Methotrexate analogues. 25. Chemical and biological studies on the γ-tert-butyl esters of methotrexate and aminopterin

A Rosowsky, JH Freisheim, H Bader…

文献索引：Rosowsky; Freisheim; Bader; Forsch; Susten; Cucchi Journal of Medicinal Chemistry, 1985 , vol. 28, # 5 p. 660 - 667

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被引用次数: 40

摘要

Chemistry. 2, 4-Diamino-6-(hydroxymethyl) pteridine (3) was prepared in 75% yield from 2, 4, 5, 6-tetraaminopyrimidine and 1, 3-dihydroxyacetone in the presence of cysteine and Oz. 20 This process is superior to that of Baugh and Shawzl in that the product is uncontaminated by 2, 4-diamino-6-methylpteridine or the 7-hydroxymethyl and 7-methyl compounds. Bromination of 3 with dibromotriphenylphosphorane in N, N- ...