| 摘要 |
The nicotinic acid derivs. I(R=H, C1-6 alkyl) were prepd. Thus, R1CHO(R1=2-naphthyl) was treated with MeO2(CH:C(OMe)CH2P+Ph3Br- to give R1CH:CHC(OMe):CHCO2Me which was demethylated to R1CH:CHCOCH2CO2Me and treated with Me2NCH (OME)2 and EtNH2 to give R1CH:CHCOC(CO2Me):CHNHEt. The latter compds. were cyclized in the presence of chloranil to give I(R=Me) which was hydrolyzed to the acid, I(R=H) was active in the turning rat turning rat test at 1 mg/kg i.p.
|
