泮托拉唑是一种抑制胃酸分泌的质子泵抑制剂。临床研究表明,与消旋体及其对映体相比,S-泮托拉唑抑酸效果好,生物利用度高,毒副作用低。目前报道的制备S-泮托拉唑的方法主要是手性拆分和不对称氧化。本文简要概述了S-泮托拉唑的制备研究状况。 Pantoprazole is one of the blockbuster gastric proton pump inhibitors (PPIs). The clinical study showed that S-pantoprazole provides better acid control, higher bio-availability and lower side effects compared to the racemic pantoprazole and R-panto-prazole. It is reported that the optical pure S-pantoprazole could be prepared by chiral resolution and catalytic asymmetric oxidation. This review briefly described the deve-lopment of the preparation method for the optically pure S- pantoprazole.
2008年,Emcure House [20] 报道了一种用手性氮氧丙烷作为氧化剂,在合适的溶剂和碱的条件下,选择性的氧化硫醚制备手性亚砜的方法。该方法指出,针对具有不同官能团的前手性硫醚需用不同溶剂条件,需使用特定的碱以及特定的氧化剂。在异丙醇中,用特定碱1,8-二氮双环[5.4.0]-7-十一烯(DBU),氧化剂为((R)-(-)樟脑磺酰基)氮氧环丙烷,氧化泮托拉唑硫醚,经过一定的纯化后处理,可以得到98.62%的对映体过量的S-泮托拉唑(Scheme 9)。
王 婷,曾银凤,彭丽君,王红丹,朱 槿,黄晴菲,王启卫. S-泮托拉唑的研究进展Recent Progress in Preparation of S-Pantoprazole[J]. 有机化学研究, 2015, 03(04): 139-146. http://dx.doi.org/10.12677/JOCR.2015.34018
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