9-ALPHA-HYDROXY STEROIDS AND PROCESS FOR THEIR PREPARATION

WIPO Patent Application WO1988002753

A3

9-Alpha-hydroxy- steroids (I) contg. a D-ring of formula (A) are new; R2 = ethynyl (provided R5 is not acetoxy if R4 = H), haloethynyl, opt. protected OH, cyano, 1'-Ra-ethenyl; or 1',1'-trimethylene dithio-ethyl; Ra = 1-6C alkoxy or alkylthio, aryloxy or arylthio; R3 = H; R4 = H, OH, alpha or beta-Me or R3and R4 are together = CH2, or R2 and R3 are together a double bond; R5 = CN, COCHR1R1', CONH2, OH, opt. halo-substd. ethynyl; sulphonate, sulphite, trialkylsilyloxy, formyloxy, opt. halo-substd. 1-6C acyloxy, C(=NR80)Me, C(NHR82)=CH2 or C(=NR80)CH2X; X = halo; R80 = H, COR81 or trialkylsilyl; R81 = H, 1-6C alkyl or phenyl (opt. substd. by 0-2 chloro, Me or NO2); R82 = COR81, trialkylsilyl or R2 and R5 are together carbonyl (provided R4 is not H); R1 = halo or opt. substd. benzoyloxy or (provided R4 is not H)OH, opt. halogenated 1-6C carboxylic acyloxy or H; R'1 = H, Cl, Br or I.

BATIST JACOBUS NICOLAAS MARIA (NL)
MARX ARTHUR FRIEDRICH (NL)
VAN ZOEST WILLEM JOHAN (NL)
KAPUR JAGDISH CHANDER (NL)

PCT/NL1987/000026

June 30, 1988

October 09, 1987

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GIST BROCADES NV (NL)
BATIST JACOBUS NICOLAAS MARIA (NL)
MARX ARTHUR FRIEDRICH (NL)
ZOEST WILLEM JOHAN VAN (NL)
KAPUR JAGDISH CHANDER (NL)

C07D235/28; C07D401/12; C07D413/12; C07D417/12; C07J3/00; C07J5/00; C07J7/00; C07J13/00; C07J21/00; C07J1/00; C07J31/00; C07J33/00; C07J41/00; C07J43/00; C07J51/00; (IPC1-7): C07J1/00; C07J5/00; C07J7/00; C07J13/00; C07J21/00; C07J41/00; C07J43/00; A61K31/565; A61K31/57

US4397947A	1983-08-09
GB2102805A	1983-02-09
EP0153001A2	1985-08-28
US4102907A	1978-07-25
US4035236A	1977-07-12

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