Methods for the synthesis of chemical compounds having PDE-IV inhibitory activity
申请(专利)号：
US08/659767
申请日期：
19960606
公开/公告号：
US05864037A
公开/公告日期：
19990126
申请(专利权)人：
EURO-CELTIQUE S.A.
被引量：
摘要：
Disclosed is a process for the preparation of a compound of Formula IV having the structure: ##STR1## wherein R.sub.6 is N(R.sub. 6a) (R.sub.6b); R.sub.3 represents a C.sub.2-8, alkyl which is unbranched or branched and unsubstituted or substituted; C.sub.3-8 cycloalkyl which is unsubstituted or substituted; C.sub.4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted; aryl or benzyl which is optionally unsubstituted or substituted; ar(C.sub.1-4)alkyl; a heterocyclyl group, ring optionally substituted; heterocyclyl (C.sub.1 -C.sub.4) alkyl ring optionally substituted;which comprises:(a) treating a compound of Formula I: ##STR2## with an effective amount of a dethionating agent to produce a compound of Formula II: ##STR3## (b) treating a compound of Formula II with an effective halogenating agent under conditions effective to produce a compound of Formula III: ##STR4## and (c) treating a compound of Formula III with an effective aminating agent under conditions effective to produce a compound of Formula IV.
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