A family of α-aryl-α-aminophosphonates and α-aryl-α-aminophosphine oxides was synthesized by the microwave-assisted solvent-free addition of dialkyl phosphites and diphenylphosphine oxide, respectively, to imines formed from benzaldehyde derivatives and primary amines. After optimization, the reactivity was mapped, and the fine mechanism was evaluated by DFT calculations. Two α-aminophosphonate...

An enantioselective dearomatization of isoquinolines has been developed using chiral anion-binding catalysis. This transformation, catalyzed by a simple and easy to prepare tert-leucine-based thiourea derivative, makes use of silyl phosphite as a nucleophile and generates cyclic α-aminophosphonates. This is the first time asymmetric anion-binding catalysis has been applied to the synthesis of α...

Four diphenyl pyrene-derived aminophosphonates were synthesized. Attempts were made to synthesize diphenyl N-(R)-α-methylbenzylamino(pyren-1-yl)methylphosphonate (3e) in order to obtain the chiral aminophosphonate bearing a pyrene moiety. Because these attempts failed, dimethyl and dibenzyl N-(R)-α-methylbenzyl substituted aminophosphonates 4 and 5 were synthesized and the predominant diastereo...

α-Aminophosphonates are bioisosteres of amino acids and have several pharmacological activities. These compounds have been synthesized by various routes from reaction between amine, aldehyde, and phosphite compounds. In order to synthesize α-aminophosphonates, catalytic effect of CuCl2 was compared with FeCl3. Also all designed structures as well as griseofulvin were docked into the active site...

Catalytic asymmetric endo-selective [3+2] cycloaddition reactions of Schiff bases of α-aminophosphonates with olefins are described. While the efficient asymmetric synthesis of several phosphonate analogues of proline derivatives is important in bioorganic chemistry, a direct catalytic method to prepare optically active endo [3+2] cycloadducts of α-aminophosphonates with olefins has never been ...

In this paper, the applicability of immobilized lanthanum (III) triflate on amine grafted graphene oxide [La(OTf)2-amine grafted-GO] as the first multifunctional catalyst is described for the efficient synthesis of α-aminophosphonates by one-pot three-component reaction of carbonyl compounds, substituted anilines and trialkyl phosphites. Various α-aminophosphonates were synthesized in good to h...

An efficient catalytic process for the synthesis of α-aminophosphonates is developed by a one-pot three-component reaction in presence In complexes at room temperature. DFT based mechanistic studies reactions are reported.

We report an organocatalyzed direct enantioselective hydrophosphonylation of N-unsubstituted ketimines that affords N-unprotected α-tetrasubstituted α-aminophosphonates without protection/deprotection steps. The reaction is suitable for isatin-derived and trifluoromethyl ketimines, affording products in high yields with excellent enantioselectivity. Applications the a proposed transition state ...

Abstract: Highly convergent Synthesis of -aminophosphonates were most conveniently achieved using organophosphorus chemistry. Synthesis of -aminophosphonates were accomplished by three-component coupling of carbonyl, amine and hydrophosphoryl compounds. These aminophosphonates exhibited promising antimicrobial, antioxidant and anticancer activity. Some recent developments and applications to th...