6,6-DISUBSTITUTED PTERIDINE DERIVATIVE

Japanese Patent JP2598609

B2

PURPOSE: To provide a 2-aminodisubstituted alkylaminopyrimidine derivative which gives 6,6-disubstituted pteridine derivative closely related-to 6,6- disubstituted tetrahydropteridines having thymidylate synthetase inhibiting activities.
CONSTITUTION: 2-Amino-6-chloro-4-hydroxy-5-nitropyrimidine represented by formula I is reacted with a 1,2-diaminoethane derivative of formula II (wherein R3 and R4 are each 1-12C alkyl, 2-7C alkenyl, 3-10C cycloalkyl or the like; and R5 is H, 1-6C alkyl, 3-7C cycloalkyl, phenyl or the like), e.g. 1,2-diamino-2- phenylpropane and the like, in anhydrous ethanol under heat and followed, if necessary, by reduction of the nitro group to give a 2-amino-2-disubstituted alkylaminopyrimidine derivative, represented by formula III (wherein R1 and R2 are each H, OH, 1-4C alkoxy, amino, cycloamino, 1-3C alkylthio or the like; and X is H, NH2 or NO2), useful as an intermediate of a 6,6-disubstituted pteridine derivative or the like.

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Eyring, Jun
Bailey, Stephen

JP7805494A

April 09, 1997

March 24, 1994

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SOUTH ALABAMA MEDICAL SCIENCE FOUNDATION

A61K31/505; A61K31/519; A61P25/00; A61P25/24; A61P25/26; A61P43/00; C07D239/42; C07D239/47; C07D239/48; C07D239/50; C07D401/12; C07D475/00; C07D475/04; (IPC1-7): C07D239/42; C07D239/47; C07D239/48; C07D239/50; C07D401/12

Kazuo Sato (2 outside)

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