申请人:SCHERING AKTIENGESELLSCHAFT
公开号:EP0849274A1
公开(公告)日:1998-06-24
Bissteroidal compounds of general formula I
in which
R1stands for hydrogen, alkyl, acyl, fluorine, and X1R5,
where X1 stands for oxygen and sulfur and
R5 can either be hydrogen, alkyl, aryl,
R2stands for hydrogen and alkyl; the stereochemistry of C-13, C-14 and C-17 may either be α or β,
Xstands for oxygen, trifluormethylsulfonyloxy, or (R6)2P,
where R6 can be aryl, alkyl and cycloalkyl,
R3stands for hydrogen, alkyl, aryl, trialkylsilyl, fluorine and X2R6,
where X2 stands for oxygen and sulfur and
R6 stands for hydrogen, trifluormethylsulfonyl, alkyl or aryl.
R4can either be a substituent in the 6 or 7 position of the steroid with the meaning of hydrogen, alkyl, aryl, fluorine, and X3R7,
where X3 stands for oxygen, sulfur or trialkylsilyl and R7 stands for hydrogen, trifluormethylsulfonyl, alkyl or aryl,
and the B-ring of the steroid contains none or two double bonds.
Enantio- and Diastereomeric derivatives of compounds of general formula I, metal complexes thereof and their use in enantioselective reactions.
一般式I的双甾类化合物,其中R1代表氢、烷基、酰基、
氟和X1R5,其中X1代表氧和
硫,R5可以是氢、烷基、芳基;R2代表氢和烷基;C-13、C-14和C-17的立体
化学可以是α或β;X代表氧、三
氟甲磺酰氧或(R6)2P,其中R6可以是芳基、烷基和环烷基;R3代表氢、烷基、芳基、三烷基
硅基、
氟和X2R6,其中X2代表氧和
硫,R6代表氢、三
氟甲磺酰基、烷基或芳基;R4可以是类
固醇的6或7位取代基,代表氢、烷基、芳基、
氟和X3R7,其中X3代表氧、
硫或三烷基
硅基,R7代表氢、三
氟甲磺酰基、烷基或芳基;类
固醇的B环中含有零或两个双键。一般式I的对映体和非对映异构体衍
生物,其
金属配合物及其在对映选择性反应中的应用。