报道一种二肽手性胺类化合物的简便合成方法。采用缩合剂苯并三氮唑-N,N,N',N'-四甲基脲六氟磷酸盐(HBTU)缩合生成酰胺的方法,以N,N-二异丙基乙胺(DIEA)为催化剂,手性氨基酸Boc-L-丙氨酸、N-Boc-L-苯甘氨酸、Boc-L-苯丙氨酸和取代苄胺为原料,按照由C端向N端依次接肽的合成策略,采用液相法合成6个二肽手性胺,收率达到45.75%-77.82%,经IR,^1H NMR,^13C NMR,^19F NMR及元素分析对所合成的化合物进行了结构确认和表征。
A simple and effective way to prepare dipeptide chiral amine compounds was put forward. The title compounds were prepared via the condensation acylation reaction of chiral amino acids( Boc- L- alanine,N- Boc- L-phenylglycine and Boc- L- phenylalanine) and substituted benzyl amine with o- Benzotriazol- 1- yl- N,N,N',N'-tetramethyluronium hexafluorophosphate( HBTU) as condensing agent and N,N- Diisopropylethylamine( DIEA) as catalyst. In accordance with the synthetic strategy by C- side to the N- side in turn connected to the peptide,They were synthesized by liquid method with yield of 45. 75% - 77. 82%. Their structures were clearly established by elemental analysis,IR,1H NMR,13 C NMR and19 F NMR spectra.