Cyclized 5,10-dideazaaminopterin compounds

Details Cyclized 5,10-dideazaaminopterin compounds Cyclized 5,10-dideazaaminopterin compounds

1989-08-29

1991-12-31

Shah, Mukund J.

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

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

544299, C07D23970

Patent

active

050774042

ABSTRACT:
5,10-Dialkyl substituted 5,10-dideazaaminopterins and a cyclized derivative thereof are disclosed as potent antineoplastic agents. Also disclosed is an improved process for the preparation of 10-ethyl-10-deazaaminopterin using the intermediate methyl 4-[[2-(2,4-diamino-6-pteridinyl)-1-ethyl]ethenyl]benzoate.

REFERENCES:
patent: 4460591 (1984-07-01), DeGraw et al.
patent: 4684653 (1987-08-01), Taylor et al.
Synthesis of the Antileukemic Agents . . . , Taylor et al., J. Med. Chem., 28, 914-921 (1985).
Synthesis of 5,10-Dideazaaminopterin . . . , DeGraw et al., J. Heterocyclic Chem., 23, 1-4 (1986).
Synthesis and Antifolate Activity . . . , Piper et al., J. Med. Chem., 31, 2164-2169.

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