- 19-nor steroids having a thiocarbonated chain in position 11beta, their preparation process and the intermediates of this process, and the intermediates of this process, their use as medicaments and compositions
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Compounds of formula (I), wherein R17and R′17are such that: either R17and R′17together form ketone, hydrazono, oxime or methylene, or R17is hydroxyl, hydroxymethyl or acyloxy and R′17is hydrogen, alkyl or optionally substitued alkenyl or alkynyl; R3is hydrogen or alkyl; R16is hydrogen, halogen or alkyl; m is 0, 1 or 2; X, Y and Z are such that: X is methylene, arylene or arylenoxy bonded to the steroid by a carbon atom; Y is a saturated or unsaturated straight or branched aliphatic chain which is optionally interrupted by oxygen; and Z is aryl, arylalkyl or straight or branched alkyl; addition salts thereof, a preparation method therefor, medicinal uses thereof, compositions containing said compounds, and resulting novel intermediates.
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- Polyfluoroaralkylamines: an improved synthesis of 4,5,6,7-tetrafluoroindole
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Tetrafluoroindole (5), a precursor for potential biologically-active compounds, was prepared previously in a four-step synthesis from C6F6.However, catalytic reduction of pentafluorophenylacetonitrile (2) to 2-pentafluorophenylethyl amine (3) is accompanied by a significant amount of a secondary amine, which, like 3, undergoes cyclization to an indoline and subsequent dehydrogenation to a new indole 8.The side-reaction in the reduction of 2 to 3 is obviated by the use of LiAlH4/AlCl3 (1:1).The final aromatization to yield 5 is vastly improved by replacing MnO2 with DDQ. - Keywords: Polyfluoroaralkylamines; Synthesis; Tetrafluoroindole; NMR spectroscopy; IR spectroscopy
- Filler, Robert,Chen, Wei,Woods, Sarah M.
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