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从一个易得的硅烷出发,经八步可制得抗癌霉素. 抗癌霉素(1)是从放射线菌分离得到的抗菌素,它具有相当的抗肿瘤活性,并已作临床应用.1被分离后不久就被人工合成出来,但所用方法没有区域控制,并不理想.随着近代合成手段的发展,它又成为热门的合成目标,最近几年间就有七个新合成的报道.从结构上讲,1是环戊酮类抗菌素中最简单的成员.本文报道合成1的一条新路线,它的特点是利用烯丙硅基的区域控制性质,而其中一个中间体还可以利用来合成这类化合物的其他成员. 我们从易得的硅烷2出发,仅经一步碳酸氢钠催化甲醇解,就得到具有与1相同碳骨架
From a readily available silane, the anticancer drug is obtained in eight steps.Antibiocin (1) is an antibiotic isolated from an actinomycete that has considerable antitumor activity and has been clinically used.1 It was synthesized shortly after being separated, but the method used was not ideal for regional control. With the development of modern synthetic methods, it has become a popular synthesis target, and there are seven newly synthesized reports in recent years. Structurally, 1 is the simplest member of cyclopentanone antibiotics. A new route to the synthesis of 1 is reported in this paper. It is characterized by the use of the regio-control properties of allyl silicon and one of the intermediates can be used to synthesize Other members of this class of compounds We proceed from readily available silane 2 and catalyze the methanolysis with only one step of sodium bicarbonate to give a compound having the same carbon skeleton as 1