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报道了一条哌啶生物碱(-)-Deoxoprosophylline的不对称合成方法.采用二碘化钐促进的手性叔丁基甲磺亚胺10与取代醛11交叉偶联为关键技术,构筑重要中间体——反式羟甲基化β-氨基醇9的立体化学,该反应的收率为77%,立体选择性为99%.这种高选择性地合成反式羟甲基化β-氨基醇的方法可方便地应用于多种含有2-羟甲基-6-取代-3-羟基哌啶生物碱的不对称合成中.
Reported an asymmetric synthesis of piperidine alkaloid (-) - Deoxoprosophylline using samarium diiodide-promoted chiral tert-butylmethanesulfimide 10 as a key technology for the cross-coupling of substituted aldehyde 11 to construct an important intermediate- The stereochemistry of the trans-methylolated β-aminoalcohol 9 was 77% with a stereoselectivity of 99% .This highly selective synthesis of trans-methylated β-aminoalcohols Can be easily applied to a variety of asymmetric synthesis of 2-hydroxymethyl-6-substituted-3-hydroxypiperidine alkaloids.