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本文通过(+)-樟脑缩苄胺(1)与不同醛、酮韵不对称加成,经转氨合成了1,2取代-2-氨基乙醇(2)。反应的非对映选择性经NMR测定为16—70％de.;苏式、赤式异构体的含量比由HPLC法测定,其值接近1。由于立体位阻的原因加成反应发生在锂化物3的Re面。
In this paper, 1, 2-substituted 2-aminoethanol (2) was synthesized via transamination of asymmetric addition of (+) - camphylbenzylamine (1) with different aldehydes and ketones. The diastereoselectivity of the reaction was 16-70% de by NMR; the content ratio of the threo-erythrocytes and the erythro isomers was determined by HPLC method to be nearly 1. The addition reaction occurs on the Re face of the lithium compound 3 due to the steric hindrance.