title: Regioselective Metal-Free Decarboxylative Multicomponent Coupling of α-Amino Acids, Aldehydes and Isonitriles Leading to N-Substituted Azacyclic-2-carboxamides with Antithrombotic Activity.
abstract: An atom-economical regioselective synthesis of N-substituted prolinamides or N-substituted piperidine-2-carboxamides via a metal-free decarboxylative multicomponent coupling between l-proline or pipecolic acid, aldehydes, and isonitriles is described. The cascade event involves sequential imine formation, decarboxylation, isonitrile insertion, and hydrolysis to afford the product in one-pot. Two of the prolinamides were found to display appreciable antithrombotic activity via inhibition of platelet aggregation.
authors.affiliation: Medicinal and Process Chemistry Division and Pharmacology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, PO Box 173, Lucknow, 226031 Uttar Pradesh, India.
authors.forename: Shashikant U
authors.initials: SU
authors.lastname: Dighe
authors.affiliation: Medicinal and Process Chemistry Division and Pharmacology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, PO Box 173, Lucknow, 226031 Uttar Pradesh, India.
authors.forename: Anil Kumar
authors.initials: AK
authors.lastname: K S
authors.affiliation: Medicinal and Process Chemistry Division and Pharmacology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, PO Box 173, Lucknow, 226031 Uttar Pradesh, India.
authors.forename: Smriti
authors.initials: S
authors.lastname: Srivastava
authors.affiliation: Medicinal and Process Chemistry Division and Pharmacology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, PO Box 173, Lucknow, 226031 Uttar Pradesh, India.
authors.forename: Pankaj
authors.initials: P
authors.lastname: Shukla
authors.affiliation: Medicinal and Process Chemistry Division and Pharmacology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, PO Box 173, Lucknow, 226031 Uttar Pradesh, India.
authors.forename: Surendra
authors.initials: S
authors.lastname: Singh
authors.affiliation: Medicinal and Process Chemistry Division and Pharmacology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, PO Box 173, Lucknow, 226031 Uttar Pradesh, India.
authors.forename: Madhu
authors.initials: M
authors.lastname: Dikshit
authors.affiliation: Medicinal and Process Chemistry Division and Pharmacology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, PO Box 173, Lucknow, 226031 Uttar Pradesh, India.
authors.forename: Sanjay
authors.initials: S
authors.lastname: Batra