发明授权
- 专利标题: Traceless solid phase synthesis of indole derivatives
- 专利标题(中): 无痕固相合成吲哚衍生物
-
申请号: US145692申请日: 1998-09-02
-
公开(公告)号: US5919947A公开(公告)日: 1999-07-06
- 发明人: Adrian Leonard Smith
- 申请人: Adrian Leonard Smith
- 申请人地址: GBX Hoddesdon
- 专利权人: Merck Sharp & Dohme Ltd.
- 当前专利权人: Merck Sharp & Dohme Ltd.
- 当前专利权人地址: GBX Hoddesdon
- 优先权: GBX9718837 19970904
- 主分类号: C07D209/08
- IPC分类号: C07D209/08 ; C07D209/12 ; C07D209/14
摘要:
The present invention relates to a traceless solid phase process for the preparation of an indole derivative, which comprises the following steps:(1) reaction of an optionally substituted 2-iodoaniline derivative via the nitrogen atom of the NH.sub.2 moiety thereof with a dihydropyran-functionalized polymeric resin under conditions effective to form an aminal linkage;(2) reaction of the tetrahydropyran aminal derivative thereby obtained with an acetylene derivative in the presence of a transition metal catalyst under conditions effective to promote indole formation;(3) treatment of the product thereby obtained with acid, whereby the aminal linkage is cleaved and the desired indole derivative is liberated from the resin; and(4) isolation of the desired indole derivative thereby obtained.
公开/授权文献
信息查询