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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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)
Provisional Application
60961353
· Jul 20, 2007