IP Library Granted Patent US 8,476,440
Granted Patent B2
US 8,476,440 · App. 13/551,774 · Granted Jul 2, 2013

Process for preparing an intermediate to mu opioid receptor antagonists

Inventors: Pierre-Jean Colson (San Francisco, CA); Ying Yu (Sunnyvale, CA); Daniel D. Long (San Francisco, CA); Ioanna Stergiades (San Francisco, CA)
Assignee: Theravance, Inc.
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Quick Facts
Patent No.
US 8,476,440
App. No.
13/551,774
Granted
Jul 2, 2013
Kind
B2
Abstract

The invention provides an efficient method for preparing 3-endo-(8-azabicyclo[3.2.1]oct-3-yl)benzamide by hydrogenation, under controlled conditions, of an amino-protected 3-(8-azabicyclo[3.2.1]oct-2-en-3-yl)benzamide intermediate in which the amino-protecting group is removable by catalytic hydrogenation.

Claims (4)

1. A compound of formula 5:

wherein P 1 is an amino-protecting group and —OR x is p-toluene sulfonate.

2. The compound of claim 1 wherein P 1 is benzyl.

3. The compound of claim 1 wherein P 1 is tert-butoxycarbonyl.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 5, 2014
From: THERAVANCE, INC.
To: THERAVANCE BIOPHARMA R&D IP, LLC
Reel/Frame 033127/0180 →
Continuity (4)
Division 13047309 · Mar 14, 2011
Division 12218383 · Jul 15, 2008
Provisional Application 60961353 · Jul 20, 2007
Related Publication 20130079523A1 · Mar 28, 2013