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Updated: Jul 15, 2026

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Double dearomatization of bis(diphenylphosphinamides) through anionic cyclization. A facile route of accessing
Gloria Ruiz-Gómez1, María José Iglesias, Manuel Serrano-Ruiz
1Area de Química Orgánica, Universidad de Almería, Carretera de Sacramento, 04120 Almería, Spain.
Abstract:
The sequential one-pot double dearomatization of bis(N-benzyl-P,P-diphenylphosphinamides) via anionic cyclization is described for the first time. Protonation and alkylation of the dearomatized dianions provide bis(tetrahydro-2,1-benzazaphospholes) in good yield and with very high regio- and stereocontrol. Acid-catalyzed methanolysis of the bisheterocycles affords bis(methyl gamma-aminophosphinates) stereospecifically. The doubly phosphorylated systems proved to be active against a series of cancer cell lines.
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