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US 5,510,490 AGranted
Process for the preparation of epibatidine
AssigneeCouncil of Scientific and Industrial Research
InventorsGanesh Pandey, Trusar D. Bagul, Gingipalli Lakshmaiah
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Abstract
A novel 6-chloro-3-vinyl-pyridine of formula ##STR1## where X represents -H, -SO.sub.2 Ph, -CO.sub.2 Et, -COCH.sub.3 and -CHO; which is used for the synthesis of Epibatidine of formula ##STR2## by reacting said 6-chloro-3-vinyl pyridine with N-1-alkyl-2,5-di(trialkyl silyl) pyrrolidine of formula ##STR3## to obtain N-alkyl Epibatidine which is hydrogenated to obtain the Epibatidine.
Claims9
A process for synthesis of epibatidine of formula:
- ##STR4## which comprises, reacting 6-chloro-3-vinyl pyridine of formula ##STR5## wherein X represents CO.sub.2 Et, CHO, SO.sub.2 Ph, COCH.sub.3 or H with N-1-alkyl-2,5 di (trialkyl silyl) pyrrolidine of formula ##STR6## where R' and R" are each an alkyl group, at a temperature of from 0.degree. to 30.degree. C. in an organic solvent to produce N-alkyl epibatidine of formula ##STR7## where R" is a defined above, and converting said N-alkyl epibatidine to epibatidine by catalytic hydrogenation.
Dependencies are inferred from the claim text.