公开(公告)号：WO2022076623A1

公开(公告)日：2022-04-14

申请号：PCT/US2021/053859

申请日：2021-10-06

Applicant: AMGEN INC.

Inventor： BEAVER, Matthew G. ,  CORBETT, Michael T. ,  FANG, Yuanqing ,  FORD, David D. ,  PARSONS, Andrew T. ,  ST-PIERRE, Gabrielle ,  TELMESANI, Reem

IPC: C07D471/04

Abstract: Provided herein is a process comprising heating a composition comprising (P)-compound A or a salt thereof and a solvent to a temperature of 250°C to 350°C to form racemized compound A. Also provided is a process for isolating (P)-compound A from a composition comprising (P)‑compound A and a tartrate, as described herein. Further provided herein, is a process for isolating a free acid of a tartrate or a hydrate thereof from a composition comprising a tartrate, (P)‑compound A, and an organic solvent. [Insert Structure] (A).

公开(公告)号：WO2021226009A1

公开(公告)日：2021-11-11

申请号：PCT/US2021/030548

申请日：2021-05-04

Applicant: AMGEN INC.

Inventor： SMITH, Austin G. ,  CORBETT, Michael T. ,  LANGILLE, Neil Fred ,  BAUCOM, Kyle D. ,  DORNAN, Peter K. ,  ST-PIERRE, Gabrielle ,  ROOSEN, Philipp C. ,  CUI, Sheng ,  PROFETA, Roberto

IPC: C07D249/18 ,  C07C69/16 ,  C07C69/78 ,  C07C309/23 ,  C07D513/08 ,  C07D513/10

Abstract: Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound F, or a salt thereof, wherein R1 and OPG2 are described herein. Compound F can be useful in synthesizing compound A1, or a salt of solvate thereof, and compound A2, or a salt of solvate thereof.

公开(公告)号：WO2021226168A1

公开(公告)日：2021-11-11

申请号：PCT/US2021/030780

申请日：2021-05-05

Applicant: AMGEN INC.

Inventor： SMITH, Austin G. ,  TEDROW, Jason S. ,  ST-PIERRE, Gabrielle ,  THIEL, Oliver Ralf ,  HUANG, Liang ,  ROOSEN, Philipp C. ,  COLYER, John T. ,  BAUCOM, Kyle D. ,  ERICSON, Ari ,  BEAVER, Matthew G. ,  SANGODKAR, Rahul P. ,  LOVETTE, Michael A. ,  MILBURN, Robert Ronald ,  CHERNEY, Alan H. ,  CUI, Sheng

IPC: C07D267/16 ,  C07D281/00 ,  C07D513/08 ,  A61P35/00 ,  A61K31/553

Abstract: Provided herein are processes for synthesizing Mcl-1 inhibitors and intermediates such as compound F that can be used to prepare them where the variable PG is as defined herein. In particular, provided herein are processes for synthesizing compound A1, and salts or solvates thereof and compound A2, and salts and solvates thereof.