一种合成四氢-β-咔啉二酮哌嗪化合物的新方法

A New Synthesis Method of Tetrahydro-β-carboline Diketopiperazine

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%。

An efficient route to synthesize tetrahydro-β-carbotinediketopiperazines starting from L tryptophan methyl ester hydrochloride via three steps process including Pictet-Spengler reaction, Schotten Baumann reaction and intramolecular ester amidation with a total yields of 80% was introduced. The molecular structures were characteride by GC-MS,LC-MS.IR.1H NMR and 13C NMR techniques.