NOUVEAUX DERIVES DE L'ACIDE PICOLIQUE ET PROCEDE POUR LEUR PREPARATION

摘要

1369718 Picolinic acid derivatives BANYU PHARMACEUTICAL CO Ltd and H HIDAKA 14 April 1972 [16 April 1971 29 Nov 1971] 17424/72 Heading C2C Novel compounds of the Formula I wherein Y is -NR1R2, R 1 is C 1-4 alkyl, R 2 is hydrogen or C 1-4 alkyl or R 1 and R 2 together with the nitrogen atom attached form a saturated 5- or 6-membered heterocyclic ring containing at least one nitrogen atom, the ring being bonded to the remainder of the picolinic acid derivative at the said nitrogen atom or at one of said nitrogen atoms, are prepared by reaction of a (halogeno-methyl) picolinic acid or an ester thereof with a required dithiocarbamic acid of the formula Y-CS-SH, followed where necessary by hydrolysis of the corresponding ester intermediate. 5-Chloromethyl picolinic acid ethyl ester may be prepared by chlorination of 5-hydroxymethyl picolinic acid ethyl ester with SOCl 2 . Pharmaceutical compositions of the compounds I show circulatory, nervous system and antiallergic activity and are especially useful for hypertension, Parkinsonism, alcoholism, schizophrenia and manic depressive disease.