L. Vo-Quang

Towards new inhibitors of D-alanine:D-alanine ligase: The synthesis of 3-amino butenylphosphonic and aminophosphonamidic acids.

Abstract The condensation of sodium salt of tetraethyl methylenediphosphonate with N-Cbz alaninal followed by the standard acidolytic removal of protecting groups provides an efficient method for the synthesis of 3-aminobutenylphosphonic acid E 3 ; N-Cbz-aminophosphonamidic acid 4 was prepared from diphenyl 1-amino ethylphosphonic acid through methyl phosphochloridate alanine methyl ester condensation in the presence of triethylamine and alkaline partial deprotection.

AN IMPROVED SYNTHESIS OF METHYL 2-N-FORMYLAMINO-2-(DIMETHOXYPHOSPHINYL)-ACETATE

Abstract The title compound was synthesized in high yield by a one pot procedure. Besides allowing an easy purification, this procedure ensures high yields and ready scaling up.

New non-proteogenic aminoacids bearing an enol aryl-ether moiety.

Abstract Aminoacids bearing an enol aryl-ether moiety have been synthesized by a new method allowing a great versatility in the introduction of N-protective groups and enol ether functions. This method involves a Wittig-Horner condensation affording alpha, beta-dehydrohomoserine ether derivatives, followed by a regio and stereoselective isomerization into the desired E enol ether. Clean deprotection was achieved providing new 2-amino-4-aryloxybut-3(E)-enoic acids 3 .

SYNTHESIS OF NEW 3-BENZYLOXYCARBONYLAMINO-1,2-OXAPHOSPHOLANES

Abstract Benzyloxycarbonylamino-1,2-oxaphos-pholane 1b, unknown so far, was synthesized by the phospholactonisation of N-Cbz-homoserine-P. dimethyl ester followed by a deprotection step.

A New and Convenient Synthesis of Alkyl 1-Amino-2 Chloroethylphosphinates

Abstract The alkyl 1-amino-2-chloroalkylphosphinates, unknown so far, are conveniently synthesized upon Michaelis-Arbusov reaction with diethyl methylphosphonite and dimetnyl phenylphosphonite, in fair to good yield.