A New family of Sulfamidophosphonates Derivatives: Microwave‐Accelerated Multicomponent Synthesis, Characterization and X‐Ray Crystallographic Study**

Abstract

In this present study, we describe a simple, effective and greener one‐pot microwave‐assisted synthesis of novel α‐sulfamidophosphonates 4(a–l), and 5(a, b) that were rationally designed and synthesized following the principle of the superposition of bioactives substructures. This reaction was accomplished by the condensation of various aromatic aldehydes, sulfamide and diethyl phosphite via the Kabachnik‐Fields reaction using ethanol as solvent under catalyst‐free conditions. The corresponding products were obtained with good yields, in short reactions time and no side product was observed. All the newly synthesized compounds were systematically characterized by IR, 1H NMR, 13C NMR and 31P NMR analysis and the structures of the compounds 4 b and 4 c were further analyzed by single crystal X‐ray diffraction.

An attempt to prepare sulfonyl analogues of fotemustine: unexpected rearrangement to sulfamate during nitrosation step

“…In continuity of our investigations concerning the preparation of novel bioactive compounds containing organo-phosphorus and sulfur moieties, 14 and in order to minimize the toxic effect of conventional nitrosoureas, 15 our aim in this paper was oriented towards the synthesis of new analogues of fotemustine. Particularly, we focused our work on the synthesis of analogues bearing a sulfamide function and an aryl substituent in place of the methyl one, on the terminal amino phosphonate moiety of fotemustine.…”