title: One-Pot Synthesis of Highly Substituted Nicotinic Acid Derivatives Based on a Formylation Strategy of Enamino Keto Esters.
abstract: A facile one-pot synthesis of 4-chloro or 4-bromonicotinic acid esters with optional 2- and 2,5-disubstitution on the pyridine ring has been developed from easily accessible enamino keto esters by a formylation followed by in situ intramolecular cyclization strategy under optimized Vilsmeier reaction conditions. The effect of the substituents on the β-carbon and the nature of the keto functionality were explored in detail to understand the mechanism of pyridine ring formation under the described conditions.
authors.affiliation: Medicinal Chemistry Division, Glenmark Research Centre, Glenmark Pharmaceuticals Ltd. , Navi Mumbai - 400709, India.
authors.forename: Sukeerthi
authors.initials: S
authors.lastname: Kumar
authors.affiliation: Medicinal Chemistry Division, Glenmark Research Centre, Glenmark Pharmaceuticals Ltd. , Navi Mumbai - 400709, India.
authors.forename: Aarti A
authors.initials: AA
authors.lastname: Sawant
authors.affiliation: Medicinal Chemistry Division, Glenmark Research Centre, Glenmark Pharmaceuticals Ltd. , Navi Mumbai - 400709, India.
authors.forename: Rajendra P
authors.initials: RP
authors.lastname: Chikhale
authors.affiliation: Medicinal Chemistry Division, Glenmark Research Centre, Glenmark Pharmaceuticals Ltd. , Navi Mumbai - 400709, India.
authors.forename: Keya
authors.initials: K
authors.lastname: Karanjai
authors.affiliation: Medicinal Chemistry Division, Glenmark Research Centre, Glenmark Pharmaceuticals Ltd. , Navi Mumbai - 400709, India.
authors.forename: Abraham
authors.initials: A
authors.lastname: Thomas