COMPOUNDS AND THEIR USE

Described herein are compounds and their use in the treatment of infections. The compound of formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, solvates, pharmaceutically acceptable salts and pharmaceutical compositions described herein are also useful as β-lactamase inhibitors, which restore or enhance the antibiotic spectrum of a suitable antibiotic agent. The compounds of formula (I) act as inhibitors of β-lactamases. These compounds restore/potentiate the activities of β-lactam antibiotics against carbapenemases. These compounds find use in diagnostic method for detecting β-lactamases. 3. The compound of claim 1 , wherein the compound is selected from:1-{[(2S,3S,5R)-2-Carboxy-3-methyl-4,4,7-trioxo-4-thia-1-azabicyclo[3.2.0]hept-3-yl]methyl}-3-methyl-1H-1,2,3-triazol-3-ium;1-{[(2S,3S,5R)-2-Carboxy-3-methyl-4,4,7-trioxo-4-thia-1-azabicyclo[3.2.0]hept-3-yl]methyl}-3-ethyl-1H-1,2,3-triazol-3-ium;1-{[(2S,3S,5R)-2-Carboxy-3-methyl-4,4,7-trioxo-4-thia-1-azabicyclo[3.2.0]hept-3-yl]methyl}-3-n-propyl-1H-1,2,3-triazol-3-ium;1-{[(2S,3S,5R)-2-Carboxy-3-methyl-4,4,7-trioxo-4-thia-1-azabicyclo[3.2.0]hept-3-yl]methyl}-3-allyl-1H-1,2,3-triazol-3-ium;1-{[(2S,3S,5R)-2-Carboxy-3-methyl-4,4,7-trioxo-4-thia-1-azabicyclo[3.2.0]hept-3-yl]methyl}-3-(2-amino-2-oxoethyl)-1H-1,2,3-triazol-3-ium and the corresponding acid;1-{[(2S,3S,5R)-2-Carboxy-3-methyl-4,4,7-trioxo-4-thia-1-azabicyclo[3.2.0]hept-3-yl]methyl}-3-(2-t-butoxy-2-oxoethyl)-1H-1,2,3-triazol-3-ium and the corresponding acid;1-{[(2S,3S,5R)-2-Carboxy-3-methyl-4,4,7-trioxo-4-thia-1-azabicyclo[3.2.0]hept-3-yl]methyl}-3-(2-morpholin-4-yl-2-oxoethyl)-1H-1,2,3-triazol-3-ium and the corresponding acid;1-{[(2S,3S,5R)-2-Carboxy-3-methyl-4,4,7-trioxo-4-thia-1-azabicyclo[3.2.0]hept-3-yl]methyl}-3-{2 [(2-ethoxy-2-oxoethyl)amino]-2-oxoethyl}-1H-1,2,3-triazol-3-ium and the corresponding acid;1-{[(2S,3S,5R)-2-Carboxy-3-methyl-4,4,7-trioxo-4-thia-1-azabicyclo[3.2.0]hept-3-yl]methyl}-3-{2-[(3-ethoxy-3-oxopropyl ...

MANGANESE (III) CATALYZED C--H AMINATIONS

Reactions that directly install nitrogen into C—H bonds of complex molecules are significant because of their potential to change the chemical and biological properties of a given compound. Selective intramolecular C—H amination reactions that achieve high levels of reactivity, while maintaining excellent site-selectivity and functional-group tolerance is a challenging problem. Herein is reported a manganese perchlorophthalocyanine catalyst [Mn(ClPc)] for intermolecular benzylic C—H amination of bioactive molecules and natural products that proceeds with unprecedented levels of reactivity and site-selectivity. In the presence of Brønsted or Lewis acid, the [Mn(ClPc)]-catalyzed C—H amination demonstrates unique tolerance for tertiary amine, pyridine and benzimidazole functionalities. Mechanistic studies indicate that C—H amination proceeds through an electrophilic metallonitrene intermediate via a stepwise pathway where C—H cleavage is the rate-determining step of the reaction. Collectively these mechanistic features contrast previous base-metal catalyzed C—H aminations. 3. The compound of wherein X is halo or SbF.4. The compound of wherein Ris halo.5. The compound of wherein Ris chloro.6. The compound of wherein n is 3 or 4.8. A composition comprising a compound of and a salt.9. The composition of wherein the salt is AgSbF.11. A method for forming a C—N bond comprising contacting an organic substrate claim 1 , a nitrogen-containing oxidant claim 1 , and a compound of claim 1 , in a solvent to form a mixture claim 1 , wherein a C—H moiety of the organic substrate is aminated claim 1 , thereby forming a C—N bond.12. The method of wherein the oxidant is an iminoiodinane.13. The method of wherein the iminoiodinane is formed in situ.14. The method of wherein the iminoiodinane is 2 claim 12 ,2 claim 12 ,2-trichloroethyl (phenyl-λ-iodanylidene)sulfamate.15. The method of wherein the oxidant and the compound of form a metallonitrene catalyst.16. The method of wherein the ...

Platform drug delivery system utilizing crystal engineering and theanine dissolution

A platform drug delivery system and a method of improving the delivery of low solubility pharmaceuticals utilizing crystal engineering and Theanine dissolution resulting in enhanced bioactivity, dissolution rate, and solid state stability.

HIGH PENETRATION PRODRUG COMPOSITIONS OF ANTIMICROBIALS AND ANTIMICROBIAL-RELATED COMPOUNDS

The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate. 1. A high penetration composition of an antimicrobial or an antimicrobial-related compound comprisinga) a functional unit;b) a linkerc) a transportational unit;wherein the functional unit is covalently linked to the transportational unit via the linker;wherein the functional unit comprises a moiety of the antimicrobial or the antimicrobial-related compound;wherein the transportational unit comprises a protonatable amine group; andwherein the linker comprises a chemical bond that is capable of being cleaved after the high penetration composition penetrates across a biological barrier.2. The high penetration composition according to claim 1 , wherein the chemical bond is selected from the group consisting of a covalent chemical bond claim 1 , an ether bond claim 1 , a thioether bond claim 1 , an ester bond claim 1 , a thioester bond claim 1 , a carbonate bond claim 1 , a carbamate bond claim 1 , a phosphate bond claim 1 , and an oxime bond.3. The high penetration composition according to claim 1 , wherein upon cleavage of the cleavable bond claim 1 ...

Beta-lactam compounds and methods of use thereof

Beta-lactam compounds to detect carbapenemases or microbial carbapenem resistance are disclosed. The compounds contain a chemical probe. Upon hydrolysis by carbapenemases, the compounds undergo intramolecular rearrangement and release the chemical probe. Detection of the released chemical probe indicates the presence of carbapenemases and the presence of microbial carbapenem resistance.

Micronized amoxicillin

The present invention relates to amoxicillin trihydrate compositions having a surface area of from 1.0 to 2.5 m 2 ·g −1 that are free of organic contaminants such as dichloromethane, isopropanol, pivalic acid and triethyl amine and that have a purity of from 97.0% to 99.99%. Furthermore, the present invention relates to a method for the preparation of said amoxicillin trihydrate compositions and to the use of said compositions for the treatment of a bacterial infection.

COMPOSITION FOR HARDENING SOFT TISSUE

The present invention relates to various compounds capable of temporarily hardening soft tissue for surgical suturing of the soft tissue. The compounds according to the present invention can temporarily increase the hardness or tension of soft tissue, thereby improving the suturing efficiency during suturing of the soft tissue, thereby preventing aftereffects or the like from occurring due to insufficient anastomosis. In addition, the compounds according to the present invention can temporarily increase the hardness or tension of soft tissue, particularly pancreas, thereby increasing the suturing efficiency during pancreaticoduodenectomy and effectively preventing pancreatic leakage. 2. The compound of claim 1 , wherein the compound is one or more selected from the group consisting of the following compounds:1) (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid;2) Allyl (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;3) Cyclohexylmethyl (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;4) 3-cyanopropyl (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;5) 3-(tert-butoxy)-3-oxopropyl (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;6) Isobutyl (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;7) 2-fluorobenzyl (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;8) 2-(2-ethoxyethoxy)ethyl (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;9) (2S,5R,6R)-6-((R)-2-amino-2-phenylacetamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid;10) (2S,5R,6R)-cyclohexylmethyl 6-((R)-2-amino-2-phenylacetamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2 ...

Composition for Hardening Soft Tissue

The present invention relates to various compounds capable of temporarily hardening soft tissue for surgical suturing of the soft tissue. The compounds according to the present invention can temporarily increase the hardness or tension of soft tissue, thereby improving the suturing efficiency during suturing of the soft tissue, thereby preventing aftereffects or the like from occurring due to insufficient anastomosis. In addition, the compounds according to the present invention can temporarily increase the hardness or tension of soft tissue, particularly pancreas, thereby increasing the suturing efficiency during pancreaticoduodenectomy and effectively preventing pancreatic leakage. 121.-. (canceled)22. A compound or a pharmaceutically acceptable salt or hydrate thereof , wherein the compound is selected from the group consisting of the following compounds:1) Cyclohexylmethyl (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;2) 3-cyanopropyl (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;3) 3-(tert-butoxy)-3-oxopropyl (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;4) Isobutyl (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;5) 2-fluorobenzyl (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenylacetaido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;6) 2-(2-ethoxyethoxy)ethyl (2S,5R,6R)-3,3-dimethyl-7-oxo-6-(2-phenlacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;7) (2S,5R,6R)-6-((R)-2-amino-2-phenylacetamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid;8) (2S,5R,6R)-cyclohexylmethyl 6-((R)-2-amino-2-phenylacetamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;9) (2S,5R,6R)-3-cyanopropyl 6-((R)-2-amino-2-phenylacetamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;10) (2S,5R,6R)-allyl 6-((R ...

SYNTHESIS PROCESS OF PRECURSORS OF DERIVATIVES OF BETA-LACTAM NUCLEI AND PRECURSORS AND DERIVATIVES THEREOF

A synthesis process of precursors of derivatives of beta-lactam compounds, said beta-lactam compounds being selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid, preferably 6-aminopenicillanic acid, comprising the following steps: a) protection of the amine group of the beta-lactam compound, selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid, preferably 6-aminopenicillanic acid, through the formation of a carbamate by reaction with a dicarbonate; b) esterification of the carboxyl group in position 2 of the beta-lactam compound obtained in step a) by reaction with propargyl alcohol. 1. A synthesis process of precursors of derivatives of β-lactam compounds , said β-lactam compounds being selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid , comprising the following steps:a) protection of the amine group of the β-lactam compound, selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid through the formation of a carbamate by reaction with a dicarbonate;b) esterification of the carboxyl group in position 2 of the β-lactam compound obtained in step a) by reaction with propargyl alcohol.2. A synthesis process of triazole derivatives of β-lactam compounds wherein the precursor obtained according to is subjected to a further step c):c) cycloaddition reaction between the precursor obtained in step b) and an organic azide, with the formation of the corresponding triazole derivative of the β-lactam compound.3. The process according to wherein step a) is carried out by reaction with an alkyl claim 1 , aromatic or cyclic dicarbonate.4. The process according to claim 1 , wherein step a) is carried out at room temperature for a time ranging from 10 to 32 hours claim 1 , in a solvent which is a mixture 1:1 by volume of 1 claim 1 ,4-dioxane and water or a mixture 1:1 by volume of tetrahydrofuran (THF) and water claim 1 , the di-(tent-butyl dicarbonate) being present in a molar ratio ranging from 2 to 1 with ...

Processo de sililacao

OXYLATION PROCESS

Amoxicillintrihydrat

Indan- und tetralinderivate

Deprotection of allylic esters and ethers

A process is disclosed for the deprotection of allylic esters and ethers. The process comprises reacting an allyl ester of a carboxylic acid or an allyl ether of a phenol with pyrrolidine or piperidine and a catalytic amount of an organic-soluble palladium complex having a coordinating phosphine ligand to cleave the allyl moiety. The resultant carboxylic acid or phenol is then recovered.

Method of obtaining 7-d-(-)-2-formyloxy-2-(4-acyloxyphenylacetamido)-cephalosporanic acids or salts thereof

Organic semiconductor containing acetylenic anthracene, and Organic thin film transistor using the same

본 발명은 유기 반도체로서 유용한 안트라센에 9- 및/또는 10-위치에 아세틸 기로 개질된 화합물과 이를 포함하는 유기박막트랜지스터에 관한 것으로서, 상세하게는 본 발명에 따른 유기반도체 화합물은 하기 화학식 1로 표시되는 안트라센 유도체인 것을 특징으로 한다. The present invention relates to a compound modified with an acetyl group at the 9- and / or 10-position in anthracene useful as an organic semiconductor, and an organic thin film transistor comprising the same. Specifically, the organic semiconductor compound according to the present invention is represented by the following formula (1) It is characterized in that the anthracene derivative. [화학식 1] [Formula 1] 상기 화합물은 유기박막트랜지스터에서 활성층(active layer)으로 사용될 때, 진공증착공정(vacuum deposition precess)에 의해 박막을 형성과 상온 습식공정(wet process)에 의해 코팅이 가능하며, 높은 전하이동도와 낮은 차단누설전류를 동시에 만족하는 유기박막 트랜지스터를 제조할 수 있는 장점이 있으며, 우수한 액정성으로 인하여 분자간 배열이 용이하게 되어 뛰어난 결정성을 가지게 되며, 본 발명에 따른 유기반도체 화합물을 적용하여 제조되는 유기박막트랜지스터는 다양한 치환체 및 치환체 그룹의 도입에 의한 분자내 혹은 분자간 전하의 이동을 용이하게 할 수 있음은 물론이고, 우수한 결정성 및 강한 파이-스태킹으로 인해 정공 및 전자의 이동도가 개선됨은 물론 우수한 점멸비를 가진다. When the compound is used as an active layer in an organic thin film transistor, it is possible to form a thin film by vacuum deposition process and to coat by wet process, high charge mobility and low blocking. The organic thin film transistor that satisfies the leakage current at the same time has the advantage, and the excellent liquid crystallinity facilitates the intermolecular arrangement has excellent crystallinity, the organic thin film manufactured by applying the organic semiconductor compound according to the present invention Transistors can facilitate the transfer of intramolecular or intermolecular charges by the introduction of various substituents and substituent groups, as well as improved hole and electron mobility due to good crystallinity and strong pi-stacking as well as excellent blinking Have rain. 유기박막트랜지스터, 액정성, 전하 이동도, 점멸비, 안트라센 Organic Thin Film Transistor, Liquid Crystal, Charge Mobility, Flasher Ratio, Anthracene

Process for preparing 2 beta substituted thiomethyl penicillin derivatives

내용 없음. No content.

The method of obtaining cipher bases of 7-amino-3-desatzfetoxycephalosporanic acid

Process for the preparation of sodium amoxycillin

Antibacterial compositions

Penicillin Sulfoxide Production Method

Method of obtaining esters of alpha-aminopenicillins or their acid-additive salts

Способ получений сложных, эфиров вб -амннопеницнллинов об1цей формулы (1) S 3 , - 1 Ri-cH-coim- СООЯу NH2 -фенил, ьксифенил, фторфенил, где R, фурил или тиенил; . «2 -группа формулы -СН-О-СО-ЕЗ СНз или -СН-0 СОО-Яз CHj где Rj - С(-С4-алкил, или их кислотно-аддитивных солей, отличаю щийс  тем, что сложный эфир 6-аминопенициллинойой кислО|ТЫ формулы (II) н тг СНз , -где R, имеет указанные значени , подвергают взаимодействию с производным кислоты формулы (III) Rt CH-COD А . где R{ имеет указанные значени ; А - аминогруппа, азидогруппа или группа формулы нин-с сн-е оснз Iи СНз О или -NH-S и у - атом галогена или группа формулы :л ©Ф -ONa или -О 1Ш2(СсН11)2 : 90 в среде этилацетата, диметилформами Э да или хлороформа в качестве растворител  при температуре от до комнатной с последующим, в случае необходимости, сн тием заместител  сА-аминогруппы или в случае, когда А - азидогруппа, превращением ее в аминогруппу и выделением целевого продукта в свободном виде или в виде кислотно-аддитивной соли. Приоритетно признакам: The method for the preparation of esters of ib-aminnano-pennylline esters of formula (1) S 3, - 1 Ri-cH-coim- NOO NH2-phenyl, xyphenyl, fluorophenyl, where R, furyl or thienyl; . “2 is a group of the formula —CH — O — CO — E3 CH 3 or —CH — 0 COO-Y 3 CH j, where R j is C (—C 4 alkyl, or their acid addition salts, characterized in that the ester is 6-aminopenicillin Acid | TY of the formula (II) n tg CH3, where R, has the indicated values, is reacted with an acid derivative of the formula (III) Rt CH-COD A. Where R {has the indicated values; A is an amino group, an azido group or a group of the formula -Cn-ebc I and CH3 O or -NH-S and y is a halogen atom or a group of the formula: L © F-ONa or-O 1 2 2 (CCHH) 2: 90 in ethyl acetate, dimethyl forms of E d or chloroform as solventat temperatures from to room temperature, followed, if necessary, by removing the substituent of the cA-amino group, or in the case when A is an azido group, converting it into an amino ...

用于改善药用化合物的生物利用度的羧酸酯

含有羧酸基团－COOH作为其化学结构一部分的药用活性化合物，其中－COOH基以羧酸酯的形式存在。

Process for preparing penicillanic acid 1,1-dioxide and derivatives

Penicillanic acid 1,1-dioxide and drirvs. of formula (I) [R=H, ester gp., cation; R1=H, halogen, OAc; R2=R3=H were prepd. by debromination of 6-bromo or 6,6-dibromo deriv. with zinc and aq. acid. Thus, 2.5g I (R=R1=H; R2=Br; R3=H, Br) in aq. MeCN and pH 5.2 was reduced with Zn-4N HCl to give 1.1g > 90% pure I (R-R3=H)

Method of preparing derivatives of 7-/d-(-)-2-amino-2(n-acetoxyphenylacetamido)/-3-cephem-4-carboxylic acid

1476981 6 - (D) - (-) - α - amino - α - (pacetoxyphenylacetamido)penicillanic acid BRISTOL MYERS CO 19 March 1975 [5 June 1974 19 Nov 1974] 24848/74 and 50016/74 Heading C2C The invention comprises the title compound [substantially free from L-(+ )-isomer], and its pharmaceutically acceptable salts. In examples, this compound is prepared by reacting aminopenicillanic acid or its trimethylsilyl ester with the acid chloride hydrochloride, of D-(-)-p-acetoxyphenylglycine, and (where applicable) hydrolysing the intermediate trimethylsilyl ester of the product. The title compound may be treated in aqueous solution with an esterase to give the p-hydroxyphenyl analogue. Therapeutic compositions having antibacterial activity, and which may be administered orally or parenterally, comprise either the title compound, or the p-hydroxyphenyl analogue which has been prepared from it.

Imidazolecarboxylic acid derivative

Method of producing 1,1-dioxo-6-brom(or-6,6-dibromine) penicillanoyloxymethyl ethers of 6-(2-azido-2-phenylacetamido)penicillanic acid

Compounds of the formula <CHEM> wherein R<1> is H or HO; Y and Z are each Cl, Br or I, or Y is H and Z is Cl, Br or I; Q is N3 or NHCO2CH2C6H4R<4> where R<4> is H, Cl, Br, NO2, CH3 or OCH3; a process for their use in production of the valuable antibacterial agents 1,1-dioxopenicillanoyloxymethyl 6-(2-amino-2-phenylacetamido)penicillanate and 1,1-dioxopenicillanoyloxymethyl 6-[2-amino-2-(p-hydroxyphenyl)acetamido]penicillanate, by catalytic hydrogenation in the presence of a noble metal catalyst and novel intermediates useful in preparing said compounds of formula (I).

Process for preparing 2-penem compounds

(I) and its pharmaceutically acceptable salts are prepd. by reacting (II) with trivalent org. phosphorus compd., selected from cyclic or acyclic phosphite, triaryl phosphite, mixed alkylarylphosphite and mixed alkylarylphosphoramide, in the inert solvent at room temp. to b.p. of the solvent. In the formula, R1=C1-4 hydroxy alkyl, R2=(un) substd. C1-6 alkyl by -OH, carboxy or amino, R3=-COOR6[R6=H or replaceable ester gp. , X=S, Z=S or O. Na or K (5R, 6S, 8R)-6-(1- hydroxyethyl)-2-ethylthio-penem-3-carboxylate is produced by the novel method.

1,3-dioxolene-2-one derivative

Co-crystal of piperacillin sodium and sulbactam sodium and preparation method thereof, as well as pharmaceutical compositions containing same and uses thereof

本发明提供了哌拉西林钠与舒巴坦钠共晶及其制备方法、以及包含该共晶的药物组合物及其在治疗产NDM-1“超级细菌”等耐药菌的感染上的应用。所述哌拉西林钠与舒巴坦钠共晶包含在X-射线粉末衍射分析谱图中由2θ表示的14.24、16.58、16.79、17.77、19.20、20.21、20.39、23.06、27.86和32.16°的衍射角。

Process for preparing penicillanic acid derivatives

내용 없음.

Novel fused bridged bicyclic heteroaryl substituted 6-alkylidene penems as potent beta-lactamase inhibitors

A compound of formula (I) or formula (Ia) Wherein R 1 , R a , R 2 , X, R 3 , Y 1 , Y 2 , A, B and C are as defined herein. Also, pharmaceutical compositions comprising such compounds and excipients, methods of treating bacterial infections comprising administering such compounds, methods for making such compounds and hydrates of such compounds.

Silylation method

(57)【要約】 或る種のカルボン酸エステル中でのシリル化による６−アミノペニシラン酸もしくは７−α−アミノ−デスアセトキシ−セファロスポラン酸のシリル化方法、並びに６−α−アミノアシル−ペニシリンおよび７−α−アミノアシル−デスアセトキシ−セファロスポリンの製造におけるその使用。

Silylation Process

본 발명은 특정한 카복실산 에스테르에서 실릴화에 의한 6-아미노페니실란산 또는 7-아미노-데스아세톡시-세팔로스포란산의 실릴화 방법 및 6-α-아미노아실-페니실린 및 7-α-아니모아실-데스아세톡시-세팔로스포린의 제조에 있어서의 이의 용도에 관한 것이다. The present invention provides a process for silylation of 6-aminophenicylic acid or 7-amino-desacetoxy-cephalosporanic acid by silylation in certain carboxylic acid esters and 6-α-aminoacyl-penicillin and 7-α-no It relates to its use in the preparation of moacyl-desacetoxy-cephalosporins.

Improved process for cephalosporin intermediate penicillin sulfoxide

一种头孢中间体青霉素亚砜的改进工艺，以青霉素G钾盐为原料，经过8.5％过氧乙酸氧化，青霉素G钾盐与过氧乙酸按摩尔比1.0～1.5:1，反应结束后加入浓度为3M的硫酸调节pH至1～2，酸化结晶得到带结晶水的青霉素亚砜，然后再将产品溶于醋酸丁酯，50℃、真空度为0.1MPa下真空干燥脱水，得到白色结晶青霉素亚砜脱水得到青霉素亚砜，本发明的有益效果在于：本发明以低浓度的过氧乙酸为氧化剂，反应条件温和，氧化制得的青霉素亚砜带有两个结晶水，通过醋酸丁酯与水的共沸减压除去，整个生产工艺简单，收率高，得到的产品纯度高，完全符合头孢类药物生产的标准。

Process for preparing 6- -bromo-6,6-dibromo penicillanic acid 1,1-dioxides

Bromopenicillanate dioxides I (R=H, Br; R1=H, halogen, OAc; R2=H, ester gp.) were prepd. diazotizing 6beta-aminopenicillanate with equiv. nitrosating agent in the presence of 1-5 equiv. strong acid in the mixt. of H2O and org. solvent. Thus, 6beta-aminopenicillanic acid 1,1-dioxide in dil. H2SO4-MeCN was reacted with pyridine hydrobromide perbromide and NaNO2 to give I (R=H, Br; R1=R2=H) in 1:8 ratio and 78.2% total yield (I) inhibits betalactamase.

Method of obtaining iodmethyl 6-(d-2-azido-2-phenyl acetamido)-penicillanoyloxymethyl carbonate

Antibacterial agents in which a pencillin and a beta-lactamase inhibitor are linked by means of a bis- hydroxymethyl carbonate bridge are of the formula and pharmaceutically acceptable acid addition salts thereof, wherein R 1 is hydrogen, hydroxy, certain acyloxy or certain alkoxycarbonyloxy groups, a method for their use, pharmaceutical compositions thereof, and intermediates useful in their production.

Process for preparing penicillanic acid 1,1-dioxide

Title compds. (I)[R=H, alkali metal cation , useful as fungicides, were prepd.. Thus, 2KHSO5.KHSO4.K2SO4 was dissolved in H2O, cooled to 5≰C, adjusted to pH 5.6 with 2N NaOH and added to a soln. of Na- penicillinate in H2O with stirring. The mixt. was adjusted to pH 4.0-5.0 with 5% Na-Disulfite, heated for 3hr at 35-40≰C and adjusted to pH 2.6 with solid Na-sulfite and later to pH 1.6 with 3N HCl. The acidic soln. was extd. with ethylacete over 2 times, and the aq. mother soln. was satd. with NaCl soln and extd. with ethylacetate. The org. phase was pooled, washed with satd. NaCl soln, dried on MgSO4, vacuum-evapd. and crystallized with ethyacetate/n-hexane to give 93% penicillanic acid 1,1-dioxide.

Intermediate for producing 6-(2-amino-2-phenylacetamide)penicillanic acid 1, 1-dioxopenicillanyloxymethyl

(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。

Biocidal salts

Robust pellet

Method of obtaining penicillanic acid derivatives or salts thereof

Method of producing carbapenem derivatives

A process is disclosed for the deprotection of allylic esters and ethers. The process comprises reacting an allyl ester of a carboxylic acid or an allyl ether of a phenol with pyrrolidine or piperidine and a catalytic amount of an organic-soluble palladium complex having a coordinating phosphine ligand to cleave the allyl moiety. The resultant carboxylic acid or phenol is then recovered.

Preparation contains the Pharmaceutical composition method of 2-methoxy-penem derivatives

本发明涉及制备一种抗菌药用组合物的制备方 法，该方法包括：将式I化合物 其中式中基团定义详见说明书，作为有效成份与 药用载体或稀释剂混合。

The method of obtaining the 7-substituted aminodesacetoxycephalosporan derivatives

Process for preparing 77trichloroacetamidee33desacetoxyy cephalosporane

The method of obtaining derivatives of 7-monochloroacetamido-3-deacetoxycephalosporanic acid

Method of producing 1,1-dioxopenicillanoyloxymethyl-6-(2-amino-2-phenylacetamido)-penicillanate or pharmaceutically acceptable acid-additive salt thereof

Novel compound, manufacture and medicinal composition

(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。

Novel ester of 6-((hexahydro-1h-azepin-1-yl)- methyleneamino)penicillanic acid and its preparation

(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 6-(2-amino-2-phenylacetamido)penicillanoyloxymethyl-1,1-dioxopenicillanoylmethyl-carbonate or its acid-additive salt

Antibacterial agents in which a pencillin and a beta-lactamase inhibitor are linked by means of a bis- hydroxymethyl carbonate bridge are of the formula and pharmaceutically acceptable acid addition salts thereof, wherein R 1 is hydrogen, hydroxy, certain acyloxy or certain alkoxycarbonyloxy groups, a method for their use, pharmaceutical compositions thereof, and intermediates useful in their production.

Process for the preparation of crystalline 1,1-dioxophenicilanoyloxymethyl 6- (D-α-amino-α-phenylacetamido) phenylanate tosylate hydrate

내용 없음

The method of obtaining derivatives of penicillin

Method of preparing phthalide ester 6-(d)-(a-aminophenilacetamido)-penicillanoic acid or its additive salts

Method for producing β-aminopenicillin esters

Manufacture of penicillin ester

Process for penem compounds

내용 없음. No content.

Process for penem intermediates

내용 없음.

Method of obtaining bis-esters of methandiol with penicillin and 1,1-dioxide of penicillanic acid

1. СПОСОБ ПОЛУЧЕНИЯ БИСЭФИРОВ МЕТАНДИОЛА С ПЕНИ1ЩЛЛИНОМ И 1,1-ДИОКСИДОМ ПЕНИЦИЛЛАНОВОЙ КИСЛОТЫ формулы И П. LS.3 f f-СНз - -o R-CH -CONH-W- , CO-0 Q. 0 / AX СНз l CK; N /, 0 где R - фенил или феноксигруппа, отличающийс  тем, что соединение формулы Н н i S .лСНз R-CHg-CONH Т Ъснз -N-ч СООМ О где R имеет указанные значени ; М - катион щелочного металла, подвергают взаимодействию с соединением формулы О, Н .$ СНз (Л сн. ,, COOCHjHai о где Ha - атом галогена, в среде пол рного органического растворител  при комнатной темпераN3 ND S NS туре 2. Способ по п. 1, отличающийс  тем, что процесс ведут в присутствии йодида натри . 35

Process for preparing penicilline derivatives in the form of their salts

Neue 6 a-Methoxy-penicilline der allgemeinen Formel in der A die Phenyl-, p-Hydroxyphenyl-, 2- oder 3-Thienylgruppe, R die Cyclopropylgruppe, eine Gruppe der allgemeinen Formel -NHR 1 , wobei R 1 einen gegebenenfalls ab Kohlenstoffatom 2 durch eine Hydroxygruppe substituierten aliphatischen, verzweigten oder unverzweigten Kohlenwasserstoffrest mit 1 bis 4 Kohlenstoffatomen, einen gegebenenfalls durch eine Hydroxygruppe substituierten Cycloalkylrest mit 3 bis 6 Kohlenstoffatomen oder eine gegebenenfalls durch eine Hydroxy-, Methylsulfinyl-, Methylsulfonyl- oder Aminosulfonylgruppe substituierte 3-Pyridyl-, 2-Furylmethyl-, 2-Thienylmethyl-, 3-lmidazolylmethyl-, 2-Thiazolylmethyl- oder 3-Pyridylmethylgruppe darstellt, eine Gruppe der allgemeinen Formel , wobei n die Zahl 0 oder 1, R 2 und R 3 , die gleich oder verschieden sein können Wasserstoffatome, Hydroxy-, Acetylamino-, Aminocarbonylamino-, Nitro-, Aminocarbonyl-, Cyan-, Methylsulfinyl-, Methylsulfonyl-, Aminosulfonyl-, Methylaminosulfonyl-, Aminocarbonylmethylaminosulfonyl-, 2'-Hydroxyäthylaminosulfonyl-, Cyanaminosulfonyl-, Aminocarbonylaminosulfonyl-, Acetylaminosulfonyl-, Methylsulfonylaminosulfonyl- oder Acetylhydrazinosulfonylgruppen darstellen, wobei m die Zahl 2,3 oder4 darstellt, oder eine Gruppe der Formel bedeuten und deren Salze mit anorganischen oder organischen Basen, welche eine Wirkung gegen grampositive und gramnegative Bakterien, beispielsweise gegen β-Lactamasetragende Escherichia coli- und Klebsiella pneumoniae-Bakterien, aufweisen. Die neuen Verbindungen können nach für analoge Verbindungen üblichen Verfahren hergestellt werden.

Method of producing derivatives of phenylglycine

The invention provides a novel method for producing phenylglycyl chloride hydrochlorides involving reaction of N-substituted phenylglycines with for example thionyl chloride and then gaseous hydrogen chloride, as well as certain novel starting materials for use in this process and certain end-products thereby produced.

Patent JPS4834192A

The method of obtaining thiazolidinazetidinone

Process for preparing -carboxy benzyl acetoamido penicillanic salts

Title compds. ≮I; M = Na, K, organic amine (H NR3), R = C2-5 alkyl) were prepd. by the reaction of 6-aminopenicillanic acid with anhydride(IV) in organic solvent. Thus, anhydride(IV) was prepd. by the reaction of acylhalide and synthetic intermediate(III) obtained from phenylmalonic acid with N, N' -bistrialkylsilylimidazolidinone (II), and anhydride(IV), R1,R2,R3 are same or not, C1-3 alkyl, R4 - R5R6R7C or C2H5O-, R5,R6R7 are same or not, C1-3 alkyl) was reacted with 6-aminopenicillanic acid in organic solvent to give I.

Method of preparing acid amides or their salts with alkaline metals or trialkylamines

1501476 Preparation of penicillanic and cephalosporanic acid compounds CHINOIN GYOGYSZER ES VEGYESZETI TERMEKEK GYARA RT 30 July 1975 [30 July 1974] 31937/75 Heading C2C Acid amides of Formula I or salts thereof, wherein R<SP>1</SP> is H or an easily removable ester-forming or a salt-forming group, R<SP>2</SP> is H, an alkyl group optionally having an aryl heterocyclic substituent, an alkenyl group, an alkaryl group or an aryl, aralkyl or heterocyclic group optionally having one or more substituents, R<SP>3</SP> is H or a salt-forming group, or an optionally substituted aryl, alkyl cycloalkyl or aralkyl group, and X is a group of the formulµ are obtained by acylating a compound of the general Formula II wherein R<SP>4</SP> is an easily-removable ester group or a salt-forming group, using as acylating agent an ester of the general Formula III wherein R<SP>5</SP> is optionally substituted aryl, alky cycloalkyl, or aralkyl, and if desired, substituents R<SP>4</SP> and/or R<SP>5</SP> is/are split off, and/or if desired the obtained product is converted into its salt or a salt is converted into the free acid. When the compound of Formula III is a dipentachlorophenyl ester of a substituted ma- Ionic acid the resulting novel product of Formula I in which R<SP>3</SP> is pentachlorophenyl, may be further reacted with an alcohol or phenol of the general formula R<SP>3</SP>OH to form a product of Formula I in which R<SP>3</SP> is as defined above.

Process for preparing alpha-substituted ureido benzyl penicillin derivatives

The title compds. of formula I (R = hydrogen or hydroxy; X = lower alkyl gorup; Y = substd. group of X), useful as antibacterial substances, were prepd. by reacting alpha-substituted ureido phenylacetic acids with 6-aminopenicillinic acids. Thus, D(-)-alpha- [3-(3,4-dihydroxybenzoyl)-3-(2-cyanoethyl)-3-(2cyanoethyl)-1- ureido phenyl acetic acid reacted with trimethylsilylchloride and triethylamine to give 6-[D(-)-alpha-[3(3,4dihydroxybenzoyl)-3-(2- cyanoethyl)-1-ureido -alpha-phenylacetamise penicillinic acid, a white powder.

Method of stabilization of novel halogenation compounds

Prevention of, or decreasing the rate of the conversion of halogenating cpds. of formula (I) to the corresp. stable cpds. comprises mixing them with a stabilizing amt. of a tert amine base in an anhydrous inert organic solvent. (I) are the kinetically controlled prods. of reacting equiv. amts. of Cl or Br, and the triaryl phosphite of formula (II). X is Cl or Br. Z is H, halo, C1-4 alkyl or Cl-4 alkoxy. Pref. the amine has a pKb of 6-10, and is pref. pyridine. Alternatively, a halide complexing agent; PCl5, AlCl3, or SbCl5 may be used instead of the amine. (I) are useful in the prepn. of 3-halo-3-cephem antibiotics.

Method for preparing cephalosporin or penicillin derivatives

Process for preparing 6-(2-aryl-2-(imidoylamino,alkanoylamino)acetamido)penicillanic acid

Manufacture of penicillin

(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。

Process for preparing 1,1-dioxopenicillanoyl-oxymethyl 6-(d-alpha-amino-alpha-phenylacetamido)penicillanate tosylate hydrate

Antibacterial penicillin crystalline bydrates are prepd.. Thus, 6.31g 1,1-dioxopenicillanoyl oxymethyl 6-(D-α-amino-α phenylacetamido) penicillanate HCl in 40ml H2O and 10ml acetone is reacted with 1.94g 4-toluene sulphonate in 10ml H2O for 1hr at room temp. and later for 2hr at 5≰C with stirring. The growing ppts. are collected, washed with H2O, and vaccumdried to give 1,1dioxopenicillanoyl oxymethyl 6-(D-α-amino-α-phenylacetamido) penicillanate tosylate.2H2O.

Method of preparing derivatives of 6-amino-2',3',5',6'-tetrahydrospiro-/penam-2,4'-/4h/(thio)-pyran/-3-carboxylic acid or pharmaceutically adopted salts

Amino-spiro[oxa(or thia)cycloalkane-penam]-carboxylic acid derivatives having the formula <IMAGE> WHEREIN X is a sulfur or oxygen atom or the sulfinyl group, n is 1 or 2, m is 1 or 2, R1 is hydrogen, R2 is one of the radicals known in the chemistry of the penicillins, preferably 2-phenylacetyl, 2-amino-2-phenylacetyl, 5-methyl-3-phenyl-4-isoxazolecarbonyl or 2,6-dimethoxybenzoyl, or R1 and R2 together represent a bivalent radical R3, preferably (hexahydro-1H-azepin-1-yl)methylene and their therapeutically acceptable non-toxic salts and process for preparing the same.

Penamylacid ester derivative

(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。

Mounting device

Deprotection of allylic esters and ethers

本发明涉及烯丙基酯类和醚类脱保护作用的方法。该方法包括羧酸的烯丙基酯和苯酚的烯丙基醚与吡咯烷或哌啶和催化量的有机溶剂可溶的有配位膦配位体的钯配合物反应，裂解烯丙基并再生成羧酸或苯酚。

Method of obtaining 3-haloidcephalosporins

СПОСОБ ПОЛУЧЕНИЯ 3-ГАЛОИДДЕФАЛОСПОРИНОВ формулы (I) R-CHiCONH -фенил или феноксигруппа; где R X -хлор или бром, путем взйимодействи  3-оксицефалоспорина формулы (П) . R-CrtiCONH-p-NY LOH NOi COO-CHt где R имеет указанные значени , (с галоидирующим реагентомв безводном инертном органическом растворителе , отличающийс  тем, что, с целью увеличени  выхода целевого продукта, в качестве галоидирующего реагента используют кинетически контролируемьй комплекс триарилфосфита с галогеном формулы (Ш) 0 РХг где Z . - водород или метил; X - имеет указанные значени , .в количестве 1,0-1,1 эквивалента на 1 эквивалент исходного цефалоспорина , и процесс ведут в присутствии пиридина в качестве основани  при температуре от -10 до . Р1 METHOD FOR OBTAINING 3-HALOIDDEPHALOSPORINS of formula (I) R-CHiCONH is phenyl or phenoxy; where R X is chlorine or bromine, by acting on the 3-oxycephalosporin of formula (P). R-CrtiCONH-p-NY LOH NOi COO-CHt where R has the indicated values (with a halogenating reagent in an anhydrous inert organic solvent, characterized in that, in order to increase the yield of the target product, a kinetically controlled triarylphosphite complex with halogen is used as a halogenating reagent where formula is hydrogen or methyl, X - has the indicated values, in the amount of 1.0-1.1 equivalents per equivalent of starting cephalosporin, and the process is carried out in the presence of pyridine as a base at a temperature from - 10 to. P1

Method of preparing 6-aminopenicillanic or 7-aminocephalosporanic acid

Preparation of Sodium Amoxacillin

내용 없음

Process for preparing derivatives of 6-acylamino-spiro(pename-2,4-piperidine)-3-carboxylic acid

The method of obtaining derivatives of 7-monochloroacetamido-3-deacetoxycephalosporanic acid

The method of obtaining derivatives of penicillin

Method of synthesis of benzyl- and phenoxymethylpenicillin sulfoxide

FIELD: chemical technology, antibiotics. SUBSTANCE: benzyl- or phenoxymethylpenicillin is sorbed from an aqueous solution with synthetic polymeric sorbent, preferably, with sorbent made on the basis of copolymer of styrene with divinylbenzene or sorbent made on the basis of copolymer of styrene with divinylbenzene containing alkylacrylate fragments in the polymeric chain. Then treatment with oxidizing agent is carried out at the phase of synthetic polymeric sorbent. Formed benzyl- or phenoxymethylpenicillin sulfoxide is desorbed with an aqueous solution of organic solvent and isolated by precipitation with mineral or organic acid. EFFECT: improved method of synthesis. 3 cl 07У96$0с ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВО ‘” 2 059 640 ' (51) МПК 13) Сл С 070 499/46 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 93000508/04, 06.01.1993 (46) Дата публикации: 10.05.1996 (56) Ссылки: Патент ФРГ М 2230372, кл. С 070 99/16, 1973. Патент Франции М 2175169, кл. С 070 99/16, 1973. Патент СССР М 495840, кл. С 070499/46. (71) Заявитель: Савельев Е А., Пушков А.Н., Богатков Л.Г., Сафиулина М.А. (72) Изобретатель: Савельев Е_А., Пушков А.Н., Богатков Л.Г., Сафиулина М.А. (73) Патентообладатель: Савельев Евгений Александрович (54) СПОСОБ ПОЛУЧЕНИЯ СУЛЬФОКСИДА БЕНЗИЛ- И ФЕНОКСИМЕТИЛПЕНИЦИЛЛИНА (57) Реферат: Сущность изобретения: бензил- или феноксиметилпенициллин сорбируют из водного раствора синтетическим полимерным сорбентом, в качестве которого наиболее предпочтительно использовать сорбент на основе сополимера стирола С дивинилбензолом или сорбент на основе сополимера стирола с дивинилбензолом, содержащий алкилакрилатные фрагменты в полимерной цепи. Затем В фазе синтетического полимерного сорбента проводят обработку окислителем. Образующийся при этом сульфоксид бензил- или феноксиметилпенициллина десорбируют водным раствором полярного органического растворителя и выделяют осаждением минеральной или органической кислотой. 2 3. п. ф- ...

Method for preparing 6- / d / - -aminophenylacetamido / penicillanic acid phthalide ester

Method for preparing 6-aminopenicillanic acid derivatives or their salts or esters

Patent JPS5512435B2

The method of obtaining derivatives of 6-aminocyclic acid or their salts

Process for preparing sodium amoxicillin

Solid Na-amoxycillin (AMX) is prepd. by spray-drying of Na-AMX soln. in the solvent contg. secondary or tertiary carbinol [at least 5 vol.% are water soluble i.e. t-butanol (TB) and water at 25 deg.C. Fine powdered AMX.3H2O (chemical titer 845 mcg/mgm) is slurried in water soluble TB contg. water 2.4 L and TB 1.5L per a kg of AMX.3H2O. Excess amts. (about 2%, 1.23 L/kg) of 1.97N NaOH aq. soln. are added to slurry for clear soln. at 25 deg.C and introduced into a dryer [inlet (180 deg.C) and outlet (120 deg.C) are cleared by N2 . Sterilized solid Na-AMX (can fill up vials directly) can be produced by the use of a nozzle under steriling conditions.

Antibacterial compound nitrate salts

FIELD: medicine, pharmacy. SUBSTANCE: invention relates to nitrate salts of cefazolin, ampicillin, clindamycin, ciprofloxacin and nitroxy-derivative of metronidazole that can be used as antibacterial medicinal agents, in particular, as antiviral, antifungal and antibacterial medicinal agents. EFFECT: valuable medicinal properties of antibacterial compounds. 5 cl, 2 tbl, 21 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 288 231 (13) C2 (51) ÌÏÊ C07D 501/59 (2006.01) A61P 31/04 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2002120480/04, 16.01.2001 (30) Êîíâåíöèîííûé ïðèîðèòåò: 26.01.2000 IT MI 2000 A 000092 (73) Ïàòåíòîîáëàäàòåëü(è): ÍÈÊÎÊÑ Ñ.À. (FR) (43) Äàòà ïóáëèêàöèè çà âêè: 27.04.2004 R U (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 16.01.2001 (72) Àâòîð(û): ÄÅËÜ ÑÎËÄÀÒÎ Ïüåððî (IT), ÁÅÍÅÄÈÍÈ Ôðàí÷åñêà (IT), ÀÍÒÎÃÍÀÖÖÀ Ïàòðèöè (IT) (45) Îïóáëèêîâàíî: 27.11.2006 Áþë. ¹ 33 2 2 8 8 2 3 1 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: RU 2071963 C1, 20.01.1997. WO 93/20812 A, 28.10.1993. WO 90/07325 A, 12.07.1990. (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 26.08.2002 Àäðåñ äë ïåðåïèñêè: 121087, Ìîñêâà, à/ 33, Â.Â.Êóðûøåâó (54) ÍÈÒÐÀÒÍÛÅ ÑÎËÈ ÀÍÒÈÌÈÊÐÎÁÍÛÕ ÑÎÅÄÈÍÅÍÈÉ (57) Ðåôåðàò: Íàñòî ùåå èçîáðåòåíèå îòíîñèòñ ê íèòðàòíûì ñîë ì öåôàçîëèíà, àìïèöèëëèíà, êëèíäàìèöèíà, öèïðîôëîêñàöèíà, ñóëüôàìåòîêñàçîëà è íèòðîêñèïðîèçâîäíîãî ìåòðîíèäàçîëà, êîòîðûå ìîãóò áûòü èñïîëüçîâàíû â êà÷åñòâå àíòèìèêðîáíûõ ëåêàðñòâåííûõ ñðåäñòâ, â îñîáåííîñòè àíòèâèðóñíûõ, ïðîòèâîãðèáêîâûõ è àíòèáàêòåðèàëüíûõ ëåêàðñòâåííûõ ñðåäñòâ. 2 í. è 3 ç.ï. ô-ëû, 2 òàáë. R U 2 2 8 8 2 3 1 (87) Ïóáëèêàöè PCT: WO 01/54691 (02.08.2001) C 2 C 2 (86) Çà âêà PCT: EP 01/00430 (16.01.2001) Страница: 1 RU RUSSIAN FEDERATION RU (19) (11) 2 288 231 (13) C2 (51) Int. Cl. C07D 501/59 (2006.01) A61P 31/04 (2006.01) FEDERAL SERVICE FOR INTELLECTUAL PROPERTY, PATENTS AND TRADEMARKS (12) ABSTRACT OF INVENTION (21 ...

Preparation method of azlocillin and preparation method of azlocillin sodium freeze-dried powder for injection

本发明公开了一种阿洛西林酸及阿洛西林钠冻干粉针的制备方法，其中，阿洛西林酸的制备方法包括：室温条件下，在反应容器中按重量份加入氨苄西林三水合物25～35份，丙酮55～65份，水240～260份，二氧六环和四氢呋喃共4～6份，搅拌均匀，二氧六环和四氢呋喃的重量份之比为6～8:1；待反应容器中的物料温度降至10～15℃时，滴加三乙胺6～12份，搅拌使反应容器中的溶液完全澄清；待物料温度降至5～10℃时，缓慢添加1?氯甲酰基?2?咪唑烷酮9.10～12.74份，保持15～20℃，搅拌反应2.5～3.5h；加入盐酸，调节pH至3～4，置于3～5℃条件下进行阿洛西林酸的结晶，析出沉淀物；过滤，取沉淀物，用丙酮淋洗后真空干燥。本发明提供的阿洛西林酸的制备方法得率高，制得的阿洛西林酸纯度高，且无溶剂残留。

Process for preparing penicillin derivatives

Substd. penicillanic acid derivs. of formula (I) and their nontoxic salts are prepared. In (I), R1 is H or trialkylsilyl; R2 is H, trialkylsilyl or COOQ, where Q is H, C1-18 alkyl or a protective ester gp. which is easily cleaved; and R3 is defined as Q. (I) are resistant to beta-lactamase and have a wide spectrum of antibiotic acitvity.

Method of producing 1-ethoxycarbonyloethyl ester of 6-/d-(-)-2-amino-2-phenylacetamido/-penicillanic acid as its additive salt with halogen acid

The novel compound alpha -bromodiethylcarbonate, its use in the preparation of 1-ethoxycarbonyloxyethyl esters of penicillins and cephalosporins, in particular bacampicillin, and improvements in the method for preparing such esters.

Method of producing optically pure (5r, 6s)-6-/1(r)-hydroxyethyl/-2-methoxy-methylpenem-3-carbolic acid or its esters or salts with alkali metals

A substantially (>/=95%) optically pure (5R,6S,1 min R) penem of formula <CHEM> and the pharmaceutically acceptable salts and the ester prodrugs thereof, are endowed with antibacterial activity.

Method of obtaining bis-esters of methadiol with penecillin and 1,1-dioxide of penicillanic acid

СПОСОБ ПОЛУЧЕНИЯ БИС-ЭФИРОВ МЕТАНДИОЛА С ПЕНИЦИЛЛИНОМ И 1,1-ДИОКСИДОМ ПЕНИЦИЛЛАНОВОЙ КИСЛОТЫ формулы Н Н н-сн,-со н -4 ш: . о о сн, Y сн, 5x5- 0 C-l R о где R - фенил или феноксигруппа, отличающийс  тем, что соединение формулы Н Н -,, VT Т. V. H,N снз Q --14-- /с-о п о о 0 ri V f«W i vS-s4- 3 т рснз S к-J.,,f.- с-о 0 в о подвергают ацилированию реакционноспособным производным карбоновой кислоты формулы ю N9 ГО R-CH,j-COOH, где R имеет указанные значени  00 при охлаждении в среде инертного растворител . METHOD OF OBTAINING METHANDIOL BIS-ETHERS WITH PENICILLIN AND 1,1-DIOXIDE OF PENICILLANIC ACID of the formula N N n-sn, -so n-4 W:. O o Cn, Y cn, 5x5-0 Cl R o where R is a phenyl or phenoxy group, characterized in that the compound of the formula HH is ,, VT T. V. H, N cps Q - 14-- / s-o p о о 0 ri V f «W i vS-s4- 3 tons of pH of S c-J. ,, f.- с-о 0 в о is subjected to acylation with a reactive carboxylic acid derivative of the formula: N9 GO R-CH, j-COOH where R has the indicated values 00 when cooled in an inert solvent.

Patent JPS6021593B2

Method of preparing 6-substituted penicillins

Process for preparing penicillanic acid 1,1-dioxide and esters therof

Penicillanic acid derivs. of formula (I) and their pharmaceutically permissible salts are prepd. by reacting compds. of formula (II) or their salts with a reactant (selected from alkali metal permanganate, alkaline metal permanganate, or organic peroxycarboxylic acid) to yield compds. of formula (III) or their salts, and then catalytically dehalogenating the prods. in an inert solvent. In the formulas, R1 is H or an ester residue that is easily hydrolyzed in vivo; X and Y are each H, Cl, Br, or I, but if the same they must both be Br. (I) are useful as antibiotics and beta-lactamase inhibitors

Process for preparing penicillanic acid compounds

내용 없음. No content.

2 beta-substituted-methylpenicillanic acid derivatives and salts and esters thereof

내용 없음. No content.

Method of producing 1,1-dioxide of penicillanic acid or ether thereof

A process for the preparation of penicillanic acid 1,1-dioxide and esters thereof readily hydrolyzable in vivo. Said process involves dehalogenation of a 6-halo or 6,6-dihalo derivative of penicillanic acid 1,1-dioxide or ester thereof readily hydrolyzable in vivo or a carboxy protected derivative thereof (e.g. by hydrogenolysis). The 6-halo and 6,6-dihalo derivatives of penicillanic acid 1,1-dioxides, esters thereof readily hydrolyzable in vivo, and carboxy protected derivatives thereof are novel intermediates. Penicillanic acid 1,1-dioxide, and esters thereof readily hydrolyzable in vivo, are known compounds which are useful as beta- lactamase inhibitors and for enhancing the effectiveness of certain beta-lactam antibiotics (e.g. the penicillins) in the treatment of bacterial infections in mammals, particularly humans.

Process for the preparation of metal complex carboxamides

The invention relates to a method for producing metal complex carboxylic acid amides characterized in that a metal complex carboxylic acid mixture consisting of metal complex carboxylic acid and at least one solubilizing substance is pretreated in dimethylsulfoxide (DSMO) with a dehydrating reagent, optionally by adding a coupling adjuvant and made to react with a amine of general formula (I): A(NH2)n, wherein A means the radical of a natural or synthetic amine and n stands for the figures 1 to 100.