STEREOSELECTIVE METHOD OF PRODUCING 6α-FLUOROPREGNANES AND INTERMEDIARIES

阅读量:

26

公开/公告号:

WO2003010181 A1

公开/公告日期:

Feb 6, 2003

发明人:

GJV MurilloGLO SilvaJJ Martín

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被引量:

2

摘要:

The invention relates to 6α-fluoropregnanes (I), wherein: the line of points between positions 1 and 2 represents a single or double bond; R1 denotes OH, OCOR2, X, SO3R3 or a (R7)(R8)(R9)SiO-group, wherein X is halogen, R2 and R3 denote C1-6 alkyl or phenyl optionally substituted by C1-4 alkyl, and R7, R8 and R9, which may be the same or different, denote C1-6 alkyl or phenyl optionally substituted by C1-4 alkyl. Said 6α-fluoropregnanes can be obtained by means of a method with high stereoselectivity that consists in reacting a 3-(trisubstituted)silyloxy-pregna-3,5-diene(IV) with a fluorination agent selected from N-fluorosulphonimides and N-fluorosulphonamides. The 6α-fluoropregnanes (I) are intermediaries for the synthesis of steroids that can be used as antiinflammatory and antiasthmatic agents.

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2003
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