A Scalable Process to the Key Intermediate of Cilazapril, (S)‑1-Benzyloxycarbonylhexahydropyridazine-3-carboxylic Acid, Through a Novel Cascade Course

A novel and efficient manufacturing technology is disclosed in the present work for the preparation of (S)-1-benzyloxycarbonylhexahydropyridazine-3-carboxylic acid, which is a key intermediate of cilazapril. The whole process includes only three steps; the first two steps were conducted in one pot,...

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Veröffentlicht in:Organic process research & development 2013-09, Vol.17 (9), p.1209-1213
Hauptverfasser: Chen, Yu, Lu, Yuwei, Zou, Qing, Chen, Huansheng, Ma, Dawei
Format: Artikel
Sprache:eng
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Zusammenfassung:A novel and efficient manufacturing technology is disclosed in the present work for the preparation of (S)-1-benzyloxycarbonylhexahydropyridazine-3-carboxylic acid, which is a key intermediate of cilazapril. The whole process includes only three steps; the first two steps were conducted in one pot, followed by a novel selective removal of a Cbz group in a cascade course.
ISSN:1083-6160
1520-586X
DOI:10.1021/op400155u