Pyrido [2, 3-d] pyrimidines. The synthesis of the 5-deaza analogs of aminopterin, methotrexate, folic acid, and N10-methylfolic acid

…, RD Elliott, JA Montgomery

文献索引：Temple, Carroll; Elliott, Robert D.; Montgomery, John A. Journal of Organic Chemistry, 1982 , vol. 47, # 5 p. 761 - 764

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被引用次数: 31

摘要

N-[4-[[(2-amin~ 4 (3H)-oxopyrido [2, 3-d] pyrimidin-6-yl) methyl] amino] benzoyl]-~-glutamate (13), which was converted to the corresponding glutamic acid 14 (5-deazafolic acid). The preferred route for the preparation of 14 involved the hydrolysis of 10 with base at reflux, which resulted in replacement of the 4-amino group and saponification of the eater groups. Methylation of 14 with formaldehyde and dum cyanoborohydride gave 5-deaza-10- ...