发明名称 |
Process for the preparation of azabicycloc derivatives |
摘要 |
A process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof: <IMAGE> (I) wherein R1 represents <IMAGE> in which r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1; R2 is a group OR4, where R4 is C1-4 alkyl, C2-4 alkenyl or C2-4 alkynyl or a group OCOR5 where R5 is hydrogen or R4; and R3 is CN; said process comprising reacting a compound of formula (II): <IMAGE> (II) wherein R1' is R1 or a group convertible thereto, and R3' is an electron withdrawing group, with a source of nitrous acid, and thereafter converting the resulting =NOH group to =NR2 wherein R2 is as defined in formula (I), converting R1' and R3' when other than R1 and R3 to R1 and R3, and thereafter optionally forming a pharmaceutically acceptable salt.
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申请公布号 |
US5773619(A) |
申请公布日期 |
1998.06.30 |
申请号 |
US19950439616 |
申请日期 |
1995.05.12 |
申请人 |
SMITHKLINE BEECHAM P.L.C. |
发明人 |
BROMIDGE, STEVEN MARK;VOYLE, MARTYN;FARUK, EROL ALI;HUGHES, MARK JASON;KITTERINGHAM, JOHN;BORRETT, GARY THOMAS |
分类号 |
C07D487/18;C07D453/02;(IPC1-7):C07D453/02 |
主分类号 |
C07D487/18 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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