The enantiopure side-chain diester of homoharringtonine (HHT) has been prepared in 38% overall yield, from cheap L-aspartic acid by a linear sequence of 10 chemical operations (mean yield per step: 91%). The experimental operation in each step is convenient, economic and prone to scale up. About 7–10 g of the side-chain diester of HHT is easily prepared within one week from 5 g of L-aspartic acid.
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