97730-49-9

Upstream product

• 189264-23-1 (S)-2-[2-(Diethoxy-phosphoryl)-acetylamino]-succinic acid di-tert-butyl ester 
• 118903-72-3 N-(Phosphonoacetyl)-L-asparaginsaeure-di-(p-nitrobenzyl)-P,P-dimethylester 
• 118903-73-4 N-(Phosphonoacetyl)-L-asparaginsaeure-di(p-nitrobenzyl)ester 

Relevant academic research and scientific papers

A new, efficient, two step procedure for the preparation of the antineoplastic agent sparfosic acid

Sparfosic acid can easily be prepared in two steps and in excellent yield from condensation of the commercially available starting materials L-aspartic acid di-tert-butyl ester hydrochloride and diethylphosphonoacetic acid, followed by a quadruple deprotection of acidic functions under mild conditions using bromotrimethylsilane.

Preparation of N-(phosphonoacetyl)-L-aspartic acid

Improved methods for preparation of the tetrasodium and disodium salts ofN-(phosphonoacetyl)-L-aspartic acid (PALA) are disclosed. The present methods are well suited for preparation of these products in large amounts. Particular aspects of these methods include: (1) the initial preparation of phosphonoacetyl chloride which is employed in producing the desired products; and (2) the use of anhydrous conditions for preparation and isolation of the cyclohexylammonium salt of dibenzyl PALA.