Department of Chemistry, University of Oxford , Chemistry Research Laboratory, Mansfield Road, Oxford, OX1 3TA, U.K.
Org Lett. 2013 Nov 1;15(21):5492-5. doi: 10.1021/ol402638n. Epub 2013 Oct 16.
The utility of the tethered aminohydroxylation (TA) has been demonstrated by synthesis of the complex β-amino acid residue of microsclerodermins A and B. The TA provided a regio- and stereoselective functionalization of a complex homoallylic alcohol. The route includes late-stage introduction of the aliphatic side chain via a cuprate addition and cross metathesis, a tactic designed to render the synthesis applicable to other microsclerodermins.
通过合成微缩菌素 A 和 B 的复杂 β-氨基酸残基,证明了束缚氨基羟化(TA)的实用性。TA 提供了一种区域和立体选择性的复杂偕丙醇官能化。该路线包括通过铜叶立德加成和交叉复分解反应在后期引入脂肪侧链,这一策略旨在使合成适用于其他微缩菌素。