Tsuda M, Muraoka Y, Nagai M, Takeuchi T, Aoyagi T
Institute of Microbial Chemistry, M. C. R. F., Tokyo, Japan.
J Antibiot (Tokyo). 1996 Mar;49(3):287-91. doi: 10.7164/antibiotics.49.287.
Total synthesis of poststatin was achieved by both liquid phase and solid phase methods. In both methods, the (2R,3S)-3-amino-2-hydroxyvaleric acid moiety was incorporated into protected pentapeptides, and was oxidized to (S)-3-amino-2-oxovaleric acid (postine). Deprotection of the oxidized pentapeptides gave a specimen identical with natural poststatin in physico-chemical properties and prolyl endopeptidase inhibitory activity.
后他汀的全合成通过液相和固相方法均得以实现。在这两种方法中，(2R,3S)-3-氨基-2-羟基戊酸部分被引入到受保护的五肽中，并被氧化为(S)-3-氨基-2-氧代戊酸（后氨酸）。氧化后的五肽脱保护后得到的样品在物理化学性质和脯氨酰内肽酶抑制活性方面与天然后他汀相同。
