末端碘代的保护氨基酸的合成

Facile Synthesis of Terminal Iodine Substituted Protected Amino Acid

采用一锅法,以(S)-1-叔丁基-2-叔丁氧羰基氨基-天冬氨酸为原料,经还原反应和碘代反应合成了标题化合物,总收率55%;以(S)-2-叔丁氧羰基氨基-丝氨酸为原料,经酯化反应和碘代反应合成了标题化合物,总收率70%。其结构经1HNMR和13CNMR表征。

（ S ）-tert-Butyl 2-tert-butoxyearbonylamino-4-io- dobutyrate was synthesized from （S）-1-tert-butyl-2-（ tert-butyloxyearbonylamino）-aspartie acid by a two-step reaction ,re- duction and iodination, in total yield of 55%. （R）-Methyl 2-tert-butyloxyearbonylamino-3-iodopropionate was synthesized from （S）-2-（ tert-butyloxycarbonylamino）-serine by a two-step reaction, esterifieation and iodination,in total yield of 70%. The structures were confirmed by ^1HNMR and ^13CNMR.