| Original document(28 pages) 中文版 |
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 (XIVa), (XIV),b) converting the OH/=O function of compounds of formula XIV/XlVa into a leaving group P with a reagent containing a leaving group, selected from the group comprising POCl3, 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 H2SO4, HCI or acetic acid, to a compound of formula (I)The compouds of formula I are valuable intermediate for the manufacture of therapeutically active compounds which have NK- I antagonist activity. |
Application Number
申请号 |
200480023284 |
Application Date
申请日 |
2004.07.10 |
| Title 名称 |
Process for preparation of 4-aryl-nicotinamide derivatives
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Publication Number
公开号 |
1835922 |
Publication Date
公开日 |
2006.09.20 |
| Approval Pub. Date |
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Granted Pub. Date |
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| International Classification 分类号 |
C07D213/81,C07D213/82,C07D213/85,C07D213/64,A61K31/4427 |
Applicant(s) Name
申请人 |
Hoffmann La Roche |
| Address 地址 |
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| Inventor(s) Name 发明人 |
Goehring Wolfgang, Harrington Peter John, Hodges Lewis M., Johnston David A. |
| Attorney & Agent 代理人 |
huang gesheng an peidong |
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