Processes for the preparation of uracil derivatives

Patent metadata

Field	Value
Publication number	US-9868706-B2
Application number	US-201715406476-A
Country	US
Kind code	B2
Filing date	Jan 13, 2017
Priority date	Nov 7, 2007
Publication date	Jan 16, 2018
Grant date	Jan 16, 2018

Abstract

The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.

First claim

What is claimed is:

1. A process for preparing a compound of structure:

wherein:
R 1a , R 1b and R 1c are the same or different and independently hydrogen, halogen, C 1-4 alkyl, hydroxy or alkoxy;
R 2a and R 2b are the same or different and independently hydrogen, halogen, trifluoromethyl, cyano or —SO 2 CH 3 ;
R 3 is hydrogen or methyl; and
comprising:
reacting a compound of structure (VII):

wherein R 2a , R 2b and R 3 are as defined above;
with a compound of structure (VIII):

wherein R is H or C 1-4 alkyl, R′ is H or C 1-4 alkyl or R and R′ taken together form C 1-6 alkanediyl; and
R 1a , R 1b , and R 1c are as defined above.

2. The process of claim 1 wherein R 1a is halogen, R 1b is methoxy and R 1c is H.

Assignees

• Chou Helen
• Neurocrine Biosciences Inc

Inventors

• Gallagher Donald J
• Treiber Laszlo R
• Hughes Robert Michael
• Campopiano Onorato
• Wang Peng
• Zhao Yuxin
• Chou Shine K
• Ouellette Michael Allen
• Hettinger Donald Nicholas

Classifications

• C07D239/54 Primary

  as doubly bound oxygen atoms or as unsubstituted hydroxy radicals · CPC title

• A61P15/00

  Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives · CPC title

• A61K9/146

  with organic macromolecular compounds · CPC title

• C07D239/553

  with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil · CPC title

• A61K9/1688

  resulting in pure drug agglomerate optionally containing up to 5% of excipient · CPC title