Methods for the synthesis of chemical compounds having PDE-IV inhibitory activity

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United States of America Patent

PATENT NO 5864037
SERIAL NO

08659767

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Abstract

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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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Patent Owner(s)

Patent OwnerAddress
EURO-CELTIQUE S A2350 LUXEMBOURG

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Cavalla, David Cambridge, GB3 28 74
Chasin, Mark Manalapan, NJ 116 12920
Hofer, Peter Liestal, CH 56 1088

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