Method for preparing n-¬4-¬¬(2,4-diamino-6- pteridinyl)-...

C - Chemistry – Metallurgy – 07 – D

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260/242.1

C07D 475/00 (2006.01) C07D 475/08 (2006.01)

Patent

CA 1167844

ABSTRACT OF THE DISCLOSURE N-[4-[[(2,4-diamino-6-pteridinyl)-methyl] methylamino]benzoyl]glutamic acid (methotrexate) is prepared by a process of alkylating diethyl N-[4-(methylamino)-benzoyl] glutamate with 2,4-diamino- 6-chloromethylpteridine hydrochloride, in the presence of potassium iodide and hydrolyzing the resultant glutamate to methotrexate. The product is of high quality, useful in the treatment of acute leukemia.

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