazol-1-yl group (unsubstituted or substituted); and Y represents a saturated or unsaturated, acyclic or cyclic C1-C12 alkyl, or aryl or aralkyl, or an alkyl or alkylene residue directly bound to the ether oxygen and having a chain once or twice interrupted by -O-, -S-, -SO- or -SO2- bridges. These compounds are effective wide spectrum fungicides and bactericides. [US4210657A]

Patent DE2633492C2

FUNGICIDAL AGENTS

Cyclopropyl-substituted azolyl methyl carbinoles, process for their preparation and their use as therapeutic agents

The present invention relates to 1-cyanocyclopropyl- and 1-carboxamido-cyclopropyl-azolylmethylcarbinol derivatives, process for the preparation thereof and the use thereof in medicaments, especially for mycoses.

1-phenethylimidazole derivatives

ABSTRACT 1-Phenethylimidazole compounds of the formula: wherein R4 and R5 are independently hydrogen or halogen, and Z is a mono or disubstituted phenyl moiety of the formula:

1-(2,2-bis-thioethyl)1-h-imidozole compounds

Abstract of the Disclosure Novel imidazole mercaptals of the formula I wherein each m is independently zero or one; and R1 and R2 each are independently selected from (lower)alkyl, cyclo-alkyl, cycloalkyl(lower)alkyl, phenyl, phenyl(lower)alkyl, thienyl, thienyl(lower)alkyl, pyridyl and pyridyl(lower)-alkyl, in which the phenyl and heterocyclic rings optionally may contain from 1 to 3 substituents, and acid addition salts thereof, are useful antimicrobial agents.

Thioketal substituted n-alkyl imidazoles and pharmaceutical compositions containing them

Derivatives of substituted n-alkyl imidazoles, their preparation and these compounds for pharmaceutical use

Group 8-10 transition metal olefin polymerization catalysts

Provided are certain transition metal complexes which are useful as catalysts in the polymerization of olefinic monomers. In particular, the invention provides complexes of certain bidentate ligands bonded to Ni, Pd, Co, or Fe, and optionally, one or more neutral Lewis acids, and their use in the polymerization of olefins.

Olefin polymerization catalysts containing group 8-10 transition metals, bidentate ligands, processes employing such catalysts and polymers obtained therefrom

Methods for preparing olefin polymers, or oligomers catalysts for preparing olefin polymers and bidentate ligand used for preparing these catalysts are disclosed. The polymers can be prepared containing the corresponding monomers with a Group 8-10 transition metal catalyst. The polymers are suitable for processing in conventional extrusion processes, and can be formed into high barrier sheets or films, or low molecular weight resins for use in synthetic waxes in wax coatings or as emulsions.

Group 8-10 transition metal olefin polymerization catalysts

Provided are certain transition metal complexes which are useful as catalysts in the polymerization of olefinic monomers. In particular, the invention provides complexes of certain bidentate ligands bonded to Ni, Pd, Co, or Fe, and optionally, one or more neutral Lewis acids, and their use in the polymerization of olefins.

[UNK]

Group 8-10 transition metal olefin polymerization catalysts

Provided are certain transition metal complexes which are useful as catalysts in the polymerization of olefinic monomers. In particular, the invention provides complexes of certain bidentate ligands bonded to Ni, Pd, Co, or Fe, and optionally, one or more neutral Lewis acids, and their use in the polymerization of olefins.

第８〜１０族遷移金属オレフィン重合触媒

(57)【要約】 オレフィンモノマーの重合で触媒として有用な、ある種の遷移金属錯体が供給される。詳しくは、本発明は、Ni，Pd，Co又はFeに結合したある種の二座配位子及び任意的な１種又はそれ以上の中性ルイス酸の錯体並びにオレフィンの重合に於けるその使用を提供する。

Group 8-10 transition metal olefin polymerization catalysts

Provided are certain transition metal complexes which are useful as catalysts in the polymerization of olefinic monomers. In particular, the invention provides complexes of certain bidentate ligands bonded to Ni, Pd, Co, or Fe, and optionally, one or more neutral Lewis acids, and their use in the polymerization of olefins.

The method of obtaining derivatives of phenylimidazolyl

Process for preparation of 1-benzylimidazole compound, and novel compound

내용없음. None.

一种咪唑类不饱和离子液体及其制备方法

本发明涉及一种咪唑类不饱和离子液体及其制备方法，将卤代试剂单体和烯基咪唑分别加入到溶剂中，在10～70℃下反应得到目标离子液体。所合成离子液体的咪唑两端侧链分别带有双键，丰富了可聚离子液体的种类，为离子液体作为可聚合单体、交联剂及在催化和分离等领域中的应用提供了更多的选择。本发明所合成的离子液体具有良好的水溶性，在生物领域具有潜在的应用价值。

Способ получения энантиомерно чистого 6-[(4-хлорфенил)-(1h-1,2,4-триазол-1-ил)метил]-1-метил-1н-бензотриазола, промежуточные соединения для их получения и способ их получения

Предлагается способ получения (+)-6-[(4-хлорфенил) (1-1,2,4 -триазол-1-ил)метил] -1-метил-1H-бензотриазола, включающий расщепление (±)-6-[(4-хлорфенил)гидразинометил]-1-метил-1H-бензотриазола и превращение проходящего энантиомерно чистого промежуточного гидразина в (+)-6-[(4-хлорфенил)(1H-1,2,4-триазол-1-ил)метил] -1-метил-1H-бензотриазол. Предложены также новые промежуточные соединения для получения целевых соединений и способы их получения.

Optically active hydroxybenzylamine derivative, optically active

내용 없음. No content.

Method for preparing 1,2,4-triazole derivatives

1-Alkoxy-1-azolylmethyloxirane, process for their preparation and their use as crop protection agents.

Patent SU408476A3

Use of polyacids to treat mineral fertilizers containing a nitrification inhibitor

THE USE OF INORGANIC OR ORGANIC POLYACIDS FOR THE TREATMENT OF INORGANIC FERTILIZERS, IN PARTICULAR THE USE OF THE POLYACIDS AS A MIXTURE WITH AT LEAST ONE NITRIFICATION INHIBITOR FOR THE TREATMENT OF INORGANIC FERTILIZERS; THE USE OF SELECTED PYRAZOLE DERIVATIVES AS NITRIFICATION INHIBITOR IN INORGANIC FERTILIZERS AND ALSO AS STABILIZERS OF LIQUID MANURE OR LIQUID FERTILIZER FORMULATIONS, AS WELL AS THE CORRESPONDING TREATED INORGANIC FERTILIZERS PER SE; AND NOVEL PYRAZOLE DERIVATIVES WHICH CAN BE USED AS NITRIFICATION INHIBITORS IN INORGANIC FERTILIZERS AND ALSO AS STABILIZERS OF LIQUID MANURE OR LIQUID FERTILIZER FORMULATIONS ARE DESCRIBED.

Process for preparing 2,4-oxazolidinediones

一种环丙基酰肼和甲氧苯类gpr119激动剂、制备方法及其用途

本发明涉及与II型糖尿病相关的药物领域。具体而言，本发明涉及一种含环丙基酰肼和甲氧基苯类结构的GPR119激动剂、其制备方法以及在制备2型糖尿病药物中的应用。

Method of producing n-cyclo-alkymethyl-2-phenylamino-imidazolines-2- or salts thereof

Method of heterocyclic compound synthesis

FIELD: chemistry. SUBSTANCE: invention concerns method of obtaining heterocycles of formula I , where X, A, R10-R17 are as defined in point 1 of the claim, while a) isothiocyanate of formula II is transformed into thiourea of formula IV by interaction with primary amine of formula III, and b) thiourea of formula IV is transformed into compound of formula I by interaction with sulfochloride R6SO 2 Cl in the presence of a base, where A, X, n, m and R10 to R17 in compounds of formulae II, III and IV are as defined in formula I, and R6 is (C 1 -C 4 )-alkyl, trifluoromethyl or phenyl non-sustituted or substituted by methyl, trifluoromethyl, F, CI, Br or polymer carreir. The transportation is shown by combination formulae EFFECT: new multipurpose synthesis technique for heterocyclic compounds of the general formula I. 8 cl, 31 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2 346 936 (13) C2 (51) ÌÏÊ C07D 233/50 C07D 265/08 C07D 235/30 C07D 413/12 C07D 277/18 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ C07D 265/18 ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ,C07D 409/12 ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ C07D 495/04 (12) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2005140090/04, 10.05.2004 (72) Àâòîð(û): ÕÀÉÍÅËÜÒ Óâå (DE), ËÀÍà Õàíñ-Éîõåí (DE) (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 10.05.2004 (43) Äàòà ïóáëèêàöèè çà âêè: 20.04.2006 2 3 4 6 9 3 6 (45) Îïóáëèêîâàíî: 20.02.2009 Áþë. ¹ 5 2 3 4 6 9 3 6 R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 22.12.2005 C 2 C 2 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: KIM Ò. Í. et al. A mild cyclodesulfurization of N-(2-hydroxyethyl)-N'phenylthioureas to 2-phenylamino-2-oxazolines using TsCl/NaOH, TETRAHEDRON, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol.57, ¹33, 13.08.2001 p.7137-7141. SU 677655 A3, 30.07.1979. (86) Çà âêà PCT: EP 2004/004955 (10.05.2004) (87) Ïóáëèêàöè PCT: WO 2004/103976 (02.12.2004) Àäðåñ äë ïåðåïèñêè: 129090, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ ...

Borate-based base generator, and base-reactive composition comprising such base generator

에폭시계 화합물 등의 염기 반응성 화합물과 혼합한 상태로 장기간 보존한 경우에도 당해 염기 반응성 화합물과 반응하는 일이 없어 보존안정성이 높은 조성물로 할 수 있으며, 또한 광(활성 에너지선)의 조사나 가열에 의해 강염기(구아니딘류, 비구아니드류, 포스파젠류 또는 포스포늄류)를 발생할 수 있는 화합물, 이들을 포함하여 이루어지는 염기 발생제 및 당해 염기 발생제와 염기 반응성 화합물을 함유하는 염기 반응성 조성물을 제공하는 것을 과제로 한다. 본 발명은 일반식 (A)로 표시되는 화합물, 당해 화합물을 포함하여 이루어진 염기 발생제, 당해 염기 발생제 및 염기 반응성 화합물을 함유하는 것을 특징으로 하는 염기 반응성 조성물 등에 관한 것이다. (식 중, R 1 은 알킬기; 할로겐 원자, 알킬기, 알콕시기, 또는 알킬티오기로 치환되어 있어도 좋은 아릴알키닐기; 알케닐기; 2-퓨릴에티닐기; 2-티오페닐에티닐기; 또는 2,6-디티아닐기를 나타내고, R 2 ~R 4 는 각각 독립적으로 알킬기; 할로겐 원자, 알킬기, 알콕시기, 또는 알킬티오기로 치환되어 있어도 좋은 아릴알키닐기; 할로겐 원자, 알킬기, 알콕시기, 또는 알킬티오기로 치환되어 있어도 좋은 아릴기; 퓨라닐기; 티에닐기; 또는 N-알킬 치환 피롤릴기를 나타내고, Z + 는 구아니디늄기, 비구아니듐기 또는 포스파제늄기를 갖는 암모늄 양이온, 혹은 포스포늄 양이온을 나타낸다.) Even when stored for a long period of time in a state of mixing with a base-reactive compound such as an epoxy-based compound, it does not react with the base-reactive compound, resulting in a composition with high storage stability. To provide a compound capable of generating a strong base (guanidine, biguanide, phosphazene or phosphonium) by make it a task The present invention relates to a compound represented by the general formula (A), a base generator comprising the compound, a base-reactive composition comprising the base generator and a base-reactive compound, and the like. (wherein, R 1 is an alkyl group; an arylalkynyl group optionally substituted with a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group; an alkenyl group; a 2-furylethynyl group; a 2-thiophenylethynyl group; or 2, represents a 6-dithianyl group, and R 2 to R 4 are each independently an alkyl group; an arylalkynyl group optionally substituted with a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group; a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group optionally substituted aryl; furanoid group; a thienyl group; or a substituted alkyl N- pyrrolyl, Z + represents an ammonium cation, or a phosphonium cation having guanidinyl nyumgi, acetabular no dyumgi ...

3-cyclyl-5-(nitrogen-containing 5-membered ring) methyl-oxazolidinone derivatives and their use as antibacterial agents

Disclosed are compounds of formula (I), wherein: -N-HET is (Id) or (If), R1 is an alkyl group, Q is Q1 or Q2, and the remaining substituents are defined herein. The compounds are used in the manufacture of medicaments for use as antibiotics.

METHOD OF OBTAINING DERIVATIVE PHENYLIMIDAZOZYLALKANES

Гербицидное средство

１，２，４−トリアゾ−ル誘導体および農園芸用殺菌剤

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Method of producing 2-bromo-6-fluoro-n-2-imidazolidinylidene-benzamine or its salt

ヒドロキシベンズアルドキシムｏ−エ−テルの製造法

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Способ получени замещенных 2-ариламиноимидазолинов-(2)

Processes for the preparation of fluorazolyl propan derivatives

A process for prepg. fluoroazolylpropane of formula (I) and its acid addn. salts, quaternary azollynium salts and metal complex salts comprise (i) reacting fluoroazolyl methyl oxirane with alcohol or thioalcohol of formula H-X-R5 in the presence of base in an inert solvent and (ii) etherification or esterification of the product. In the formula, Az is imidazol-1-yl or 1,2,4triazol-1-yl; R1 is H, Me, Et or mono-substd. benzyl by F or Cl; R2 is t-Bu; R3 is H, me or acetyl; R5 is n-Bu, Ph or mono- or di-substd. Ph; X is O or S; Y is halogen or org. or inorg. acid radical.

The way to fight fungi

1-아릴-2-플루오로-2-아졸릴 알카논 및 알칸올의 제조방법

내용 없음.

Itraconazole and saperconazole stereoisomers

본 발명은 일반식 (시스-(Ⅰ))로 표시될 수 있는 이트라코나졸(X=Cl) 및 사퍼코나졸(X=F)의 입체이성체, 및 그의 약제학적으로 허용되는 산 부가염, 이들 입체이성체의 제조방법, 이들 입체이성체와 사이클로덱스트린의 복합체, 이 복합체를 함유하는 약제학적 조성물, 및 이들 복합체 및 약제학적 조성물을 제조하는 방법에 관한 것이다. The present invention relates to stereoisomers of itraconazole (X = Cl) and saperconazole (X = F), which can be represented by the general formula (cis- (I)), and pharmaceutically acceptable acid addition salts thereof, these stereoisomers It relates to a process for the preparation of these compounds, complexes of these stereoisomers and cyclodextrins, pharmaceutical compositions containing these complexes, and methods of preparing these complexes and pharmaceutical compositions. 상기식에서, 세 개의 *는 세개의 키랄 중심(chiral center)을 나타내며, '시스'는 (1H-1,2,4-트리아졸-1-일메틸) 부위를 의미하고, Wherein three * represent three chiral centers, 'cis' means (1H-1,2,4-triazol-1-ylmethyl) moiety, 치환된 페녹시 부위는 1,3-디옥솔란 환에 의해 규정되는 평면상의 동일한 면에 위치한다. The substituted phenoxy moiety is located on the same side of the plane defined by the 1,3-dioxolane ring.

Ｎ−〔１−トリアゾ−ル−（１）−イル−２，２，２−トリクロロエチル〕−置換アミド誘導体及び該誘導体を含有するうどんこ病防除剤

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Tetrahydrofuran antifungals

A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R 1 is a straight or branched chain (C 3 to C 8 ) alkyl group substituted by one or two phosphate ester groups (e.g., a phosphate ester convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.

Производные 3-циклического-5-(азотсодержащего 5-членного кольцевого) метил-оксазолидинона и их применение в качестве антибактериальных средств

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (51) ÌÏÊ 7 (11) 2004 129 276 (13) A C 07 D 413/14 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2004129276/04, 25.02.2003 (71) Çà âèòåëü(è): ÀÑÒÐÀÇÅÍÅÊÀ ÀÁ (SE) (30) Ïðèîðèòåò: 28.02.2002 US 60/360,957 (43) Äàòà ïóáëèêàöèè çà âêè: 10.06.2005 Áþë. ¹ 16 (86) Çà âêà PCT: GB 03/00785 (25.02.2003) (74) Ïàòåíòíûé ïîâåðåííûé: Âåñåëèöêà Èðèíà Àëåêñàíäðîâíà Àäðåñ äë ïåðåïèñêè: 101000, Ìîñêâà, Ì.Çëàòîóñòèíñêèé ïåð., ä.10, êâ.15, "ÅÂÐÎÌÀÐÊÏÀÒ", È.À.Âåñåëèöêîé (54) ÏÐÎÈÇÂÎÄÍÛÅ 3-ÖÈÊËÈ×ÅÑÊÎÃÎ-5-(ÀÇÎÒÑÎÄÅÐÆÀÙÅÃÎ 5-×ËÅÍÍÎÃÎ ÊÎËÜÖÅÂÎÃÎ) Ôîðìóëà èçîáðåòåíè 1. Ñîåäèíåíèå ôîðìóëû (I), èëè åãî ôàðìàöåâòè÷åñêè ïðèåìëåìà ñîëü, èëè ñëîæíûé ýôèð, êîòîðûé ñïîñîáåí ê ãèäðîëèçó â óñëîâè õ in vivo A ãäå -N-HET âûáðàí èç íèæåïðèâåäåííûõ ñòðóêòóð (la)-(If): R U 2 0 0 4 1 2 9 2 7 6 A ÌÅÒÈË-ÎÊÑÀÇÎËÈÄÈÍÎÍÀ È ÈÕ ÏÐÈÌÅÍÅÍÈÅ Â ÊÀ×ÅÑÒÂÅ ÀÍÒÈÁÀÊÒÅÐÈÀËÜÍÛÕ ÑÐÅÄÑÒ Ñòðàíèöà: 1 RU 2 0 0 4 1 2 9 2 7 6 (87) Ïóáëèêàöè PCT: WO 03/072575 (04.09.2003) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 28.09.2004 (72) Àâòîð(û): Ìàéêë Áàððè ÃÐÅÉÂÑÒÎÊÊ (US), Íèë Äæåéìñ ÕÅÉËÑ (US), Ôîëüêåðò ÐÅÊÊ (US), Ôåé ÄÆÎÓ (US), Ïîë Ðîáåðò ÔËÅÌÈÍà (US), Äàíèåë Ðîáåðò ÊÀÐÊÀÍÀÃÜÞ (US), Ìàðê Ìèøåëü ÆÈÐÀÐÄÎ (US) ãäå u è v íåçàâèñèìî ïðåäñòàâë þò ñîáîé 0 èëè 1; R1 ïðåäñòàâë åò ñîáîé Ñ1-Ñ4-àëêèëüíóþ ãðóïïó; Q âûáðàí èç Q1-Q6: 2 0 0 4 1 2 9 2 7 6 R U A Ñòðàíèöà: 2 2 0 0 4 1 2 9 2 7 6 A R U ãäå R 2 è R 3 íåçàâèñèìî âûáðàíû èç Í, F, Cl, CF3, ÎÌå, SMe, Me è Et; B1 ïðåäñòàâë åò ñîáîé Î èëè S; Ò âûáðàí èç ãðóïï â (ÒÀ) - (ÒÅ), óêàçàííûõ íèæå (ãäå AR1, AR2, AR2a, AR2b, AR3, AR3a, AR3b, AR4, AR4a, CY1 è CY2 èìåþò çíà÷åíè , óêàçàííûå íèæå); (ÒÀ) Ò âûáðàí èç ñëåäóþùèõ ãðóïï: (ÒÀà) AR1 èëè AR3; èëè (TAb) ãðóïïà ôîðìóëû (TAb1) - (TAb6): A 2 0 0 4 1 2 9 2 7 6 R U A Ñòðàíèöà: 3 2 0 0 4 1 2 9 2 7 6 R 4 è R 5 íåçàâèñèìî âûáðàíû èç âîäîðîäà, ãàëîãåíà, òðèôòîðìåòèëà, öèàíî, àçèäî, íèòðî, Ñ1-Ñ4-àëêîêñè, Ñ1-Ñ4-àëêèëS(O)q- (q ïðåäñòàâë åò ...

旋光吡咯化合物及其制法和用途

式(I)旋光性的吡咯化合物或其盐，可用作杀菌 剂。式中R 1 和R 2 独立地为氢、卤素、卤代烷基、卤 代烷氧基或必要时被取代的含氮杂环基；R 3 是氢或 酰基；Q是CH或N； 是至少有两个可被取代 的相邻氮原子作为成环原子的含氮芳族五元杂环基 或有两个或更多可被取代的氮原子作为成环原子的 芳族稠合杂环基；标有(R)的碳原子表示R-构型；条 件是R 1 和R 2 之一当 是1H-1，2，4-三唑-1- 基时应为必要时被取代的含氮杂环基。

Method of producing 2-(2,6-dichlorophenylamino)-2-imidazoline hydrochloride

FIELD: chemistry. SUBSTANCE: invention relates to organic chemistry, specifically to a method of producing 2-(2,6-dichlorophenylamino)-2-imidazoline hydrochloride, which includes condensation in the medium of phosphorus oxychloride of 2,6-dichloroaniline with 1-acetylimidazolidone-2, obtained by acetylation of ethylene urea with acetic anhydride. Acetylation is carried out at a temperature of 80–90 °C and holding for 3–4 hours, condensation is carried out for 3–4 hours at a temperature of 90–100 °C. After the condensation reaction, excess phosphorus oxychloride is distilled from the reaction mass, the residue is mixed with water and ice, the resulting aqueous solution is diacetylated or the reaction mass is mixed with water and ice, the resulting acidic solution is diacetylated. EFFECT: novel, advanced and safer method is developed for use on an industrial scale, which simultaneously increases the yield and purity of the desired product – 2-(2,6-dichlorophenylamino)-2-imidazoline hydrochloride, which is used in medicine to reduce blood pressure, intraocular pressure, heart rate, and has a sedative effect. 1 cl, 2 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 652 125 C1 (51) МПК C07D 233/50 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 233/50 (2006.01) (21)(22) Заявка: 2017134255, 02.10.2017 (24) Дата начала отсчета срока действия патента: Дата регистрации: Приоритет(ы): (22) Дата подачи заявки: 02.10.2017 (56) Список документов, цитированных в отчете о поиске: SU 511000 A3, 15.04.1976. RU (45) Опубликовано: 25.04.2018 Бюл. № 12 2 6 5 2 1 2 5 R U 2133247 C1, 20.07.1999. US 3988345 A, 26.10.1976, формула. JP 50101357 A, 11.08.1975, реферат. (54) Способ получения 2-(2,6-дихлорфениламино)-2-имидазолина гидрохлорида (57) Реферат: Изобретение относится к органической химии, водный раствор диацетилируют или реакционную а именно к способу получения 2-(2,6массу смешивают с водой и льдом, образующийся ...

Method of fighting true mildew

There are desclosed compounds of formula: wherein R = H, an alkyl, an alkenyl, an alkynyl, an alkoxyl, a phenyl, a phenoxy, an alkoxycarbonyl, an alkylcarbonyl, a benzoyl or a cyano group; R' and R 2 = an alkyl, an alkenyl, an alkynyl, a phenyl, an alkoxycarbonyl, an alkylcarbonyl or a cyano group; or R and R 2 together form an orthocondensed benzene ring; X = CH or N. The compounds of formula I are endowed with fungicide activity against phytopathogenous fungi.

Method of preparing imidazole derivatives or thir salts

Imidazole derivatives of the formula I and pharmaceutically acceptable acid addition salts thereof are provided: <IMAGE> I In the formula, R4 1- or 2-naphthyl, optionally substituted with Cl, Br, or I; 1,2,3,4-tetrahydro-6-naphthyl; 3-duryl, optionally 6-substituted by Cl, Br, I, NO2, CH3 or benzyl; mesityl, phenyl 2-, 3- or 4-substituted by OH, NH2, NO2, CH3CONH, phenyl, phenoxy, cyclohexyl, phenylthio, benzylthio, C1-C6 alkyl or C1C6 alkylthio; 4-bibenzylyl; 3,4-dihydroxyphenyl, n=0, 1 or 2 and (a) R=H, alkyl having 1 to 6 carbon atoms or phenyl R1=H, alkyl having 1 to 6 carbon atoms or phenyl one of R2 and R3=H the other of R2 and R3=H, OH, benzoyloxy, C2-C7 alkanoyloxy, N-(C1-C6 alkyl)-carbamoyloxy, N,N-[di-(C1C6)alkyl]-carbamoyloxy, but if R2=R3=H then R=R1=H, or (b) R=H, C1-C6 alkyl, phenyl R1=H, C1-C6 alkyl, phenyl R2+R3=O, or <IMAGE> (c) The compounds of formula I are anti-convulsivants.

Method of producing derivatives of 3-(1-triazolyl)-furan

There are desclosed compounds of formula: wherein R = H, an alkyl, an alkenyl, an alkynyl, an alkoxyl, a phenyl, a phenoxy, an alkoxycarbonyl, an alkylcarbonyl, a benzoyl or a cyano group; R' and R 2 = an alkyl, an alkenyl, an alkynyl, a phenyl, an alkoxycarbonyl, an alkylcarbonyl or a cyano group; or R and R 2 together form an orthocondensed benzene ring; X = CH or N. The compounds of formula I are endowed with fungicide activity against phytopathogenous fungi.

Azolylmethyl-cyclopropylcarbinol derivative

COMPOUNDS OF INDANYL AND TETRAHYDRONAFTIL-AMINO-AZOLINE FOR THE FIGHT AGAINST ANIMAL PEST

1. Таутомерное соединение инданил- или тетрагидронафтил-амино-азолина формулы I ! ! в которой ! n принимает значение 1 или 2; ! m принимает значение 1, 2, 3 или 4, причем, когда m больше 1, радикалы R2 могут принимать одинаковое или разное значение; ! Х означает О, S, NR3, где ! R3 выбран из водорода, циано, нитро, формила, C(=O)R3c, C1-C6-алкила, C2-C6-алкенила, C2-C6-алкинила, С3-С8-циклоалкила, C1-C6-алкокси, C2-C6-алкиниламино, ди(C2-C6-алкинил)амино, (C1-C6-алкокси)метилена, C1-C6-алкилсульфинила, C1-C6-алкилсульфенила или C1-C6-алкилсульфонила, где атомы углерода в алифатических радикалах вышеупомянутых групп могут нести любую комбинацию 1, 2 или 3 радикалов, независимо друг от друга выбранных из группы, состоящей из галогена, циано, нитро, гидрокси, меркапто, амино, карбоксила, C1-C6-алкила, C1-C6-алкокси, C2-C6-алкенилокси, С2-C6-алкинилокси, C1-C6-галоалкокси и C1-C6-алкилтио, или C(O)NR3aR3b, (SO2)NR3aR3b, фенила, фенилокси или бензила, причем каждый из трех радикалов, упомянутых последними, может быть незамещенным или замещенным 1-5 радикалами, независимо друг от друга выбранными из группы, состоящей из галогена, C1-C6-алкила, C1-C6-галоалкила, C1-C6-алкилтио, C1-C6-галоалкилтио, C1-C6-алкокси и C1-C6-галоалкокси; и где ! R3a и R3b независимо друг от друга означают водород, C1-C6-алкил, C1-C6-галоалкил, C2-C6-алкенил или C2-C6-алкинил, ! R3c выбран из водорода, C1-C6-алкила, C2-C6-алкенила, C2-C6-алкинила, С3-С8-циклоалкила, C1-C6-алкилтио, C1-C6-алкокси, (C1-C6-алкил)амино, ди(C1-C6-алкил)амино, фенила и гетероарила, который может представлять собой моно- или бициклическое 5-10-членное гетероароматическое кольцо, содержащее 1, 2, 3 или 4 гетероатомов, выбранных из О, S и N; ! R1 выбран из водорода, циано, нитро, формила, C(=O)R10, C1-C6-алкила, C2-C6-алкенила, C2-C6-алки РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2008 125 301 (13) A (51) МПК C07D 233/50 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ...

METHOD OF OBTAINING N-TRIPHENYLMETHILIMIDAZOLES