通过多功能催化对映选择性烯醇化物羟醛加成反应全合成大环内酯A
Total Synthesis of Macrolactin A with Versatile Catalytic, Enantioselective Dienolate Aldol Addition Reactions.
作者信息
Kim Yuntae, Singer Robert A, Carreira Erick M
机构信息
California Institute of Technology, Division of Chemistry and Chemical Engineering, 164-30, 1201 East CA Boulevard, Pasedena, CA 91125 (USA), Fax: (+1) 626-564-9297.
出版信息
Angew Chem Int Ed Engl. 1998 May 18;37(9):1261-1263. doi: 10.1002/(SICI)1521-3773(19980518)37:9<1261::AID-ANIE1261>3.0.CO;2-2.
A highly convergent total synthesis of macrolactin A (1) utilizes modern asymmetric catalytic C-C coupling methods. The longest linear sequence in the route is 16 steps with an average yield of 86% per step. This total synthesis is valuable, because 1, which has been shown to possess activity against HIV, is not readily accessible from its natural source, a taxonomically unclassified deep-sea bacterium.
对大环内酯A（1）进行的高度汇聚式全合成采用了现代不对称催化碳-碳偶联方法。该路线中最长的线性序列为16步，每步平均产率为86%。这种全合成具有重要价值，因为已证明具有抗HIV活性的1不易从其天然来源（一种分类学上未分类的深海细菌）获得。
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