【摘要】 研究了地氯雷他定和5-甲基烟酸在DCC和HOBT作用下合成卢帕他定酰胺。然后卢帕他定酰胺经硼氢化钠在三氟乙酸作用下还原,再经成盐得到富马酸卢帕他定。该方法采用避免了昂贵和剧毒试剂的试用,使生产成本大大降低,并提高了产品质量。更多还原

【Abstract】 The synthesis of rupatadine amide was studied with desloratadine and 5-Methylnicotinic acid with DCC and HOBT,and the synthesis of rupatadine by the reduction of rupatadine amide with sodium tetrahydroborate at the presence of trifluoroaceticacid and rupatadine fumarate were also studied.The advantage of the process is that the yield and purity of the product are improved without expensive and hypertoxic chemicals.更多还原