A practical synthesis of multitargeted antifolate LY231514

…, TM Wilson, ME Kobierski

文献索引：Barnett, Charles J.; Wilson, Thomas M.; Kobierski, Michael E. Organic Process Research and Development, 1999 , vol. 3, # 3 p. 184 - 188

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被引用次数: 45

摘要

A concise and scalable synthesis of LY231514 (1), a new pyrrolo [2, 3-d] pyrimidine-based antitumor agent, is presented. Reaction of 2-bromo-4-arylbutanal 9 with 2, 4-diamino-6- hydroxypyrimidine (10) regioselectively provided pyrrolo [2, 3-d] pyrimidine 11, representing the core structure of the drug, in good yield. Assimilation of the glutamic acid residue by conventional means completed the synthesis. Development of the optimized synthetic ...