| 摘要 |
<p>derivs. of formula (I), and their D-homo analogues, when W = H, are new: In (I) A is H or, when Y is (H, beta OH), it may be F, Cl or Me); B is H or B+Q is 14 alpha, 17 alpha-alkylideneoxy; X is H, F, Cl or Br; Y is H2 when X is H, or O, (H, beta OH) or (H, beta OCOH), or Y is (H, beta-halo) when X is Cl or Br, the halo being F, Cl or Br and being as electronegative as X; Z is F, Cl, Br or I; Q is H when W is H2 or (H, alkyl), or Q is Cl, Br or OV; V is H or 1-12C hydrocarbylcarboxylic acid acyl or PhCO substd. by halogen or MeO; W is H2, (H, alkyl), (H, alpha-OV1) or =CHT; V1 is a V substituent or retinoyl or isonicotinoyl; T is H, alkyl, F or Cl; W and Q together are 16 alpha, 17 alpha-alkylidenedioxy, 16 alpha, 16 alpha-cycloalkylidenedioxy, -S-CRR-O- or -N=CR1-O- R is alkyl; R1 is alkyl or Ph; M is OR2 (when Q is O-acyl), CHO or their acetals, hemiacetals, or acylals, COOR3, CH2G or OV2; R2 is alkyl or haloalkyl; R3 is 1-12C alkyl; G is H, F, Cl or Br; V2 is a V1 substituent or a phosphoric acid gp. or their mono- or di-alkali(ne earth) metal salts; or OV + OV2 is alkylidenedioxy or alkylorthoalkanoate. The alkyls etc. are "lower", and pref. have 1-4C. (I) have enhanced activity over that shown by the corresp. 7-unsubstd. cpds. In an example, 7 alpha-chloro-16 alpha-methyl-1,4-pregnadiene-11 beta, 17 alpha, 21-triol-3,20-dione, 17,21-dipropionate was obtd. by treating the corresp. 1,4,6-pregnatriene with HCl in dioxan.</p> |
