Verfahren zur Herstellung von Bis-(hydroxymethyl)-pyridindicarbamatderivaten

摘要

The invention comprises compounds of formula wherein R1 is a hydrogen or halogen atom or an alkoxy, dialkylamino, alkylthio, arylthio, or alkylsulphonyl group, R2 is a hydrogen atom or an alkyl, cycloalkyl, alkenyl, aryl, aralkyl, furfuryl, pyridyl or picolyl group and R3 is a hydrogen atom or an alkyl group, or R2 and R3 in combination form an alkylene radical, one CH2OCONR2R3 group being present in the 2-positio and the other in the 5- or 6-position, and their preparation by reaction of the corresponding bis-hydroxymethyl compounds with (a) a compound of formula R2NCO, or a compound convertible thereto during reaction, (b) a compound of formula R2R3NCOX, wherein X is a halogen atom or an alkoxy or phenoxy group, or (c) phosgene and an amine R2R3NH. The compounds of the invention have anti-inflammatory activity. Bis - hydroxymethylpyridines of formula are prepared by reduction of the corresponding bis-carboxylic acid, or a functional derivative thereof, with an alkali metal borohydride.