Matijin-Su （1） is a phenylalanine dipeptide compound with anti-hepatitis B virus （HBV） activity. Previous re- ports suggest that the synthesis of glycosylated Matijin-Su derivatives needs at least 10 steps. To sim...Matijin-Su （1） is a phenylalanine dipeptide compound with anti-hepatitis B virus （HBV） activity. Previous re- ports suggest that the synthesis of glycosylated Matijin-Su derivatives needs at least 10 steps. To simplify the syn- thetic procedure, we have developed a shorter and more efficient method for the preparation via ultrasound irradiation. Two galactopyranosylated （2） and two glucopyranosylated （3） derivatives were synthesized in 6 or 7 steps. The overall yields for the total synthesis of galactopyranosylated derivatives were markedly increased to 39% （2a） or 22% （2b）. And the yields for glucopyranosylated derivatives also reached 29% （3a） or 16% （3b）.展开更多
文摘Matijin-Su （1） is a phenylalanine dipeptide compound with anti-hepatitis B virus （HBV） activity. Previous re- ports suggest that the synthesis of glycosylated Matijin-Su derivatives needs at least 10 steps. To simplify the syn- thetic procedure, we have developed a shorter and more efficient method for the preparation via ultrasound irradiation. Two galactopyranosylated （2） and two glucopyranosylated （3） derivatives were synthesized in 6 or 7 steps. The overall yields for the total synthesis of galactopyranosylated derivatives were markedly increased to 39% （2a） or 22% （2b）. And the yields for glucopyranosylated derivatives also reached 29% （3a） or 16% （3b）.
