Patent ID: 6040468
Filing Date: 2000-03-21
Classification: C07J

Abstract:
A method of preparing a 16.alpha., 17.alpha.-dialkylated steroid of the formula ##STR5## wherein R.sup.1 is H or CHR.sup.4 R.sup.5 ; R.sup.2 is C.sub.1 -C.sub.4 alkyl;R.sup.3 is H, C.sub.1 -C.sub.3 alkyl, C.tbd.CH, CH.dbd.CH.sub.2, or phenyl;X is OSiR.sup.7 R.sup.8 R.sup.9 or OC(.dbd.O)R.sup.6 ;Y is H, F, or Cl; or X and Y taken together are a covalent bonds; or X and Y taken together form an epoxide group; ##STR6## R.sup.4, R.sup.5 and R.sup.6 are independently H or C.sub.1 -C.sub.4 alkyl;R.sup.7, R.sup.8 and R.sup.9 are independently C.sub.1 -C.sub.4 alkyl; andQ is H or CH.sub.3 ;comprising reacting in a solvent an enol silyl ether of the formula ##STR7## with an enol silyl ether cleaving agent and an alkylating agent of the formula R.sup.3 CH.sub.2 ZwhereinR.sup.3 is selected from the group consisting of hydrogen, a primary alkyl group of up to three carbon atoms total, an ethenyl group, an ethynyl group, and a phenyl group; andZ is Cl, Br or I.