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Cyclization for preparing antifolate compounds
 
   
Document Number
US Patent 5969136
Issued Date
October 19, 1999
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Abstract
This invention provides a process for preparing a compound of formula III ##STR1## wherein R.sup.1 is bromo, iodo or COOR.sup.2 ; R.sup.2 is H, C.sub.1 -C.sub.4 alkyl, phenyl which may be substituted or benzyl; and A is a 5- or 6-membered aromatic residue which may contain up to three hetero atoms and which may optionally be substituted with one or two groups selected from the group consisting of halo, hydroxy, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy; or a salt thereof, which comprises (a) reacting a compound of formula I ##STR2## wherein R is C.sub.1 -C.sub.4 alkyl or phenyl which may be substituted; and R.sup.1, R.sup.2, and A are as defined above; or a salt thereof, with a sulfurization agent; (b) cyclizing the reaction product from step (a) with guanidine; and (c) optionally salifying the reaction product from step (b).
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Cyclization for preparing antifolate compounds - US Patent 5969136 Drawing
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Number of Claims:
12
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Owner
Eli Lilly and Company (Indianapolis, IN)
Published
October 19, 1999
Application Number
08/096,099
Filed
July 23, 1993
US Classification
544/279   546/212 546/214 546/221
Int'l Classification
C07D   211/00   (20060101)   C07D   211/78   (20060101)   C07D   471/04   (20060101)   C07D   471/00   (20060101)  
Examiner
Parent Case
This application is a Continuation-In-Part of Ser. No. 07/961,572, filed Oct. 15, 1992, now abandoned.
USPTO Field of Search
544/276   544/279  
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