摘要
对硼替佐米合成工艺进行优化:以异戊醛与R-(+)-苯乙胺为起始原料经缩合、加成、催化氢化和成盐得到中间体5;另外以L-苯丙氨酸为原料,经酯化、酰化及水解得中间体9;最后中间体5与中间体9经缩合、水解制得目标产物硼替佐米,总收率38.2%(以异戊醛计)。
Intermediate 5 was synthesized from 3-Methyl butanal and（R）-（＋）-1-Phenylethylamine by condensation,addition,catalytic hydrogenation and salt-forming.Furthermore,intermediate 9 was synthesized from L-phenylalanine by esterification,acylation and hydrolysis.Finally,the target product,bortezomib was synthesized by condensation of intermediate 5 and intermediate 9 and hydrolysis.The overall yield was 38.2%（based on 3-methyl butanal）.
出处
《药学与临床研究》
2014年第2期121-123,共3页
Pharmaceutical and Clinical Research
