N-[N-(tetrahydropyrido[2,3-D]pyrimidinylmethyl)-aminomethylbenzo

Details N-[N-(tetrahydropyrido[2,3-D]pyrimidinylmethyl)-aminomethylbenzo N-[N-(tetrahydropyrido[2,3-D]pyrimidinylmethyl)-aminomethylbenzo

1988-05-31

1989-10-03

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

544279, A61K 31505, C07D47100

Patent

active

048717460

ABSTRACT:
N-[N-(Tetrahydropyrido[2,3-d]pyrimidinylmethyl) aminomethylbenzoyl]glutamic acid derivatives are antineoplastic agents with an effect on one or more enzymes which utilize metabolic derivatives of folic acid. The compounds can be prepared by allowing a protected aminomethylbenzoylglutamic acid derivative to react with 2-amino-4-hydroxy-6-formylpyrido[2,3-d]pyrimidine, reducing the intermediate Schiff base, and subjecting the intermediate to catalytic hydrogenation. A typical embodiment is (S,S) N-[N-(2-amino-4-hydroxy-5,6,7,8- tetrahydropyrido-[2,3-d]pyrimidin-6-ylmethyl)-4-aminomethylbenzoyl]-glutam ic acid.

REFERENCES:
patent: 4596805 (1986-06-01), Jiang
Cutting, "Handbook of Pharmacology", Prentice-Hall, Norwalk, Connecticut, (1984), pp. 119-140.

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