公开(公告)号：US20200223832A1

公开(公告)日：2020-07-16

申请号：US16741276

申请日：2020-01-13

申请人： Apotex Inc.

发明人： Michael R. Emmett ,  Prabhudas Bodhuri ,  Yajun Zhao ,  Eduardo Gustavo Cammisa ,  Stuart P. Green

IPC分类号： C07D405/12 ,  C07D317/60 ,  C07C211/52

摘要： The present invention provides processes for the preparation of Tezacaftor, as well as intermediates useful in the preparation thereof. In particular, processes are provided for the preparation of a compound of Formula (3), and its conversion to Tezacaftor (1).

公开(公告)号：US11046638B2

公开(公告)日：2021-06-29

申请号：US17095707

申请日：2020-11-11

申请人： Apotex Inc.

发明人： Avedis Karadeolian ,  Fabio E. S. Souza ,  Michael R. Emmett ,  Allan W. Rey

IPC分类号： C07C213/02 ,  B01J23/755 ,  C07C217/60

摘要： The present invention provides processes for the preparation of zuclomiphene, as well as intermediates useful in the preparation thereof. In particular, processes are provided for the carbometallation of diphenylacetylene with a compound of Formula (3) to afford either zuclomiphene or an intermediate which is converted to zuclomiphene.

公开(公告)号：US20210147337A1

公开(公告)日：2021-05-20

申请号：US17095707

申请日：2020-11-11

申请人： Apotex Inc.

发明人： Avedis Karadeolian ,  Fabio E. S. Souza ,  Michael R. Emmett ,  Allan W. Rey

IPC分类号： C07C213/02 ,  B01J23/755

摘要： The present invention provides processes for the preparation of zuclomiphene, as well as intermediates useful in the preparation thereof. In particular, processes are provided for the carbometallation of diphenylacetylene with a compound of Formula (3) to afford either zuclomiphene or an intermediate which is converted to zuclomiphene.

公开(公告)号：US10513504B2

公开(公告)日：2019-12-24

申请号：US16294259

申请日：2019-03-06

申请人： Apotex Inc.

发明人： Prabhudas Bodhuri ,  Alfredo Paul Ceccarelli ,  Michael R. Emmett ,  Avedis Karadeolian ,  Fabio E. S. Souza ,  Gamini Weeratunga ,  Boris Gorin

IPC分类号： C07D401/04 ,  C07C231/12 ,  C07D249/04 ,  C07D207/40 ,  C07D233/56 ,  C07C237/30

摘要： The present invention provides processes for the preparation of Apalutamide (1), as well as intermediates useful in the preparation thereof. In particular, the process of the invention utilizes the intermediate compound of Formula (2), wherein G is OH or a leaving group, which provides improvements over the known processes for the preparation of Apalutamide (1).

公开(公告)号：US20190276424A1

公开(公告)日：2019-09-12

申请号：US16294259

申请日：2019-03-06

申请人： Apotex Inc.

发明人： Prabhudas Bodhuri ,  Alfredo Paul Ceccarelli ,  Michael R. Emmett ,  Avedis Karadeolian ,  Fabio E. S. Souza ,  Gamini Weeratunga ,  Boris Gorin

IPC分类号： C07D401/04 ,  C07C231/12 ,  C07C237/30 ,  C07D207/40 ,  C07D233/56 ,  C07D249/04

摘要： The present invention provides processes for the preparation of Apalutamide (1), as well as intermediates useful in the preparation thereof. In particular, the process of the invention utilizes the intermediate compound of Formula (2), wherein G is OH or a leaving group, which provides improvements over the known processes for the preparation of Apalutamide (1).