Piperidine derivatives and process for their production

Piperidine derivatives and process for their production

Piperidine derivatives and process for their production

YOU LEAVE THE ACID BORONICO AND ITS USE IN THE MEDICINE PREPARATION FOR THE TREATMENT OF THE TROMBOSE

USE OF HUMAN CB2 RECEPTOR AGONIST COMPOUNDS FOR THE PREPARATION OF IMMUNOMODULATORY DRUGS, NOVEL CB2 RECEPTOR AGONIST COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Process for production of piperidine derivatives

Cb 2? receptor agonist compounds

The use of human CB2 receptor-specific agonists of formula (I) or (I') for preparing immunomodulating drugs is disclosed. In formulae (I) and (I'), R1 is a group selected from -CH2CHR10NR6R11, -(CH2)2NR'6R'11, -CHR9CH2NR'6R'11, -(CH2)nZ and -COR8; R'1 is a -CH2CHR10NR6R11 or -(CH2)2NR'6R'11 group; R2 and R'2 are hydrogen, halogen or C1-4 alkyl; R3 is hydrogen, C1-4 alkyl or a group selected from -CH2CHR10NR6R11, -(CH2)2NR'6R'11 and -COR8; R'3 is a =CR6R8 group; R4 has one of the meanings given for R5 or is a -COR8 group; R5 is hydrogen, C1-4 alkyl, C1-4 alkoxy, a halogen atom, a CF3 group, an OCF3 group or C1-4 alkylthio; R'5 has one of the meanings given for R5 and is in the 5 or 6 position of the indene ring; R6 is hydrogen or C1-4 alkyl; R'6 is C1-4 alkyl; R7 has one of the meanings given for R5 or R7 and R9 together form a -Y-CH2- group attached to the indole ring in the 7 position by a group Y; R8 is phenyl substituted one to four times by a substituent selected from halogen, C1-4 alkyl or C1-4 alkoxy; a polycyclic ring selected from naphth-1-yl, naphth-2-yl, 1,2,3,4-tetrahydronaphth-1-yl, 1,2,3,4-tetrahydronaphth-5-yl, anthryl, benzofuryl, benzothien-2-yl, benzothien-3-yl, 2-, 3-, 4- or 8-quinolyl, said polycyclic rings optionally being substituted once or twice by a substituent selected from C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, halogen, cyano, hydroxyl, trifluoromethyl and imidazol-1-yl; R10 and R11 together are a group selected from -CH2-O-CH2-CR12R13- and -(CH2)p-CR12R13-, wherein the carbon atom substituted by R12 and R13 is attached to the nitrogen atom; R'11 is C1-4 alkyl; or R'11 and R'6, taken together with the nitrogen atom to which they are attached, form a group selected from morpholin-4-yl, thiomorpholin-4-yl, piperidin-1-yl and pyrolidin-1-yl; each of R12 and R13 is independently hydrogen or C1-4 alkyl; n is 2, 3, 4 or 5; p is 2 or 3; Z is a methyl group or a halogen atom; ...

USE OF HUMAN CB2 RECEPTOR AGONISTIC COMPOUNDS FOR THE PREPARATION OF IMMUNOMODULATORY DRUGS, NOVEL AGONIST COMPOUNDS OF CB2 RECEPTOR AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

The use of human CB2 receptor-specific agonists of formula (I) or (I') for preparing immunomodulating drugs is disclosed. In formulae (I) and (I'), R1 is a group selected from -CH2CHR10NR6R11, -(CH2)2NR'6R'11, -CHR9CH2NR'6R'11, -(CH2)nZ and -COR8; R'1 is a -CH2CHR10NR6R11 or -(CH2)2NR'6R'11 group; R2 and R'2 are hydrogen, halogen or C1-4 alkyl; R3 is hydrogen, C1-4 alkyl or a group selected from -CH2CHR10NR6R11, -(CH2)2NR'6R'11 and -COR8; R'3 is a =CR6R8 group; R4 has one of the meanings given for R5 or is a -COR8 group; R5 is hydrogen, C1-4 alkyl, C1-4 alkoxy, a halogen atom, a CF3 group, an OCF3 group or C1-4 alkylthio; R'5 has one of the meanings given for R5 and is in the 5 or 6 position of the indene ring; R6 is hydrogen or C1-4 alkyl; R'6 is C1-4 alkyl; R7 has one of the meanings given for R5 or R7 and R9 together form a -Y-CH2- group attached to the indole ring in the 7 position by a group Y; R8 is phenyl substituted one to four times by a substituent selected from halogen, C1-4 alkyl or C1-4 alkoxy; a polycyclic ring selected from naphth-1-yl, naphth-2-yl, 1,2,3,4-tetrahydronaphth-1-yl, 1,2,3,4-tetrahydronaphth-5-yl, anthryl, benzofuryl, benzothien-2-yl, benzothien-3-yl, 2-, 3-, 4- or 8-quinolyl, said polycyclic rings optionally being substituted once or twice by a substituent selected from C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, halogen, cyano, hydroxyl, trifluoromethyl and imidazol-1-yl; R10 and R11 together are a group selected from -CH2-O-CH2-CR12R13- and -(CH2)p-CR12R13-, wherein the carbon atom substituted by R12 and R13 is attached to the nitrogen atom; R'11 is C1-4 alkyl; or R'11 and R'6, taken together with the nitrogen atom to which they are attached, form a group selected from morpholin-4-yl, thiomorpholin-4-yl, piperidin-1-yl and pyrolidin-1-yl; each of R12 and R13 is independently hydrogen or C1-4 alkyl; n is 2, 3, 4 or 5; p is 2 or 3; Z is a methyl group or a halogen atom; ...

3-arylcarbonyl-1-(c-attached-n-heteryl)-1h-indoles

2-R 2 -R 4 -substituted-3-R 3 -CO-1-[(C-attached-N-herteryl)-(Alk) n ]-1H-indoles useful as analgesic, anti-rheumatic, anti-inflammatory or anti-glaucoma agents.

Process for production of piperidine derivatives

The present invention discloses processes for preparing piperidine derivative compounds of formulae (I) or (II) wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is -COOH or -COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents. One process comprises providing a regioisomer of formula (III) wherein Z is -CG1G2G3, (IV) or (V), m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; and R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and converting the regioisomer to the piperidine derivative compound with a piperidine compound. Another process for producing piperidine derivative compounds comprises providing an .alpha.,.alpha.-disubstituted-methylbenzene derivative having formula (VI) wherein X1 is a halogen, trialkyl or triaryl tin, trialkyl or triaryl borate trialkyl silicon, alkylhalo silicon, a substituted sulfonic ester, or substituents useful in organometallic coupling reactions and converting the .alpha.,.alpha.-disubstituted-methylbenzene derivative to the piperidine derivative compound with a piperidine compound. In yet another process, a 4-(.alpha.,.alpha.-disubstituted)-toluic acid derivative having formula (VII) wherein X2 is ...

USEFUL COMPOUNDS AS INTERMEDIATE PRODUCTS IN THE PRODUCTION OF PIPERIDINE DERIVATIVES.

Un procedimiento para preparar un regioisómero substancialmente puro de fórmula I, en la que R3 es -COOH o -COOR4; R4 es un alquilo con 1 a 6 átomos de carbono; A son los sustituyentes de su anillo, cada uno de los cuales puede ser diferente o el mismo y se seleccionan del grupo que consiste en hidrógeno, halógenos, alquilo, hidroxi o alcoxi. dicho procedimiento comprende recuperar, mediante cristalización, el regioisómero de fórmula I substancialmente puro de una mezcla de regioisómeros de fórmula III: A process for preparing a substantially pure regioisomer of formula I, wherein R3 is -COOH or -COOR4; R4 is an alkyl with 1 to 6 carbon atoms; A are the substituents of its ring, each of which may be different or the same and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy or alkoxy. said process comprises recovering, by crystallization, the substantially pure regioisomer of formula I from a mixture of regioisomers of formula III:

Synthesis of substantially pure terfenadine derivatives

The present invention relates to substantially pure piperidine derivative compounds of formulae (I) or (II) wherein R 1 is hydrogen or hydroxy; R 2 is hydrogen; or R 1 and R 2 taken together form a second bond between the carbon atoms bearing R 1 and R 2 ; R 3 is -COOH or -COOR 4 ; R 4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents.

Process for production of piperidine derivatives

The present invention discloses processes for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R 1 is hydrogen or hydroxy; R 2 is hydrogen; or, when n is 0, R 1 and R 2 taken together form a second bond between the carbon atoms bearing R 1 and R 2 , provided that when n is 1, R 1 and R 2 are each hydrogen; R 3 is —COOH or —COOR 4 ; R 4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.

Process for the preparation of compounds useful as intermediates

Piperidine derivatives and process for their production

The present invention relates to substantially pure piperidine derivative compounds as shown below, wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is -COOH or -COOH4; R4 is an alkyl with 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed. (see formula I) or (see formula II)

Process for the preparation of piperidine derivatives

Det er beskrevet en fremgangsmåte for fremstilling av l det vesentlige rene plperldlnderlvatforblndelser av formelene (I) eller (II) hvor R! er hydrogen eller hydroksy; R2 er hydrogen; eller R^ og R2 tatt sammen danner en andre binding mellom karbonatomene som bærer R! og R2; R3 er -COOH eller -COOR4; R4 har l til 6 karbonatomer; A, B og D er substituentene av deres respektive ringer, disse kan være like eller for- skjellige og er hydrogen, halogener, alkyl, hydroksy, alkoksy eller andre substituenter.

PIPERIDINE DERIVATIVES AND PROCESS FOR ITS PRODUCTION.

LA PRESENTE INVENCION SE REFIERE A COMPUESTOS DERIVADOS DE PIPERIDINA SUSTANCIALMENTE PUROS DE FORMULA (I) O (II), DONDE R{SUB,1} ES HIDROGENO O HIDROXI; R{SUB,2} ES HIDROGENO; O R{SUB,1} Y R{SUB,2} JUNTOS FORMAN UNA SEGUNDA UNION ENTRE LOS ATOMOS DE CARBONO QUE PORTAN R{SUB,1} Y R{SUB,2}; R{SUB,3} ES COOH O -COOR{SUB,4}; R{SUB,4} TIENE DE 1 A 6 ATOMOS DE CARBONO; A, B Y D SON LOS SUSTITUYENTES DE SUS ANILLOS CORRESPONDIENTES, PUDIENDO SER CADA UNO DIFERENTE O IGUAL, Y SON HIDROGENO, HALOGENOS, ALQUIL, HIDROXI, ALCOXI, U OTROS SUSTITUYENTES.TAMBIEN SE EXPONE UN PROCESO PARA PREPARAR TALES COMPUESTOS DERIVADOS DE PIPERIDINA EN UNA FORMA SUSTANCIALMENTE PURA. THE PRESENT INVENTION REFERS TO SUBSTANTIALLY PURE PIPERIDINE-DERIVED COMPOUNDS OF FORMULA (I) OR (II), WHERE R {SUB, 1} IS HYDROGEN OR HYDROXY; R {SUB, 2} IS HYDROGEN; OR R {SUB, 1} AND R {SUB, 2} TOGETHER FORM A SECOND UNION BETWEEN THE CARBON ATOMS CARRIED BY R {SUB, 1} AND R {SUB, 2}; R {SUB, 3} IS COOH OR -COOR {SUB, 4}; R {SUB, 4} HAS 1 TO 6 ATOMS OF CARBON; A, BYD ARE THE SUBSTITUTES FOR THEIR CORRESPONDING RINGS, MAY BE EACH ONE DIFFERENT OR THE SAME, AND THEY ARE HYDROGEN, HALOGEN, RENT, HYDROXY, ALCOXY, OR OTHER SUBSTITUTE PURPOSES IN A COMPOSITE PROCESS FOR THEM. SUBSTANTIALLY PURE.

Process for production of piperidine derivatives

The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is —CG 1 G 2 G 3 ; G 1 , G 2 , and G 3 are the same or different and are selected from the group consisting of OR 8 , SR 8 , and NR 8 R 9 ; and R 8, and R 9 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety.

Cb2 receptor agonist compounds

The use of human CB2 receptor-specific agonists of formula (I) or (I') for preparing immunomodulating drugs is disclosed. In formulae (I) and (I'), R1 is a group selected from -CH2CHR10NR6R11, -(CH2)2NR'6R'11, -CHR9CH2NR'6R'11, (CH2)nZ and -COR8; R'1 is a -CH2CHR10NR6R11 or -(CH2)2NR'6R'11 group; R2 and R'2 are hydrogen, halogen or C1-4 alkyl; R3 is hydrogen, C1-4 alkyl or a group selected from -CH2CHR10NR6R11, -(CH2)2NR'6R'11 and -COR8; R'3 is a =CR6R8 group; R4 has one of the meanings given for R5 or is a -COR8 group; R5 is hydrogen, C1-4 alkyl, C1-4 alkoxy, a halogen atom, a CF3 group, an OCF3 group or C1-4 alkylthio; R'5 has one of the meanings given for R5 and is in the 5 or 6 position of the indene ring; R6 is hydrogen or C1-4 alkyl; R'6 is C1-4 alkyl; R7 has one of the meanings given for R5 or R7 and R9 together form a -Y-CH2- group attached to the indole ring in the 7 position by a group Y; R8 is phenyl substituted one to four times by a substituent selected from halogen, C1-4 alkyl or C1-4 alkoxy; a polycyclic ring selected from naphth-1-yl, naphth2-yl, 1,2,3,4-tetrahydronaphth-1-yl, 1,2,3,4-tetrahydronaphth-5-yl, anthryl, benzofuryl, benzothien-2-yl, benzothien-3-yl, 2-, 3-, 4- or 8-quinolyl, said polycyclic rings optionally being substituted once or twice by a substituent selected from C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, halogen, cyano, hydroxyl, trifluoromethyl and imidazol-1-yl; R10 and R11 together are a group selected from -CH2-O-CH2-CR12R13- and -(CH2)p-CR12R13-, wherein the carbon atom substituted by R12 and R13 is attached to the nitrogen atom; R'11 is C1-4 alkyl; or R'11 and R'6, taken together with the nitrogen atom to which they are attached, form a group selected from morpholin-4-yl, thiomorpholin-4-yl, piperidin-1-yl and pyrolidin-1-yl; each of R12 and R13 is independently hydrogen or C1-4 alkyl; n is 2, 3, 4 or 5; p is 2 or 3; Z is a methyl group or a halogen atom; ...

Antiarrhythmic diarylamidines

Novel diarylamidines, and compositions and methods for treating cardiac arrhythmias in mammals utilizing the novel and related known diarylamidines of formula I, II, III and IV ##STR1##

Amine preparation

A method of making (R)-N- 1-(3-methoxyphenyl)ethyl!-3-(2-chlorobenzene)propanamine which involves reducing the appropriate amidyl or iminyl precursor with an appropriate reducing agent. The appropriate amidyl or iminyl precursor is made from a synthesis involving the use of (R)-3-methoxy-α-methylbenzylamine. A method of condensing a nitrile with a primary or secondary amine to form an imine involves the reaction of a nitrile with diisobutylaluminum hydride; and then reacting the resultant compound with a primary or secondary amine to form the imine. The process is especially useful for producing enantiomerically pure chiral imines, and, ultimately, amines. Typical such imines have the formula: ##STR1## wherein R, R 1 , R 2 and R 3 are independently selected from the group consisting of hydrogen, substituted or unsubstituted alkyl, aryl and aralkyl.

Process for production of piperidine derivatives

Process for production of piperidine derivatives

The present invention relates to a process for preparing piperidine derivative compounds of formulae (I, II), wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R' and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is -COOH or -COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents. The process comprises providing a regioisomer of formula (III), wherein Z is -CG1G2G3 (IV) or (V), m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; and R5, R8, and R9 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety and converting the regioisomer to the piperidine derivative compound with a piperidine compound.

Process for production of piperidine derivatives

The present invention relates to a process for preparing piperidine derivative compounds of formulae (I, II), wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R?1 and R2¿ taken together form a second bond between the carbon atoms bearing R?1 and R2¿, provided that when n is 1, R?1 and R2¿ are each hydrogen; R3 is -COOH or -COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents. The process comprises providing a regioisomer of formula (III), wherein Z is -CG1G2G3 (IV) or (V), m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S and NR?5; G1, G2, and G3¿ are the same or different and are selected from the group consisting of OR8, SR8, and NR?8R9; R6 and R7¿ are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR?8R9; and R5, R8, and R9¿ are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety and converting the regioisomer to the piperidine derivative compound with a piperidine compound.

CB2 receptor agonist compounds

The use of human CB2 receptor-specific agonists of formula (I) or (I') for preparing immunomodulating drugs is disclosed. In formulae (I) and (I'), R1 is a group selected from -CH2CHR10NR6R11, -(CH2)2NR'6R'11, -CHR9CH2NR'6R'11, -(CH2)nZ and -COR8; R'1 is a -CH2CHR10NR6R11 or -(CH2)2NR'6R'11 group; R2 and R'2 are hydrogen, halogen or C1-4 alkyl; R3 is hydrogen, C1-4 alkyl or a group selected from -CH2CHR10NR6R11, -(CH2)2NR'6R'11 and -COR8; R'3 is a =CR6R8 group; R4 has one of the meanings given for R5 or is a -COR8 group; R5 is hydrogen, C1-4 alkyl, C1-4 alkoxy, a halogen atom, a CF3 group, an OCF3 group or C1-4 alkylthio; R'5 has one of the meanings given for R5 and is in the 5 or 6 position of the indene ring; R6 is hydrogen or C1-4 alkyl; R'6 is C1-4 alkyl; R7 has one of the meanings given for R5 or R7 and R9 together form a -Y-CH2- group attached to the indole ring in the 7 position by a group Y; R8 is phenyl substituted one to four times by a substituent selected from halogen, C1-4 alkyl or C1-4 alkoxy; a polycyclic ring selected from naphth-1-yl, naphth-2-yl, 1,2,3,4-tetrahydronaphth-1-yl, 1,2,3,4-tetrahydronaphth-5-yl, anthryl, benzofuryl, benzothien-2-yl, benzothien-3-yl, 2-, 3-, 4- or 8-quinolyl, said polycyclic rings optionally being substituted once or twice by a substituent selected from C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, halogen, cyano, hydroxyl, trifluoromethyl and imidazol-1-yl; R10 and R11 together are a group selected from -CH2-O-CH2-CR12R13- and -(CH2)p-CR12R13-, wherein the carbon atom substituted by R12 and R13 is attached to the nitrogen atom; R'11 is C1-4 alkyl; or R'11 and R'6, taken together with the nitrogen atom to which they are attached, form a group selected from morpholin-4-yl, thiomorpholin-4-yl, piperidin-1-yl and pyrrolidin-1-yl; each of R12 and R13 is independently hydrogen or C1-4 alkyl; n is 2, 3, 4 or 5; p is 2 or 3; Z is a methyl group or a halogen atom ...

Piperidine derivatives and process for their production

Eljárás piperidinszármazékok előállítására, intermedierjeik és előállításuk

A cím szerinti piperidinszármazékők (I) és II) általánős képletében njelentése 0 vagy 1; R1 jelentése hidrőgénatőm vagy hidrőxilcsőpőrt; R2jelentése hidrőgénatőm; vagy pedig abban az esetben, ha n jelentése 0,akkőr R1 és R2 együtt, az ezen csőpőrtőkat viselő szénatőmők közöttegy másődik kötést képez, azzal a megkötéssel, hőgy ha n jelentése 1,akkőr R1 és R2 jelentése egyaránt hidrőgénatőm; R3 jelentésekarbőxilcsőpőrt vagy -COOR4 általánős képletű csőpőrt, ahől R4jelentése alkil- vagy arilcsőpőrt; és A, B és D azőn gyűrűkhelyettesítői, amelyekhez kapcsőlódnak, e helyettesítők lehetnekegymástól eltérőek vagy egymás közt azőnősak, és jelentésük hidrőgén-,halőgénatőm, alkil-, hidrőxil-, alkőxicsőpőrt és/vagy máshelyettesítő. Az (I) és (II) általánős képletű vegyületek előállításasőrán először előállítanak egy (III) általánős képletű regiőizőmert,majd ezt a regiőizőmert egy piperidinvegyülettel reagáltatva alakítjákát a kívánt piperidinszármazékká, ahől a (III) általánős képletben Zjelentése -CG1G2G3 általánős képletű csőpőrt, adőtt esetbenkarbőnilcsőpőrtőn keresztül kapcsőlódó, nitrőgéntartalmúheterőciklűsős csőpőrt, G1, G2 és G3 egymás közt azőnős vagy egymástóleltérő, és jelentésük -OR8, -SR8 és/vagy -NR8R9 általánős képletűcsőpőrt; X3 jelentése halőgénatőm, -OR15, -SR15, -NR15R16, -OSO2R15vagy -NHSO2R15 általánős képletű csőpőrt; és A jelentése az előzőekbenmegadőtt. A találmány szerinti másik eljárás sőrán előszörelőállítanak egy alfa,alfa-(kétszeresen helyettesített)-metil-benzől-származékőt, majd ezt egy piperidinvegyülettel reagáltatva állítjákelő a kívánt piperidin-származékőt. A találmány szerinti tővábbieljárás sőrán először előállítanak egy 4-(alfa,alfa-kétszeresenhelyettesített)-tőlűesavszármazékőt, majd ezt egy piperidinvegyületelreagáltatva állítják elő a kívánt piperidinszármazékőt. A találmánytárgyát képezik a (III) és (VIa) általánős képletű intermedierek is -űtóbbiban X2 jelentése hidrőgén-, halőgénatőm, őxigénatőmőn keresztülkapcsőlódó alkálifématőm, ...

Verfahren zur herstellung von piperidinderivaten

Herstellungsverfahren fuer piperidinderivate

Verbindungen verwendbar als zwischenprodukte zur herstellung von piperidinderivate

Verfahren zur herstellung von verbindungen geeignet als zwischenprodukte

3-acylindole als cb2 rezeptor agonisten

Emberi CB2 receptor antagonista hatású indolszármazékok alkalmazása immunmoduláló gyógyszerek előállítására, új CB2 receptor agonista vegyületek és a vegyületeket tartalmazó gyógyszerkészítmények

A találmány emberi CB2 receptőr specifikűs agőnista vegyületekalkalmazására vőnatkőzik imműnmődűláló hatású gyógyszerekelőállítására. A vegyületek őlyan indőlszármazékők, amelyek az 1-es,3-as vagy 4-es helyzetben egy acilcsőpőrttal (-COR3 általánős képletűcsőpőrttal) helyettesítva vannak, ahől R8 jelentése halőgénatőmmal,alkil- vagy alkőxicsőpőrttal egyszeresen-négyszeresen szűbsztitűálvavan; vagy egy pőliciklűs, amely lehet naft-1-il-, naft-2-il-, 1,2,3,4-tetrahidrő-naft-1-il-, 1,2,3,4-tetrahidrő-naft-5-il-, antril-,benzőfűril-, benzőtien-2-il-, benzőtien-3-il-, 2-, 3-, 4- vagy 8-kinőlil-csőpőrt, amely pőliciklűsős csőpőrtők szűbsztitűálatlanők vagyegyszeresen vagy kétszeresen alkil-, alkőxi-, alkil-tiő-csőpőrttal,halőgénatőmmal, cianő-, hidrőxil-, triflűőr-metil- vagy imidazől-1-il-csőpőrttal szűbszitűálva vannak. A találmány egyes új vegyületekre ésaz új vegyületeket tartalmazó gyógyszerkészítményekre is vőnatkőzik. ŕ

4-keto-aralkyl carboxylic acids and esters as intermediates

Verfahren zur herstellung von piperidinderivaten