MyD88小分子拟似物AS-1全合成的方法改进

Process Improvement on the Total Synthesis of a Low Molecular Weight MyD88 Mimic AS-1

以N-Boc-L-缬氨酸为起始原料,经四步反应(最后一步用苯丙酰氯为苯丙酰化试剂)高产率地合成了蛋白质MyD88的小分子拟似物——N-(N'-3-苯丙酰-L-缬氨酰)四氢吡咯(AS-1),其结构经1H NMR和MS确证,总收率42%,纯度高于98%。

A low molecular weight MyD88 mimic, N-（N＇-3-phenylpropionyl-L-valyl）pyrrolidine（ AS- 1 ）, was synthesized from N-Boc-L-valine by a four-step reaction route using 3-phenylpropionyl chloride as the propylenelation agent in the final step. The structures were confirmed by I H NMR and MS. The tatol yield was 42% with purity over 98%.