Invention Grant
- Patent Title: Process for preparation of pyridine derivatives
- Patent Title (中): 吡啶衍生物的制备方法
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Application No.: US10888912Application Date: 2004-07-09
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Publication No.: US07288658B2Publication Date: 2007-10-30
- Inventor: Wolfgang Goehring , Peter John Harrington , Lewis M Hodges , David A Johnston , Goesta Rimmler
- Applicant: Wolfgang Goehring , Peter John Harrington , Lewis M Hodges , David A Johnston , Goesta Rimmler
- Applicant Address: US NJ Nutley
- Assignee: Hoffmann-La Roche Inc.
- Current Assignee: Hoffmann-La Roche Inc.
- Current Assignee Address: US NJ Nutley
- Agent George W. Johnston; Patricia S. Rocha-Tramaloni; Kimberly J. Prior
- Priority: EP0301559 20030715
- Main IPC: C07D401/02
- IPC: C07D401/02 ; C07D213/02

Abstract:
The present invention relates to a process for the manufacture of compounds of formula wherein the substituents are as described herein which comprises the steps of a) reacting a compound of formula with a compound of formula to form a compound of formula b) converting the OH/═O function of compounds of formula XIV/XIVa into a leaving group P with a reagent containing a leaving group, selected from POCl3, PBr3, MeI and (F3CSO2)2O to form a compound of formula wherein P is halogen or trifluoromethanesulfonate; c) substituting R2 for the leaving group P by reacting compound XV with HR2 to form a compound of formula and d) hydrolyzing the nitrile function in an acidic medium selected from H2SO4, HCl and acetic acid, to form a compound of formula I The compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds which have NK-1 antagonist activity.
Public/Granted literature
- US20050014792A1 Process for preparation of pyridine derivatives Public/Granted day:2005-01-20
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