17.alpha.-HYDROXY-1,3,5(10),15-ESTRATETRAENES AND PROCESS FOR TH

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...

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26023955R, 2603974, 2603975, 424243, A61K 3158

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active

040162699

ABSTRACT:
Novel estrogenic 17.alpha.-hydroxy-1,3,5(10),15-estratetraenes of the formula ##STR1## wherein R.sub.1 is H, lower alkyl or lower acyl, R.sub.2 is lower alkyl and R.sub.3 is H, lower alkyl, lower acyl or tetrahydropyranyloxy, are produced by (a) reacting a 16.alpha.,17.alpha.-epoxy-estratriene with lithium halide or HCl in glacial acetic acid; converting the resulting halohydrin into a 16-halo-17-tetrahydropyranyl ether; and splitting off hydrogen halide from therefrom; or (b) reacting the 16.alpha.,17.alpha.-epoxy-estratriene with diphenylselenide and alkali metal borohydride; oxidizing the thus-produced 17.alpha.-hydroxy-16.beta.-phenylselenide to the corresponding phenylselenide oxide; and forming the .DELTA..sup.15 double bond by heating with removal of phenyl--Se--OH.

REFERENCES:
patent: 3079408 (1973-02-01), Mueller
patent: 3433785 (1969-03-01), Manson et al.
patent: 3501509 (1970-03-01), Kuo et al.

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