公开(公告)号：EP1775347A2

公开(公告)日：2007-04-18

申请号：EP06021182.8

申请日：2006-10-09

Applicant: Procos S.p.A.

Inventor： Bertolini, Giorgio ,  Bogogna, Luigi ,  Pregnolato, Massimo ,  Terreni, Marco ,  Velardi, Francesco

IPC: C12P17/10 ,  C12P41/00

CPC classification number: C12P17/10 ,  C12P41/007

Abstract: A process for the enantiomeric resolution of 1-substituted 2-(aminomethyl)pyrrolidines of formula (I)

in which R is C1-C6 alkyl,
which process comprises the reaction of the racemic amine with benzyl acetate in acetonitrile in the presence of a lipase selected from Pseudomonas cepacia, Pseudomonas fluorescens or Candida rugosa lipases, to give the corresponding 1-substituted N-(pyrrolidin-2-yl-methyl)-acetamides of formula (II), with R configuration,

and the residual amine with S configuration,
and, if desired, the subsequent hydrolysis of the amide to obtain the amine with R configuration.

Abstract translation: 用于对映体拆分式（I）的1-取代的2-（氨基甲基）吡咯烷的方法，其中R是C 1 -C 6烷基，该方法包括在脂肪酶存在下外消旋胺与乙酸苄酯在乙腈中的反应 选自洋葱假单胞菌（Pseudomonas cepacia），荧光假单胞菌（Pseudomonas fluorescens）或假丝酵母（Candida rugosa）脂肪酶，得到具有R构型的相应的式（II）的1-取代的N-（吡咯烷-2-基 - 甲基） - 乙酰胺， 并且如果需要，随后水解酰胺以获得具有R构型的胺。

公开(公告)号：EP1775347A3

公开(公告)日：2007-07-25

申请号：EP06021182.8

申请日：2006-10-09

Applicant: Procos S.p.A.

Inventor： Bertolini, Giorgio ,  Bogogna, Luigi ,  Pregnolato, Massimo ,  Terreni, Marco ,  Velardi, Francesco

IPC: C12P17/10 ,  C12P41/00

CPC classification number: C12P17/10 ,  C12P41/007

Abstract: A process for the enantiomeric resolution of 1-substituted 2-(aminomethyl)pyrrolidines of formula (I)

in which R is C1-C6 alkyl,
which process comprises the reaction of the racemic amine with benzyl acetate in acetonitrile in the presence of a lipase selected from Pseudomonas cepacia, Pseudomonas fluorescens or Candida rugosa lipases, to give the corresponding 1-substituted N-(pyrrolidin-2-yl-methyl)-acetamides of formula (II), with R configuration,

and the residual amine with S configuration,
and, if desired, the subsequent hydrolysis of the amide to obtain the amine with R configuration.

公开(公告)号：EP0684224A1

公开(公告)日：1995-11-29

申请号：EP95103315.8

申请日：1995-03-08

Applicant: PROCOS S.p.A.

Inventor： Lavacchielli, Augusto ,  Fornaroli, Mirco ,  Velardi, Francesco

IPC: C07C217/16 ,  C07C213/08 ,  C07C255/13

CPC classification number: C07C255/13 ,  C07C213/02 ,  C07C217/16

Abstract: A process for the preparation of 2-(4-N-methylaminobutoxy)diphenylmethane of formula (I)

and the pharmaceutically acceptable acid salts thereof, starting from 2-(3-cyanopropoxy)diphenylmethane.

Abstract translation: 从2-（3-氰基丙氧基）二苯基甲烷开始制备式（I）的2-（4-N-甲基氨基丁氧基）二苯基甲烷及其药学上可接受的酸式盐的方法。