Abstract: Described herein is a process for the preparation of 6&agr;-fluorosteroids of formula (I), in which R is chosen from H, OH and an alkyl group with from 1 to 4 carbon atoms and R′ is a carboxyalkyl group with from 1 to 4 carbon atoms in the alkyl chain, comprising the selective fluorination at the 6&agr;-position
by treatment of the compound of formula (III), wherein R and R′ are as defined above, with an electrophilic fluorinating agent.
Abstract: 16.alpha., 17.alpha.-dialkylated steroids are prepared by reacting a 16.alpha.-alkyl-17(20)-enyl-20-silyl ether with an alkylating agent and an enol silyl ether cleaving agent in a suitable solvent.
Abstract: A compound of the formula ##STR1## wherein R is hydrogen or an ester remainder, X is hydrogen or fluorine and Y combined with the doted lines represents ##STR2## or X is hydrogen and and Y combined with the dotted lines is ##STR3## and R.sub.1 is the remainder of an enol ether or ester.
Type:
Grant
Filed:
May 15, 1995
Date of Patent:
September 17, 1996
Assignee:
Roussel Uclaf
Inventors:
Jean-Yves Godard, Philippe Mackiewicz, Denis Prat, Christian Richard
Abstract: A compound of the formula ##STR1## wherein R is selected from the group consisting of alkyl, alkenyl and alkynyl of up to 4 carbon atoms, Y is .dbd.O or ##STR2## R.sub.1 is hydrogen or acyl, n is 0, 1 or 2, D is .dbd.O or ##STR3## and A and B form a second carbon-carbon or an .alpha.-epoxy useful for aromatase inhibition and a process and intermediates for their preparation.
Abstract: C.sub.16 -unsaturated corticoids are readily transformed to the corresponding 16.alpha.-methyl-17.alpha.-hydroxy corticoids by use of a .DELTA..sup.17 (.sup.20)-20-silyl ether.
Abstract: Novel 17-(formamidosulfonylmethylene)-steroids of the formula ##STR1## useful as intermediates for the novel 17-(isocyanosulfonylmethylene)-steroids of the formula ##STR2## which are useful intermediates for 21-hydroxy-20-keto-.DELTA..sup.16 -steroids and 20-keto-.DELTA..sup.16 -steroids.
Type:
Grant
Filed:
April 27, 1984
Date of Patent:
March 3, 1987
Assignee:
Gist-Brocades N.V.
Inventors:
Albert M. van Leusen, Adriaan M. van Leusen
Abstract: The process of the present invention transforms 16.alpha.- or 16.beta.-methyl-17-keto steroids (I) to the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-16.alpha.- or 16.beta.-methyl steroids (II) without epimerization and loss of stereochemistry of the 16.alpha.- or 16.beta.-methyl group.
Abstract: The process of the present invention transforms 16-methylene-17-keto steroids (I) to the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-16-methylene steroids (II).