1471276 5-Benzylpicolinic acid derivatives NIPPON SHINYAKU CO Ltd and TAKARA SHUZO CO Ltd 12 Jan 1976 [22 Jan 1975 (6) 00963/76 Heading C2C The invention comprises compounds of general formula where RSP1/SP and RSP2/SP, which may be the same or different, represent hydrogen, C 1 -C 6 alkyl, halogen, C 1 -C 6 alkoxy, nitro, amino, acetylamino, hydroxy or acetoxy, and R represents hydroxy, alkoxy or -NR 4 R 5 where R and RSP5/SP are hydrogen, C 1 -C 6 alkyl, aralkyl or phenyl. An acid of Formula I (R=OH) may be prepared from the corresponding compound in which there is a methyl group in the 2-position of the pyridine ring either directly by oxidation (e.g. with selenium dioxide) or by first oxidizing with a peracid to the N-oxide, treating this with acetic anhydride to obtain the compound corresponding to I but with a CH 3 COCH 2 - group in the 2-position, hydrolysing this to the HOCH 2 - group and oxidizing, e.g. with permanganic acid, to HOOC-. With compounds of Formula I in which R is hydroxy or alkoxy, the following interconversions of RSP2/SP groups and/or RSP3/SP groups may be carried out by conventional methods: and alkoxy#hydroxy. The free acid (R=OH) may be converted to the ester (R = alkoxy) and the acid or ester may be converted to the amide (H = -NRSP4/SPRSP5/SP). Some of the compounds are isolated as the hydrochlorides. Compounds of Formula I have pharmaceutical activity.
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