| 摘要 |
Prepn. of 6beta,7-methylene-3-oxo-Delta4-steroids of formula (I) are prepd. from the corresp. 3,5-dihydroxy-Delta6-steroids of formula (II) by (a) reacting with CH2I2 in the presence of Zn/Cu; (b) treating the resulting 6beta,7-methylene-3,5-diol (after liberating the 3-OG gp., if necessary) with an oxidising agent to dehydrate the 3-OH gp; and (c) eliminating the 5-OH gp. Additional steps can be performed between (a) and (c) to convert the R gp. - In the formula n= 1 or 2; R is (i) opt. ketalised oxo, (ii) an opt. etherified or esterified OH gp. together with an H atom or n opt. substd. lower aliphatic hydrocarbon radical, (iii) an H atom together with an opt. substd. lower alkyl gp., or (iii) a gp. of formula (III): R1 is 2 H atoms, an oxo gp., or a lower alkoxy gp. and an H atom; R2 is OH opt. etherified by an easily removable protecting gp. or esterified by a carboxylic acid. - Intermediates of formula (II) are new cpds. Cpds. (I) where n=1, R=(III) and R1=2H or O are aldosterone inhibitors. The other cpds. (I) are useful as intermediates for these and other pharmaceuticals and food additives.
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