Scott Jack D, Williams Robert M
Department of Chemistry, Colorado State University, Fort Collins, CO 80523, USA.
J Am Chem Soc. 2002 Mar 27;124(12):2951-6. doi: 10.1021/ja0174027.
The first total synthesis of the potent antitumor antibiotic (-)-tetrazomine has been accomplished. A new method for the formation of the allylic amine precursor to an azomethine ylide has been developed and exploited in an efficient [1,3]-dipolar cycloaddition to afford the key tetracyclic intermediate used in the synthesis of (-)-tetrazomine. Several analogues of tetrazomine have been synthesized and tested for antimicrobial and biochemical activity.
强效抗肿瘤抗生素（-）-四唑米星的首次全合成已经完成。已开发出一种形成甲亚胺叶立德烯丙基胺前体的新方法，并将其用于高效的[1,3]-偶极环加成反应中，以提供用于合成（-）-四唑米星的关键四环中间体。已经合成了几种四唑米星类似物，并对其抗菌和生化活性进行了测试。
