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以L-色氨酸甲酯盐酸盐为起始原料,与醛发生Pictet-Spengler反应得到四氢-β-咔啉,然后通过结晶诱导不对称转化(CIAT)过程得到单一对映体,再经Schotten-Baumann反应,酰胺形成及脱保护过程即得目标产物,结构经GC-MS,LC-MS,IR,1 H NMR,13C NMR确证,总收率80%。
L-Tryptophan methyl ester hydrochloride as the starting material, Pictet-Spengler reaction with aldehydes to obtain tetrahydro-β-carboline, and then through the crystallization induced asymmetric transformation (CIAT) process to obtain a single enantiomer, and then The Schotten-Baumann reaction, amide formation and deprotection process gave the desired product. The structure was confirmed by GC-MS, LC-MS, IR, 1 H NMR and 13C NMR. The overall yield was 80%.