摘要 |
1506824 9 - Deoxo - 9 - methyleneprostaglandins UPJOHN CO 12 Feb 1976 [10 Mareh 1975] 29138/77 Divided out of 1506822 Heading C2C [Also in Division C3] The invention comprises 9 - deoxo - 9- methyleneprostaglandins of the Formula I wherein Z is -CH 2 CH 2 - or cis-CH=CH-; one of A 1 and As is H, methyl or ethyl and the other is hydroxy; R 2 and R 3 are H, methyl or ethyl with the proviso that R 2 and R 3 are both H if one of A 1 and A 2 is methyl or ethyl; and R is H or C 1-4 alkyl. The compounds are prepared by silylating the C-11 and C-15 hydroxy groups of the Formula II reacting the silylated products with the carbanions of N,S-dimethyl-S-phenylsulphoxime, removing the silyl ether groups from the resulting products, treating the adducts of the Formula II thus obtained in which the 9-oxo group is replaced by a group of the formula with aluminium amalgam, and, if desired, hydrolysing the resulting alkyl esters of Formula I above. Pharmaceutically compositions, suitable for oral, parenteral, rectal, vaginal or topical administration, contain the above prostaglandins of Formula I together with pharmaceutically acceptable carriers. The compounds possess similar pharmacological activities to the naturally occurring prostaglandins.
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