| 摘要 |
<p>1283804 3,4 - Dihydroxyphenylalanine derivatives F HOFFMANN-LA ROCHE & CO AG 12 May 1970 [14 May 1969] 22808/70 Heading C2C Compounds of Formula I in which R 1 represents hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro or amino, n stands for 1, 2 or 3, R 2 represents hydrogen or lower alkyl, R 3 represents hydroxy or optionally mono- or di-lower alkyl-substituted amino, R 4 represents hydrogen, lower alkyl, lower alkanoyl or aroyl and R 5 represents hydrogen or lower alkyl, "lower" denoting groups containing up to 6 carbon atoms, and salts thereof, which process comprises subjecting a compound of the general Formula II wherein one of the substituents R 6 and R 7 is hydroxy and the other substituent is lower alkanoyl, aroyl or carboxy, or a salt of such a compound to an oxidative rearrangement and saponifying the carboxylic acid ester obtained and, in any desired sequence, hydrolysing the product obtained if desired, resolving a racemate obtained into its optically active forms, if desired, and converting a product obtained into a salt if desired. Pharmaceutical compositions in conventional forms and having hypotensive and anti- Parkison activity comprise a novel compound of Formula I above, i.e. one in which n is 1 and R 1 is halogen or C 1-6 alkyl provided that R 2 is alkyl when R 1 is in the 2-position and R 2 is alkyl when R 1 is alkyl, and a carrier or diluent. Reference has been directed by the Comptroller to Specification 1,023,204.</p> |
