Short Step Synthesis of Antitumor Natural Products Having Indolo [2, 3α] carbazole as a Common Skeleton

1. 吲哚[2,3-α]咔唑的研究我们用工业上可用的化学物质靛蓝为原料，用我们自己的新反应制备了2,2'-联吲哚基、3-乙酰-2,2'-联吲哚基、1-乙酰-2,3-二氢-2,2'-联吲哚基等重要组成部分。以这些化合物为起始原料，开发了4条短步合成抗生素6-氰基-5-甲氧基吲哚[2,3-α]咔唑的全合成路线。还制备了n -糖基2,2'-双吲哚，并发现它是制备n -糖基lindolo [2,3-α]咔唑的优良底物。上述方法广泛适用于各种吲哚[2,3-α]咔唑类化合物的合成。通过1-甲氧基吲哚-2-基锂的氧化偶联制备了1-羟基吲哚- 2,2'-联吲哚，并转化为吲哚[2,3-α]咔唑，这是第五种合成途径。1-羟基吲哚是吲哚化学中的新化合物，是由1-羟基吲哚合成的。人们对1-羟基吲哚的化学性质进行了广泛的研究，并发现了许多新的发现，这些发现是迄今为止已知的吲哚化学所没有预料到的。吲哚化学的一个新领域正在打开。

1. Study toward Indolo [2,3-α] carbazolesImportant building blocks such as 2,2'-biindolyl, 3-acetoxy-2,2'-biindolyl, 1-acetyl-2,3-dihydro-2,2'-biindolyl were prepared by our own new reactions from industrially available chemical, indigo. Utilizing these compounds as starting materials, four short step total synthetic routes to an antibiotic, 6-cyano-5-methoxyindolo [2,3-α] carbazole, were developed.N-Glycosyl 2,2'-biindolyls were also prepared and found to be excellent substrates for producing N-glycosylindolo [2,3-α] carbazoles.Above methods are widely applicable for the syntheses of various kinds of indolo [2,3-α] carbazoles.2. The Chemistry of 1-Hydroxyindoles2,2'-Biindolyl was also prepared through oxidative coupling of lithium 1-methoxyindol-2-yl and converted to indolo [2,3-α] carbazoles which constituted the fifth synthetic route.1-Methoxyindoles are prepared from 1-hydroxyindoles, which are new compounds in indole chemistry. The chemistry of 1-hydroxyindoles was widely examined and found to be rich in a lot of new findings that were not expected from thusfar known indole chemistry.A frontier in indole chemistry is now open.