| 摘要 |
<p>1364362 2,2,17α- Trimethyl steroids ROUSSEL UCLAF 3 Feb 1972 [3 Feb 1971] 5019/72 Heading C2U The invention comprises compounds of formulae wherein R<SP>1</SP> is C 1 -C 4 alkyl; R<SP>2</SP> is Cl, Br, I, OH or C 1 -C 18 carboxylic acyloxy; R<SP>3</SP> is H, alkyl, substituted alkyl, cycloalkyl, heterocyclyl or C 1 -C 18 carboxylic acyl; Z is a "blocking" group (other than one within the scope of R<SP>3</SP>), e.g. trimethylsilyl; and Hal is Cl, Br or I. Compounds I and IV are prepared from the corresponding 4-unsubstituted compounds (in which the 17-hydroxy function is in protected form) by 4-halogenation (e.g. with a sulphuryl halide or N-haloimide) optionally followed by one or more steps selected as appropriate from (i) conversion of 4-Cl or Br into iodo using alkali metal iodide; (ii) acidolysis of the 17-protecting group; (iii) conversion of 4-halo to 4-hydroxy with an alkali metal base; (iv) 4-acylation; (v) 17-esterification or etherification. 2,2,17α-Trimethyl - 17# - (2 - tetrahydropyranyloxy) estra-4,9,11-trien-3-one is prepared from the corresponding 17-ol with dihydropyran. Antiandrogenic compositions for oral, parenteral and rectal administration comprise a compound I and a carrier.</p> |
