Title:
4-アリル-ニコチンアミド誘導体の製造方法
Document Type and Number:
Japanese Patent JP4575918
Kind Code:
B2
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.
Inventors:
Gering, Wolfgang
Harrington, Peter John
Hodges, Louis M
Johnston, David A
Rimlar, Gesta
Harrington, Peter John
Hodges, Louis M
Johnston, David A
Rimlar, Gesta
Application Number:
JP2006519843A
Publication Date:
November 04, 2010
Filing Date:
July 10, 2004
Export Citation:
Assignee:
F. HOFFMANN-LA ROCHE AKTIENGESELLSCHAFT
International Classes:
C07D213/82; C07D213/85; C07D411/04
Domestic Patent References:
| JP2001151755A | ||||
| JP2000247957A |
Foreign References:
| WO2002008232A1 |
Attorney, Agent or Firm:
Hajime Tsukuni
Fumio Shinoda
Fumio Shinoda