110461-12-6

Upstream product

• 103-72-0 phenyl isothiocyanate 
• 762-04-9 phosphonic acid diethyl ester 
• 1021879-82-2 α-(diethoxyphosphoryl)methyl 5-(1-phenyl)-1H-tetrazolyl sulfoxide 
• 62-53-3 aniline 
• 14540-22-8 diethyl (tert-butyl) phosphite 
• 122-52-1 triethyl phosphite 

Relevant academic research and scientific papers

Synthesis and structural Studies of phosphonothioamidates

The reaction of isothiocyanates with dialkylphosphites in the presence of strong base yielded the phosphonothioamides 2. Treatment of 2 with methyl iodide afforded the corresponding thioimidates 3 with high yields. All compounds were characterized on the

CeCl3.7H2O-SiO2 catalyzed ultrasonicated solvent-free synthesis of carbamoyl/carbamothioyl phosphonates and antimicrobial activity evaluation

an expeditious and green method has been developed for the synthesis of a series of PC bond derivatives, diethyl substituted phenylcarbamoylphosphonates 6(a-e)/phenylcarbamothioylphosphonates 7(a-f) in high yields via simple addition reaction of isocyanates/isothiocyanates with diethyl phosphite in the presence of silica supported Lewis acid catalyst, SiO2-CeCl3.7H2O under solvent-free and sonication conditions. The advantages of this method are high yields, avoiding of harmful solvents, operational simplicity, shorter reaction time, and recoverability and recyclability of the catalyst. Antimicrobial activity was assayed for the title compounds, whereas the compounds 6c, 7b, and 7e against bacteria, and 6a, 7b, 7c, and 7e against fungi exhibited potential growth of inhibition.

Synthesis, Design, and Biological Evaluation of Novel Diethylphenylcarbamothioylphosphonate

Abstract: The aim of this work was to synthesize a diethyl phenylcarbamothioyl phosphonate (EThmP) and evaluate its biological activities. ThmP has been prepared with high yields and its conformation was determined. This phosphonothioamidate derivative was characterized by IR, and NMR Spectroscopy (1H, 13C, and 31P). On the component of EThmP, the Hirshfeld surface analysis indicates that the major contributions for the crystal packing are H···H (53.3%), H···O (12.9%) H···S (14.5%), and C···H (17.6%) interactions. An anti-nociceptive test (the formaline test) showed that the EThmP modulates the pain during the early and late phases proved by rat behavior characterized by absence of licking, biting and shaking of the affected paw. The modulation of pain by the EThmP may be due to its anti-inflammatory effect. The Hot Plate test showed that the pretreatment with the EThmP did not modulate the pain nociception induced by maintaining the rat at a fixed temperature of 48°C. The treated rats’ behavior was characterized by elevating, licking the paw, jumping and fleeing. EThmP did not affect the memory capacity and acetylcholinesterase activity. The morbidity of rats was normal with no mortality or sign of toxicity. The in vitro study showed that the EThmP has no antibacterial, antifungal and antioxidant activities. The EThmP has an important dose dependent anti-inflammatory activity.

An efficient method for the phosphonation of C=X compounds

Reaction of trialkyl phosphites with C=X electrophiles (aldehydes, ketones, ketophosphonates, aldimines, ketimines, isocyanates, isothiocyanates, and activated olefins) in the presence of amines and anilines hydrohalides was studied. We found that pyridine hydrohalides effectively activate the reaction of tralkyl phosphites with various C=X electrophiles: aldehydes, ketones, ketophosphonates, aldimines, ketimines, isocyanates, isothiocyanates, and activated olefins. Particularly high activity showed pyridine hydroiodide. This reaction is a convenient method of synthesis of hydroxyphosphonates, aminophosphonates, carbamoylphosphonates, carbamoylthiophosphonates, and methylenebisphosphonates. Pleiades Publishing, Ltd., 2010.

A novel and convenient method for synthesis of carbamoyl and thiocarbamoyl phosphonates

A simple, efficient, and general method has been developed for the synthesis of carbamoyl and thiocarbamoyl phosphonic esters using CaCl 2 as an efficient Lewis base catalyst. Carbamoyl and thiocarbamoyl phosphonic esters were obtained in good

Thermolyses of α-phosphorylmethyl tetrazolyl sulfoxides in the presence of 2,3-dimethyl-1,3-butadiene and their reactions with several amines

We have synthesized α-(phosphoryl)methyl tetrazolyl sulfoxides and examined the reactivities in the thermolyses and in the presence of several amines, such as aniline, benzylamine, piperidine, pyrrolidine, and morpholine. Thermolyses of the derivatives in the presence of 2,3-dimethyl-1,3-butadiene afforded 2-phosphoryl substituted 4,5-dimethyl-3,6-dihydro-2H-thiopyran S-oxide. In addition, novel phosphinecarbothioamides were obtained in the reaction of the derivatives with amines.