MyD88小分子拟似物AS-1全合成的方法改进

摘要

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 1H NMR and MS, The tatol yield was 42% with purity over 98%.