Abstract: 6&agr;-fluorpregnanes (I), where the dotted line between positions 1 and 2 represents a single or double bond; R1 is OH, OCOR2, X, SO3R3, or an (R7)(R8)(R9)SiO— group, where X is halogen, R2 and R3 are C1-6 alkyl or phenyl optionally substituted by C1-4 alkyl, and R7, R8 and R9, equal or different, are C1-6 alkyl or phenyl optionally substituted by C1-4 alkyl, can be obtained by means of a high stereoselectivity process comprising reacting a 3-(trisubstituted)silyloxy-pregna-3,5-diene (IV) with a fluorinating agent selected among N-fluorosulfonimides and N-fluorosulfonamides. The 6&agr;-fluorpregnanes (I) are intermediates for the synthesis of steroids useful as anti-inflammatory and anti-asthmatic agents.
Type:
Application
Filed:
January 26, 2004
Publication date:
September 16, 2004
Applicant:
Ragactives, S.L.
Inventors:
Jose Vicente Murillo Garrido, Luis Octavio Silva Guisasola, Jorge Martin Juarez