一种作为抗转移剂的选择性明胶酶抑制剂的简便合成方法。
A convenient synthesis of a selective gelatinase inhibitor as an antimetastatic agent.
作者信息
Lim In Taek, Brown Stephen, Mobashery Shahriar
机构信息
Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, Indiana 46556, USA.
出版信息
J Org Chem. 2004 May 14;69(10):3572-3. doi: 10.1021/jo049857v.
Compound 1, 2-(4-phenoxyphenylsulfonylmethyl)thiirane, is a potent and selective inhibitor for human gelatinases (J. Am. Chem. Soc. 2000, 122, 6799-6800), enzymes implicated in a number of diseases, including cancer. This compound is showing excellent promise in animal trials in a number of disease models. Large quantities of this compound were necessary for these studies. A convenient four-step synthetic route for compound 1 is described herein. The synthesis is amenable to scale-up to tens of grams and gives an overall yield of 57% for this important compound.
化合物1，即2-(4-苯氧基苯基磺酰甲基)硫杂环丙烷，是一种对人明胶酶具有强效且选择性的抑制剂（《美国化学会志》，2000年，第122卷，6799 - 6800页），明胶酶与包括癌症在内的多种疾病有关。该化合物在多个疾病模型的动物试验中显示出极佳的前景。这些研究需要大量的该化合物。本文描述了一种合成化合物1的简便的四步合成路线。该合成方法适合放大至几十克规模，对于这种重要化合物的总产率为57%。
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