摘要 |
<p>1,226,813. Glyceryl ester derivatives. SCHERICO Ltd. 5 April, 1968 [10 April, 1967], No. 16479/68. Heading C2C. Novel compounds of general Formula I in which R<SP>a</SP> and R<SP>b</SP> are hydrogen atoms or alkyl radicals, the total number of carbon atoms in R<SP>a</SP> and R<SP>b</SP> being not more than 3, and n is 0 or 1 and their pharmaceutically acceptable cyclic acetals and ketals, preferably of Formula II in which R<SP>1</SP> and R<SP>2</SP> are H, alkyl, aryl or aralkyl or together form a polymethylene group are prepared by condensing a compound of formula Y.CH 2 .X<SP>1</SP> by known methods with a compound of formula Z.CO.CR<SP>a</SP>R<SP>b</SP>.A in which X<SP>1</SP> is anα,#-dihydroxy-ethyl or a cyclic acetal or ketal thereof or a vinyl or epoxy ethyl group and either Y and Z represent groups capable of condensing during esterification one of Y and Z providing the grouping III and A is H or Y represents the group IV and Z and A together represent a further C-C bond and where X<SP>1</SP> is a vinyl or epoxyethyl group converting the product by known methods of oxidation or hydrolysis to the ester I. Intermediates isolated are cyanomethyl salicylate (from reaction of chloroacetonitrile with salicylic acid); #,γ- isopropylidenedioxypropyl salicylate (from reaction of cyano derivative with 2,2 - dimethyl - 4 - hydroxymethyl - 1,3- dioxolan); and 0 - (#,γ- isopropylidenedioxypropyl) - N<SP>1</SP>,N - dicyclohexyl - isourea (by reacting dicyclohexylcarbodiimide with 2,2-dimethyl- 4-hydroxymethyl-1,3-dioxolan). Pharmaceutical compositions used in relief of inflammation and pain comprise a compound I in association with a suitable excipient and may be administered enterally, parenterally or topically.</p> |