公开(公告)号：WO2018146306A1

公开(公告)日：2018-08-16

申请号：PCT/EP2018/053434

申请日：2018-02-12

申请人： PATHEON AUSTRIA GMBH & CO KG

发明人： KOHLS, Paul ,  PÖCHLAUER, Peter ,  STEINHOFER, Stefan ,  SCHUSTER, Christian

IPC分类号： C07C67/343 ,  C07C45/52 ,  C07C69/732 ,  C07C47/22

摘要： The invention pertains to a process for preparing a compound of formula (1), wherein R 1 is independently chosen from C 1 -C 6 alkyl, cycloalkyl, aralkyl and aryl, and R 2 , R 3 and R 4 are independently chosen from hydrogen and C 1 -C 6 alkyl, cycloalkyl, aralkyl and aryl; which process comprises the steps of: a) contacting a compound of formula (2), wherein R 1 and R 2 are as above and M + is a monovalent metal ion, with a compound of formula (3), wherein R 3 and R 4 are as above, to form a compound of formula (4); and b) followed by contacting the compound of formula (4) with an acid to give a compound of formula (1), wherein step (a) and/or step (b) are conducted in continuous mode.

公开(公告)号：WO2020126484A1

公开(公告)日：2020-06-25

申请号：PCT/EP2019/083541

申请日：2019-12-03

申请人： PATHEON AUSTRIA GMBH & CO KG

发明人： POECHLAUER, Peter ,  SELIG, Philipp ,  ZINGANELL, Christopher ,  PITZER, Julia ,  GLIEDER, Anton ,  KROUTIL, Wolfgang ,  STEINER, Kerstin

IPC分类号： C12P13/02 ,  C12N9/20

摘要： The present invention relates to a process for biocatalytic amidation of non-protected amino acids comprising the step of contacting a non-protected amino acid with an ammonia source in the presence of an organic solvent and an enzyme.

公开(公告)号：WO2018060512A1

公开(公告)日：2018-04-05

申请号：PCT/EP2017/074943

申请日：2017-10-02

申请人： PATHEON AUSTRIA GMBH & CO KG ,  DPX FINE CHEMICALS AUSTRIA GMBH & CO KG

发明人： DE VRIES, Andre ,  LEFORT, Laurent ,  VERZIJL, Gerard

IPC分类号： C07D211/56

CPC分类号： C07D211/56

摘要： The invention pertains to a process for the preparation of an amine having at least two chiral centers from a ketone having a chiral center at the a position and an amine comprising the steps of: (a) contacting a ketone having a chiral center at the a position and a primary amine thereby forming an imine; (b) contacting the imine with a reducing agent in the presence of an enantioselective catalyst to form an amine having at least two chiral centers, wherein step (a) and/or step (b) are conducted under racemization-enhancing conditions, wherein the racemization-enhancing conditions are achieved by addition of an acid and/or by addition of a salt of a primary amine and an acid, which salt is added in addition to or instead of the primary amine, and wherein the reducing agent is hydrogen.

摘要翻译： 本发明涉及制备具有至少两个手性中心的胺的方法，所述手性中心由在一个位置具有手性中心的酮和胺组成，所述方法包括以下步骤：（a）使 在α位具有手性中心的酮和伯胺，从而形成亚胺; （b）使亚胺与还原剂在对映选择性催化剂存在下接触以形成具有至少两个手性中心的胺，其中步骤（a）和/或步骤（b）在外消旋化增强条件下进行，其中 通过加入酸和/或通过加入伯胺和酸的盐实现外消旋化增强条件，除了伯胺之外或代替伯胺添加盐，并且其中还原剂是氢。 / p>