Microwave-assisted synthesis of N-heterocycles and their evaluation using an acetylcholinesterase immobilized capillary reactor

Author(s)

Diego P. Sangi ^{[1, 2]} ; Julia L. Monteiro ^[1] ; Kenia L. Vanzolini ^[1] ; Quezia B. Cass ^[1] ; Marcio W. Paixão ^[5] ; Arlene G. Corrêa ^[6]

Affiliation

^[1] Univ Fed Sao Carlos, Dept Quim, BR-13565905 Sao Carlos, SP - Brazil

^[2] Univ Fed Fluminense, Inst Ciencias Exatas, BR-27213145 Volta Redonda, RJ - Brazil

^[3] Universidade Federal de São Carlos. Departamento de Química - Brasil

^[4] Universidade Federal de São Carlos. Departamento de Química - Brasil

• Document type: Journal article
• Source: Journal of the Brazilian Chemical Society; v. 25, n. 5, p. 887-889, 2014-05-00.

Abstract

Polarized ketene dithioketals have been recognized as useful building blocks in many synthetic operations. In this work, a transition-metal-free annulations of 1,1-bis(thiomethyl)-2-nitroethylene with hydroxylalkylamines or alkyldiamines have been reported. This methodology provides a directed approach to N-heterocycles, e.g., imidazolidines, oxazolidines and benzoxazoles under microwave conditions. These compounds were evaluated as acetylcholinesterase inhibitors by using an enzyme immobilized capillary reactor-tandem mass spectrometry. (AU)

• FAPESP's process: 09/54040-8 - Acquisition of a high-resolution Orbitrap mass spectrometer for the discovery and structural analysis of biologically active compounds: applications in proteomics, biomarkers, synthesis, isolation, and characterization of natural products, studies of redox systems in food and enzymatic synthesis
• Grantee: Emanuel Carrilho
• Support Opportunities: Multi-user Equipment Program
• FAPESP's process: 09/07281-0 - Asymmetric organocatalysis: design of new organocatalysts and development of new methodologies
• Grantee: Márcio Weber Paixão
• Support Opportunities: Research Grants - Young Investigators Grants