Synthesis of 2,4-diamino-6-hydroxymethylpteridine

Details Synthesis of 2,4-diamino-6-hydroxymethylpteridine Synthesis of 2,4-diamino-6-hydroxymethylpteridine

1980-03-25

1981-12-15

Coughlan, Jr., Paul M.

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

Organic compounds

Plural nitrogens bonded directly to the pteridine ring system

C07D47508

Patent

active

043060641

ABSTRACT:
In a method of preparing methotrexate from a coupling of 2,4-bis(triphenylphosphazino)-6-bromomethylpteridine hydrobromide with ethyl N-(p-methylamino)-benzoyl-L-glutamate to produce the phosphazino derivative of methotrexate ester and subsequently hydrolyzing the phosphazino and ester groups to produce the free methotrexate, the pteridine synthesis step wherein molecular oxygen is substituted for reaction air and the pH throughout the pteridine synthesis is regulated to between 2.5 and 5.4, the preferred pH being about 3.0 and producing from tetraaminopyrimidine and dihydroxyacetone the isomer 2,4-diamino-6-hydroxymethylpteridine over 2,4-diamino-7-hydroxymethylpteridine in a ratio of about 20:1. Exemplary of other situations involving pteridine where the molecular oxygen may be substituted for reaction air are: in the production of folic acid, tetrahydrofolic acid, etc.

REFERENCES:
patent: 3989703 (1976-11-01), Niculescu-Duvaz et al.
patent: 4080325 (1978-03-01), Ellard
Boyle et al., Chem. Ber., 113, 1514-1523, No. 4, Apr. 1980.

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