Processes and intermediates for preparing MCL1 inhibitors

Patent metadata

Field	Value
Publication number	US-11325891-B2
Application number	US-202017100107-A
Country	US
Kind code	B2
Filing date	Nov 20, 2020
Priority date	Nov 26, 2019
Publication date	May 10, 2022
Grant date	May 10, 2022

Abstract

The present disclosure provides methods for preparing MCL1 inhibitors or a salt thereof and related key intermediates.

First claim

What is claimed is:

1. A compound selected from:

or a salt thereof; wherein
R y is H or C 1-6 alkyl;
R 2 and R 3 are independently H or C 1-6 alkyl;
R 6 is halogen;
each R n is independently C 1-6 alkyl, or the two R n moieties join together to form a C 2-4 alkyl bridge, wherein the bridge is optionally substituted by one to four groups independently selected from C 1-3 alkyl and phenyl; and
R p is selected from H, —C(═O)—C 1-6 alkyl, —C(═O)-heteroaryl, —C(═O)—O—C 1-6 alkyl, and —C(═O)—O—C 1-6 alkyl-phenyl, wherein each phenyl or heteroaryl is optionally substituted with one to four groups independently selected from C 1-3 alkyl and —OC 1-3 alkyl;
wherein each heteroaryl has one to four heteroatoms, and each heteroatom is independently selected from N, O, and S; and wherein each heteroaryl has 5 to 10 ring members.

2. The compound of claim 1 selected from:

or a salt thereof.

Assignees

• Gilead Sciences Inc

Inventors

• Brak Katrien
• Bullock Kae M
• Cizio Greg
• Dao Kathy
• Dixon Darryl D
• Dunetz Joshua R
• Humphreys Luke D
• Huynh Valerie
• Ischay Michael A
• Johnson Trevor C
• Merit Jeffrey E
• Regens Christopher S
• Standley Eric A
• Steinhuebel Dietrich P
• Su Justin Y
• Wu Tao
• Young Marshall D

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• A61K31/553

  having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine · CPC title

• C07D513/10 Primary

  Spiro-condensed systems · CPC title

• C07C2602/28

  Hydrogenated naphthalenes · CPC title

• C07C2601/04

  with a four-membered ring · CPC title