| 摘要 |
1306404 Indenopyridine derivatives SANDOZ Ltd 10 April 1970 [7 May 1969 11 Dec 1969 5 Feb 1970] 17080/70 Heading C2C Novel acid addition salts of compounds of formula wherein R 1 is H, F, Cl, Br or C 1-4 alkyl, R 2 is CN, COOR 5 wherein R 5 is H or C 1-6 alkyl, or R 2 is -CONR 5 R 6 where R 5 is H or C 1-6 alkyl and R 6 is H or C 1-6 alkyl or NR 5 R 6 is a 5 to 7 membered heterocyclic ring, R 3 and R 4 are H or C 1-4 alkyl, and n is 0 to 3, are prepared by removing water from a compound of Formula II by treatment with a strong acid or the chloride, bromide or iodide of a strong acid (e.g. thionyl chloride) and optionally hydrolysing or esterifying the product to convert one value of R 2 to another. Intermediates of Formula II above are prepared by reaction of a compound of formula or with an intermediate of formula Intermediates of Formula III wherein R 1 is Cl, methyl or ethyl are prepared by action of hot KOH on the 5-acetoxy-2-ethoxycarbonyl compound obtained by action of acetic anhydride then chloroformic acid ethyl ester on the 7-R 1 - 1,3,4,4a,5,9b - hexahydro - 2 - methyl - 5(2H)- indeno[1,2c]-pyridinol. Pharmaceutical compositions in conventional forms and having antiphlogistic, ulcer-protective and hypotensive activity comprise an above novel salt and a pharmaceutically acceptable carrier or diluent.
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