公开(公告)号：US20050261341A1

公开(公告)日：2005-11-24

申请号：US11114381

申请日：2005-04-26

申请人： Wolfgang Laux ,  Gerard Guillamot ,  Frederick Laskovics ,  Chi-Hsin King ,  James Hitt ,  Sandra Stolz-Dunn ,  Ian Tomlinson ,  Johannes Koek

发明人： Wolfgang Laux ,  Gerard Guillamot ,  Frederick Laskovics ,  Chi-Hsin King ,  James Hitt ,  Sandra Stolz-Dunn ,  Ian Tomlinson ,  Johannes Koek

IPC分类号： A61K31/445 ,  C07D211/20 ,  C07D211/22

CPC分类号： C07D211/22 ,  C07D211/32

摘要： The present invention provides various processes for the preparation of (R)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol. These processes may be characterized by the following scheme:

摘要翻译： 本发明提供制备（R）-α-（2,3-二甲氧基苯基）-1- [2-（4-氟苯基）乙基] -4-哌啶甲醇的各种方法。 这些过程可以通过以下方案来表征：

公开(公告)号：US20090227798A1

公开(公告)日：2009-09-10

申请号：US12403768

申请日：2009-03-13

申请人： Wolfgang Laux ,  Gerard Guillamot ,  Frederick M. Laskovics ,  Chi-Hsin R. King ,  James E. Hitt ,  Sandra K. Stolz-Dunn ,  Ian A. Tomlinson ,  Johannes Nicolaas Koek

发明人： Wolfgang Laux ,  Gerard Guillamot ,  Frederick M. Laskovics ,  Chi-Hsin R. King ,  James E. Hitt ,  Sandra K. Stolz-Dunn ,  Ian A. Tomlinson ,  Johannes Nicolaas Koek

IPC分类号： C07D211/32 ,  C07D211/22

CPC分类号： C07D211/22 ,  C07D211/32

摘要： The present invention provides various processes for the preparation of (R)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol. These processes may be characterized by the following scheme:

摘要翻译： 本发明提供制备（R）-α-（2,3-二甲氧基苯基）-1- [2-（4-氟苯基）乙基] -4-哌啶甲醇的各种方法。 这些过程可以通过以下方案来表征：

公开(公告)号：US09145570B2

公开(公告)日：2015-09-29

申请号：US13812978

申请日：2011-07-29

申请人： Juliette Martin ,  Gerard Guillamot ,  Laurent Fourage ,  Denis Wahler

发明人： Juliette Martin ,  Gerard Guillamot ,  Laurent Fourage ,  Denis Wahler

IPC分类号： C12P7/62 ,  C12P9/00 ,  C12P11/00 ,  C12P13/02 ,  C12P17/06

CPC分类号： C12P7/62 ,  C12P9/00 ,  C12P11/00 ,  C12P13/02 ,  C12P17/06

摘要： The invention relates to an enzymatic acylation method including at least the following steps of: contacting at least one compound having at least one function selected from among the amine, alcohol, or thiol functions, at least one microorganism having an acyl transfer activity and/or an acyl transfer enzyme, and at least one acylphosphonate donor of formula (I), where: R is an alkyl, alkene, alkyne, aryl, or aralkyl radical, or is —ORa, —SRa, —NRaRb, where Ra and Rb are identical or different and are H, an alkyl, alkene, alkyne, aryl or aralkyl radical, the alkyl, alkene, alkyne, aryl or aralkyl radicals being optionally substituted; X is O or S; Y and Z, which are identical or different, are —OR1, —OR2, —SR1, —SR2, —NR′1R″1, —NR′2R″2; R1, R2, R′1, R′2, R″1 and R″2, which are identical or different, are an alkyl, alkene, alkyne, aryl or aralkyl radical, said alkyl, alkene, alkyne, aryl or aralkyl radicals being optionally substituted; and recovering the compound including at least one acyl function, said function being selected from among the amine, alcohol, or thiol functions.

摘要翻译： 本发明涉及酶促酰化方法，其包括至少以下步骤：使至少一种具有至少一种选自胺，醇或硫醇官能团的官能团的化合物，至少一种具有酰基转移活性的微生物和/或 酰基转移酶和至少一种式（I）的酰基膦酸盐供体，其中：R是烷基，烯烃，炔烃，芳基或芳烷基，或是-OR a，-SR a，-NR a R b，其中R a和R b是 烷基，烯烃，炔烃，芳基或芳烷基，烷基，烯烃，炔烃，芳基或芳烷基任选被取代; X是O或S; Y和Z相同或不同，为-OR1，-OR2，-SR1，-SR2，-NR'1R“1，-NR'2R”2; 所述烷基，烯烃，炔烃，芳基或芳烷基，R 1，R 2，R'1，R'2，R“1和R”2是相同或不同的，所述烷基，烯烃，炔，芳基或芳烷基 任选取代; 并回收包含至少一个酰基官能团的化合物，所述官能团选自胺，醇或巯基官能团。

公开(公告)号：US20070106079A1

公开(公告)日：2007-05-10

申请号：US10583472

申请日：2004-12-15

申请人： Valéry Dambrin ,  Jean-Yves Lenoir ,  Jean-Marie Schneider ,  Gerard Guillamot ,  Michel Follet ,  Abram Becker

发明人： Valéry Dambrin ,  Jean-Yves Lenoir ,  Jean-Marie Schneider ,  Gerard Guillamot ,  Michel Follet ,  Abram Becker

IPC分类号： C07D277/04 ,  C07D263/02

CPC分类号： C07C323/67 ,  C07C303/40 ,  C07C311/37 ,  C07C311/46 ,  C07C319/20 ,  C07D263/06 ,  C07D263/14 ,  C07D263/24 ,  C07D277/04 ,  C07D277/10 ,  C07D277/14 ,  Y02P20/55

摘要： A subject matter of the present invention is novel intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts, and also the associated preparation process.

摘要翻译： 本发明的主题是用于合成（R） - 桑索罗辛及其药学上可接受的盐的新型中间体，以及相关的制备方法。

公开(公告)号：US20130130337A1

公开(公告)日：2013-05-23

申请号：US13812978

申请日：2011-07-29

申请人： Juliette Martin ,  Gerard Guillamot ,  Laurent Fourage ,  Denis Wahler

发明人： Juliette Martin ,  Gerard Guillamot ,  Laurent Fourage ,  Denis Wahler

IPC分类号： C12P7/62 ,  C12P9/00

CPC分类号： C12P7/62 ,  C12P9/00 ,  C12P11/00 ,  C12P13/02 ,  C12P17/06

摘要： The invention relates to an enzymatic acylation method including at least the following steps of: contacting at least one compound having at least one function selected from among the amine, alcohol, or thiol functions, at least one microorganism having an acyl transfer activity and/or an acyl transfer enzyme, and at least one acylphosphonate donor of formula (I), where: R is an alkyl, alkene, uikyne, aryl, or aralkyl radical, or is —ORa, —SRa, —NRaRb, where Ra and Rb are identical or different and are H, an alkyl, alkene, alkyne, aryl or aralkyl radical, the alkyl, alkene, alkyne, aryl or aralkyl radicals being optionally substituted; X is O or S; Y and Z, which are identical or different, are —OR1, —OR2, —SR1, —SR2, —NR′1R″1, —NR′2R″2; R1, R2, R′1, R′2, R″1 and R″2, which are identical or different, are an alkyl, alkene, alkyne, aryl or aralkyl radical, said alkyl, alkene, alkyne, aryl or aralkyl radicals being optionally substituted; and recovering the compound including at least one acyl function, said function being selected from among the amine, alcohol, or thiol functions.

摘要翻译： 本发明涉及酶促酰化方法，其包括至少以下步骤：使至少一种具有至少一种选自胺，醇或硫醇官能团的官能团的化合物，至少一种具有酰基转移活性的微生物和/或 酰基转移酶和至少一种式（I）的酰基膦酸盐供体，其中：R是烷基，烯烃，乙炔基，芳基或芳烷基，或是-OR a，-SR a，-NR a R b，其中R a和R b是 烷基，烯烃，炔烃，芳基或芳烷基，烷基，烯烃，炔烃，芳基或芳烷基任选被取代; X是O或S; Y和Z相同或不同，为-OR1，-OR2，-SR1，-SR2，-NR'1R'1，-NR'2R'2; R1，R2，R'1，R'2，R'1和R'2相同或不同，是烷基，烯烃，炔，芳基或芳烷基，所述烷基，烯烃，炔烃，芳基或 芳烷基任选被取代; 并回收包含至少一个酰基官能团的化合物，所述官能团选自胺，醇或巯基官能团。