泊沙康唑关键中间体合成的新方法

New Method for Synthesis of Key Intermediate of Posacaonzaole

N'-[(2S,3S)-2-苄氧基]戊基-3-甲酰肼作为泊沙康唑的关键中间体,在化工医药中有着重要的研究价值和市场前景。以L-乳酸甲酯为起始原料,经过取代、还原、缩合、取代而得到,总收率64.50%,化合物结构经1H NMR和MS确证。该工艺路线具有操作简单、反应条件温和、危险性小和有利于工业化生产等优点。

As the key intermediate of posacaonzaole, N′-[(2S,3S)-2-(benzyloxy)pentan-3-yl]formothydrazide has important research value and market prospect, the target product with an overall yield of 64.50% was obtained via substitution reaction, reduction, condensation reaction and substitution reaction from L-methyl lactate. The chemical structure of target product was identified by 1HNMR and MS. This new synthetic route has the advantages of simplicity in operation, reaction under mild and safe conditions,low risk in synthesis and beneficial to industrial production.