Paper
Synthesis of 8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepten[1,2-b]pyridine-11-one
Published 2013 · Z. Guan
Chinese Journal of Pharmaceuticals
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Abstract
8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepten[1,2-b]pyridine-11-one, the important intermediate of loratadine, was synthesized from 2-cyano-3-methylpyridine via Ritter reaction and alkylation to give 3-[2-(3-chlorophenyl)ethyl]-N-(1,1-dimethylethyl)-2-pyridinecarboxamide, which was subjected to hydrolysis with methanesulfonic acid, treatment with sulfi nyl chloride and Friedel-Crafts acylation with an overall yield of about 36%.
8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepten[1,2-b]pyridine-11-one, an intermediate in loratadine, was synthesized from 2-cyano-3-methylpyridine via the Ritter reaction and alkylation
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