A Facile Synthesis of 2-Chloro-5,7-dihydro-pyrrolo[3,4-b]pyridine-6-carboxamidine, an Annulated Nicotinoid

摘要

The chloropyridine moiety confers high potency to several types of analgesics and insecticides acting at nicotinic acetylcholine receptors (nAChRs).This includes (-)-epibatidine 1,isolated from the skin of Ecuadorian poison frog Epipedobates tricolor.The pharmacological profiles of 1 show the exceptionally strong analgesic activity and the high affinity for nAChR.Recent advances in the search for nAChR ligands include the discovery of ABT-594 2,currently in development for the treatment of Parkinson's and Alzheimer's disease.Whereas,imidacloprid 3,one of the most important synthetic insecticides,acts selectively at the insect versus the mammalian nAChR.