Patent ID: 6794503
Filing Date: 2004-09-21
Classification: C07J

Abstract:
Process for the preparation of 6&agr;-fluorosteroids of formula (I) wherein R is a substituent at the &agr;- or &bgr;-position, chosen from H, OH and an alkyl group with from 1 to 4 carbon atoms, Ac is an acetyl group, and wherein a double bond may be present between positions 1 and 2, said process comprising:reaction of the compound of formula (II) with isopropenyl acetate to obtain the compound of formula (III) wherein R is as defined above; reaction of the compound of formula (III) with an electrophilic fluorinating agent to give the compound of formula (I) wherein R is as defined above, and wherein said electrophilic fluorinating agent is selected from the group consisting of N-fluoro N-chloromethyl triethylenediamine bis-tetrafluoroborate, 1-fluoro-4-hydroxy-1,4-diazabicyclo[2.2.2]octane-bis-tetrafluoroborate, and 1-fluoro-benzenesulfonamide.