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环二肽在自然界及天然产物中广泛存在,由于其结构特殊,使得环二肽成为药物化学中一个重要的药效团,许多环二肽具有强的生理活性.以N-叔丁氧羰基-L-天冬氨酸-β-苄酯和L-脯氨酸甲酯盐酸盐为原料,经DCC缩合得直链二肽,再经HCl/Et2O脱Boc保护,弱碱性条件下成环,最后Pd/C催化氢解得环(L-天冬氨-L-脯)二肽.结构经ESI-MS、IR、1HNMR、13CNMR等表征.
Cyclic dipeptide is widely existed in nature and natural products, and because of its special structure, cyclic dipeptide has become an important pharmacophore in pharmaceutical chemistry, and many cyclic dipeptides have strong physiological activity.With N-tert-butoxycarbonyl- L-aspartic acid -β-benzyl ester and L-proline methyl ester hydrochloride as raw materials, the DCC condensation of the linear dipeptide, and then deprotected by Boc HCl / Et2O, under mild alkaline conditions , And finally the dipeptide (L-aspartame-L-propeptide) was obtained by catalytic hydrogenolysis of Pd / C.The structure was characterized by ESI-MS, IR, 1HNMR and 13CNMR.