Process for preparing 10-deazaaminopterins and 5,10-and 8,10-did

Details Process for preparing 10-deazaaminopterins and 5,10-and 8,10-did Process for preparing 10-deazaaminopterins and 5,10-and 8,10-did

1993-03-09

1994-12-20

Daus, Donald R.

Organic compounds -- part of the class 532-570 series

Organic compounds

Plural nitrogens bonded directly to the pteridine ring system

544279, 548136, 548201, 546318, 546326, C07D47508

Patent

active

053747267

ABSTRACT:
A process is provided for the preparation of 10-deazaaminopterins and 5,10- and 8,10-dideazaaminopterins starting from the corresponding homoterephthalic acid diester coupling the corresponding dicarboxylic acid diester having the formula: ##STR1## with the corresponding diaminopterin 6-methylene halide having the formula: ##STR2## thereby forming a pteroic acid diester having the formula: ##STR3## hydrolysing the two ester groups to form the corresponding carboxylic acid groups, and then monodecarboxylating the diacid, thereby removing the carboxylic acid group attached to the carbon alpha to the A group and forming a pteroic acid.

REFERENCES:
patent: 4369319 (1983-01-01), De Graw et al.
patent: 4460591 (1984-07-01), De Graw et al.
patent: 4746659 (1988-05-01), De Graw et al.

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