公开(公告)号：EP2046733B1

公开(公告)日：2011-10-05

申请号：EP06776610.5

申请日：2006-08-04

申请人： F.I.S. Fabbrica Italiana Sintetici S.p.A.

发明人： SERAFINI, Siro ,  MOTTERLE, Riccardo ,  BRASOLA, Elena

IPC分类号： C07C269/04 ,  C07D249/18

CPC分类号： C07C269/04 ,  C07D249/18 ,  C07C271/22

摘要： A process for the preparation of ω-alkoxycarbonylamino-α-aminoacids and α,ω orthogonally diprotected diaminoacids from α,ω-diaminoacids using 1- alkoxycarbonylbenzotriazoles as protecting agents is disclosed. In an alternative embodiment, carbamoylating agents in the presence of benzotriazoles are used instead of 1-alkoxycarbonylbenzotriazoles. This reaction is preferably applied to the preparation of ε- alkoxycarbonyllysines from lysine. A process for the preparation of t-butoxycarbonylbenzotriazoles and novel complexes of ω-alkoxycarbonylamino-α-aminoacids with benzotriazoles are also disclosed.

公开(公告)号：EP3280714B1

公开(公告)日：2019-02-06

申请号：EP16741296.4

申请日：2016-07-18

申请人： F.I.S. Fabbrica Italiana Sintetici S.p.A.

发明人： BRASOLA, Elena ,  TOMASI, Filippo ,  PERUZZI, Loris

IPC分类号： C07D471/04

公开(公告)号：EP3280714A1

公开(公告)日：2018-02-14

申请号：EP16741296.4

申请日：2016-07-18

申请人： F.I.S. Fabbrica Italiana Sintetici S.p.A.

发明人： BRASOLA, Elena ,  TOMASI, Filippo ,  PERUZZI, Loris

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  B01D11/02 ,  C07B63/00 ,  C07D413/04 ,  C07D413/14 ,  G01N30/36 ,  G01N30/7233 ,  G01N2030/027

摘要： Object of the present invention are dimer impurities of the active ingredient Apixaban, analytical methods for identifying and/or quantifying them and a synthetic method for removing said impurities from Apixaban and synthetic precursors thereof.

公开(公告)号：EP2046733A1

公开(公告)日：2009-04-15

申请号：EP06776610.5

申请日：2006-08-04

申请人： F.I.S. Fabbrica Italiana Sintetici S.p.A.

发明人： SERAFINI, Siro ,  MOTTERLE, Riccardo ,  BRASOLA, Elena

IPC分类号： C07C269/04 ,  C07D249/18

CPC分类号： C07C269/04 ,  C07D249/18 ,  C07C271/22

摘要： A process for the preparation of ω-alkoxycarbonylamino-α-aminoacids and α,ω orthogonally diprotected diaminoacids from α,ω-diaminoacids using 1- alkoxycarbonylbenzotriazoles as protecting agents is disclosed. In an alternative embodiment, carbamoylating agents in the presence of benzotriazoles are used instead of 1-alkoxycarbonylbenzotriazoles. This reaction is preferably applied to the preparation of ε- alkoxycarbonyllysines from lysine. A process for the preparation of t-butoxycarbonylbenzotriazoles and novel complexes of ω-alkoxycarbonylamino-α-aminoacids with benzotriazoles are also disclosed.