Journal
ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 7, Issue 5, Pages 700-706Publisher
AMER CHEMICAL SOC
DOI: 10.1021/op0340661
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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 dramatically increased yield.
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