Ke Xianbing, Hu Hao, Zhang Keda, Xu Wenjin, Zhu Qifeng, Wu Lamei, Hu Xianming
State Key Laboratory of Virology, College of Pharmacy, Wuhan University, Wuhan, P. R. China.
Chem Commun (Camb). 2009 Mar 7(9):1037-9. doi: 10.1039/b817910g. Epub 2009 Jan 27.
4alpha-Aminosteroids were synthesized by the substitution of a 2alpha-bromo ketone using K(2)CO(3) as an activator; 4beta-aminosteroids were synthesized in excellent yields by a highly regioselective and trans-stereospecific ring opening of a steroidal 3,4alpha-epoxide using ZnCl(2)-H(2)O as a catalyst.
通过使用碳酸钾(K₂CO₃)作为活化剂,用2α-溴代酮进行取代反应合成了4α-氨基甾体;通过使用氯化锌(ZnCl₂)-水作为催化剂,对甾体3,4α-环氧化物进行高度区域选择性和反式立体专一性的开环反应,以优异的产率合成了4β-氨基甾体。