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目的寻找N-(9-芴甲氧羰基)-N’-(2-乙酰氨基-2-脱氧-3,4,6-三-O-乙酰基-β-D-吡喃葡萄糖基)-L-天冬酰胺(Fmoc-Asn(Ac3GlcNAc)-OH)选择性脱除O-乙酰保护基的方法。方法采用HPLC法对反应进行监测,考察超声条件下Fmoc-Asn(Ac3GlcNAc)-OH脱除保护基的反应,寻找选择性脱除O-乙酰保护基的方法。结果在碱试剂的条件下脱除O-乙酰保护基的反应有很多杂质产生。但在超声条件下,反应无杂质生成且产率较高。结论超声条件下,Fmoc-Asn(Ac3GlcNAc)-OH和Fmoc-Ser(Ac3GlcNAc)-OH选择性脱除O-乙酰基,收率高于90%。
Aim To find out the potential of N- (9-fluorenylmethoxycarbonyl) -N ’- (2-acetylamino-2-deoxy-3,4,6-tri-O-acetyl-β-D-glucopyranosyl) -L - Asparagine (Fmoc-Asn (Ac3GlcNAc) -OH) for the selective removal of O-acetyl protecting groups. Methods The reaction was monitored by HPLC. The reaction of removing the protecting group with Fmoc-Asn (Ac3GlcNAc) -OH under ultrasonic condition was investigated in order to find the method of selective removal of O-acetyl protecting group. As a result, many impurities are generated in the reaction for removing the O-acetyl protecting group under the conditions of an alkaline reagent. However, under ultrasonic conditions, the reaction is free of impurities and the yield is high. CONCLUSIONS O-acetyl groups were selectively removed by Fmoc-Asn (Ac3GlcNAc) -OH and Fmoc-Ser (Ac3GlcNAc) -OH under ultrasonic conditions with a yield higher than 90%.