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[Synthesis of [1,6-bis(L-alpha, beta-diaminopropionic acid) oxytocin].

作者信息

Wu Kaiqun, Weng Lingling, Zheng Hu

机构信息

West China School of Pharmacy, Sichuan University, Chengdu 610041, China.

出版信息

Sheng Wu Yi Xue Gong Cheng Xue Za Zhi. 2006 Aug;23(4):818-21.

Abstract

A novel derivative of oxytocin containing nonprotein amino acid L-alpha, beta-diaminopropionic acid (L-Dap) was synthesized by 7+2 fragment combination in solution. N beta of all the amino acid necessary was protected by carbobenzoxy (Z) and N beta of L-Dap was protected by tert. -butoxycarbonyl (Boc) . The important intermediate, heptapeptide, was synthesized by the stepwise elongation method using carbobenzoxy amino acid p-nitrophenyl esters in solution. Azide synthesis was used to get the nonapeptide. Z group was removed by treatment with 5% Pd/C and Boc with CF3COOH. Eight new compounds incorporating L-Dap were obtained and confirmed by the amino acid analysis and mass spectral detection.

摘要

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