A Concise And Scalable Formal Synthesis Of The Enantiopure Side-Chain Diester Of Homoharringtonine

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.