【摘要】 卡格列净(canagliflozin)是一种由强生开发的SGLT2抑制剂,可以用于治疗成年患者的II型糖尿病,是糖尿病治疗市场上的又一重磅药物。本文的目的是再提供一种制备卡格列净关键中间体的方法,即使用催化量的镍络合物为催化剂(1.5 mol%),通过Kumada偶联高效地合成卡格列净关键中间体:2-(4-氟苯基)噻吩,该方法能够有效解决卡格列净关键中间体2-(4-氟苯基)噻吩制备及成本问题,而且可以在相对比较温和的条件下合成2-(4-氟苯基)噻吩,适合工业化大规模生产。更多还原

【Abstract】 Canagliflozin is one kind of SGLT2 inhibitors which is mainly used for the treatment of adult patients with type II diabetes prepared by Johnson & Johnson. It is a blockbuster drug for the market of the treatment of diabetes. A method was used to provide for preparing key intermediates of Canagliflozin: 2-( 4- fluorophenyl) thiophene,using a catalytic amount of nickel complex as catalyst( 1. 5mol%),efficiently synthesizing the key intermediates of Canagliflozin through Kumada coupling method,mainly solving the sources and cost issues of key intermediates of Canagliflozin.Otherwise,this method could be prepared 2-( 4- fluorophenyl) thiophene in the mild environment,which was easily for industrialized mass production.更多还原