一类含噻唑环非天然氨基酸的合成及其拆分

Syntheses and resolution of a kind of unnatrual amino acid involving thiazolic ring

用乙酰基转移酶拆分3－（今噻唑基）－DL-乙酰丙氨酸可直接得到供合成多肽药物使用的L-型氨基酸．该方法合成路线短，分离效果好（e．e．值在99％以上）.类似地合成并拆分了3－（2－R－4噻唑基）-丙氨酸（R=CH3，Ph），获得同样好的效果．

The DL-3-(4-thiazolyl)-N-acetoalanine is synthesized from diethyl (4-thiazolyl)-methyl acetamidomalonate via basic hydrolysis and decarboxylation, and can be resolved to form the L-amino acid used for synthesizing peptide pharmaceuticals with acylase. In this method, the synthetic route is shorter and the resolution effect is better (e- e. ≥99%). In same ways, the 3- (2-R-4-thiazoly)-alanine (R=CH,, Ph ) is also synthesized and resolved, and the effect is as well as the former. This method is adaptable to such resolution as (2-phenyl-4-thiazoly)-DL-acetoalanine, especially. Because the pl of corresponding aminoacid is in the range of activiting acid-base of acylase which pH is between 7. 3~7. 8. Obviously,superiority of the method performe that L-aminoacid resolved separate continuously out from reaction solution, so that following operating progress is more simpler.