The process development of a novel aldose reductase inhibitor, FK366. Part 1. Improvement of discovery process and new syntheses of 1-substituted …

S Goto, H Tsuboi, M Kanoda, K Mukai…

文献索引：Goto, Shunsuke; Tsuboi, Hiroyuki; Kanoda, Masami; Mukai, Koji; Kagara, Kooji Organic Process Research and Development, 2003 , vol. 7, # 5 p. 700 - 706

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被引用次数: 17

摘要

This contribution describes part 1 of process development of a novel aldose reductase inhibitor FK366 (1). The original process applied on a laboratory scale was improved from the safety viewpoint to manufacture materials on 500-L scale suitable for toxicological and pharmacological evaluations. A new process, including regioselective alkylation of silylated quinazolinedione, provided a practical and cost-effective synthesis of FK366 in a ...