GOEHRING WOLFGANG,HARRINGTON PETER JOHN,HODGES LEWIS M,JOHNSTON DAVID A,RIMMLER GOESTA
申请号：
IN154/CHENP/2006
公开号：
IN251131B
申请日:
2006.01.12
申请国别(地区):
IN
年份:
2012
代理人:
摘要：
The present invention relates to a process for the manufacture of compounds of general formula wherein the substituents are as described in claim I characterized in that it comprises the steps of a) reacting a compound of formula (X), with a compound of formula (Xiii), to a compound of formula (XlVa), (XIV),b) converting the OH/=0 function of compounds of formula XlV/XIVa into a leaving group P with a reagent containing a leaving group, selected from the group comprising POCI3, PBr3, Mel or (F3CS02)2O to form a compound of formula (XV), wherein P is halogen or trifluoromethanesulfonate, c) substituting the leaving group P by R<2> with HR<2> to form a compound of formula (XVI) d) hydrolyzing the nitrile function in an acidic medium comprising H2S04, HCI or acetic acid, to a compound of formula (l)The compouds of formula I are valuable intermediate for the manufacture of therapeutically active compounds which have NK- I antagonist activity.
