80902-08-5

Upstream product

• 18108-16-2 benzyl hypophosphite 
• 74-88-4 methyl iodide 
• 4206-94-4 methylphosphinic acid 
• 100-51-6 benzyl alcohol 

Downstream Products

• 874292-16-7 O-benzyl methyl-[[(N-benzyloxycarbonyl-L-γ-glutamyl(α-benzyl ester)-L-leucyl)amino]methyl]phosphinate 
• 874292-09-8 O-benzyl methyl(aminomethyl)phosphinate 
• 880335-30-8 benzyl (N-benzyloxycarbonyl-4-piperidinyl)methylphosphinate 

Relevant academic research and scientific papers

Direct monoalkylation of alkyl phosphinates to access H-phosphinic acid esters

Simple alkyl phosphinates prepared by the silicate esterification method can be alkylated under Barbier-like conditions with butyl lithium at -78 °C followed by warming to room temperature. The method is limited to the more reactive electrophile such as allylic bromides and alkyl iodides. With these electrophiles good yields of H-phosphinic acid esters are generally obtained in a straightforward manner. Georg Thieme Verlag Stuttgart.

Design, synthesis, and biological evaluation of phosphinopeptides against Trypanosoma cruzi targeting trypanothione biosynthesis

As a part of our project aimed at the search for new safe chemotherapeutic and chemoprophylactic agents against American trypanosomiasis (Chagas's disease); a series of phosphinopeptides structurally related to glutathione was designed, synthesized, and evaluated as antiproliferative agents against the parasite responsible for this disease, the hemoflagellated protozoan Trypanosoma cruzi. The rationale for the synthesis of these compounds was supported on the basis that the presence of the phosphinic acid moiety would mimic the tetrahedral transition state of trypanothione synthase (TryS), a typical C:N ligase, and the molecular target of these drugs. Of the designed compounds, 53 and 54 were potent growth inhibitors against the clinically more relevant form of T. cruzi (amastigotes) growing in myoblasts. The efficacy for these drugs was comparable to that exhibited by the well-known antiparasitic agent WC-9. The simple phosphinopeptide structure found as a pharmacophore in the present study constitutes a starting point for the development of straightforward optimized drugs.

Prodrugs of NAALAdase inhibitors

The present invention relates to prodrugs of NAALADase inhibitors, pharmaceutical compositions comprising the same, and methods of using the same to treat glutamate abnormalities and prostate diseases.

NAALADase inhibitors

The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit N-Acetylated alpha -Linked Acidic Dipeptidase (NAALADase) enzyme

Inhibitors of NAALADase enzyme activity

The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel methods of using phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives to inhibit N-Acetylated alpha -Linked Acidic Dipeptidase (NA

Pharmaceutical compositions and methods of treating a glutamate abnormality and effecting a neuronal activity in an animal using NAALADase inhibitors

The present invention relates to a method of treating a glutamate abnormality and a method of effecting a neuronal activity in an animal using a NAALADase inhibitor, and a pharmaceutical composition comprising an effective amount of a NAALADase inhibitor

Certain dioic acid derivatives useful as NAALADase inhibitors

The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit N-Acetylated alpha -Linked Acidic Dipeptidase (NAALADase) enzyme

Methods of cancer treatment using naaladase inhibitors

The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel methods of using phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives to inhibit N-Acetylated alpha -Linked Acidic Dipeptidase (NA

PHARMACEUTICAL COMPOSITIONS AND METHODS OF TREATING COMPULSIVE DISORDERS USING NAALADASE INHIBITORS

The present invention relates to a pharmaceutical composition and a method for treating a compulsive disorder using a NAALADase inhibitor.