中文摘要：

蛋白酪氨酸磷酸酶1B（PTP1B）是治疗2型糖尿病和肥胖症的新靶点.根据已报道的磷酸酪氨酸拟似物类PTP1B抑制剂A,通过计算机药物辅助设计,经Negishi偶联、亚磺酰亚胺烯醇式不对称加成及Dess-Martin氧化等11步反应成功合成了一个结构新颖的PTP1B抑制剂1,其对体外人重组PTP1B的半抑制浓度为54.17μmol？L-1.

英文摘要：

Protein tyrosine phosphatase 1B（PTP1B） has been known to be a promising target for the treatment of type 2 diabetes and obesity. According to the reported phosphotyrosyl mimetics A, a new PTP1 B inhibitor 1 was designed via computer-assisted drug design. The target compound 1 was achieved through eleven steps with Negishi cross-coupling reaction, diastereoselective sulfinylimine enolate addition reaction and the Dess-Martin oxidation as key steps. The compound 1 inhibited PTP1 B competitively with an IC50 value of 54.17 μmol·L-1 in vitro.