公开(公告)号：US20250129072A1

公开(公告)日：2025-04-24

申请号：US18987521

申请日：2024-12-19

Applicant: AMGEN INC.

Inventor： Michal ACHMATOWICZ ,  John T. COLYER ,  Michael T. CORBETT ,  Daniel J. GRIFFIN ,  Andrew T. PARSONS ,  Joanna ROBINSON ,  Kyle QUASDORF

IPC: C07D471/04

Abstract: Provided herein is a process for preparing compound A comprising (a) admixing 2-isopropyl-4-methylpyridin-3-amine (Compound B), or a salt thereof, a first base, and a reactive compound comprising phosgene or a phosgene equivalent in an organic solvent to form 3-isocyanato-2-isopropyl-4-methylpyridine (Compound C); (b) admixing Compound C and 2,6-dichloro-5-fluoronicotinamide (Compound D) to form 2,6-dichloro-5-fluoro-N-((2-isopropyl-4-methylpyridin-3-yl)carbamoyl)nicotinamide (Compound E); and (c) admixing Compound E and a second base to form a product mixture comprising Compound A and the second base. Also provided herein is a process for synthesizing AMG 510 comprising using Compound A prepared according to the disclosed processes

公开(公告)号：US20230167130A1

公开(公告)日：2023-06-01

申请号：US17922619

申请日：2021-05-05

Applicant: AMGEN INC.

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

IPC: C07D513/10 ,  C07D267/16

CPC classification number: C07D513/10 ,  C07D267/16

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.