97338-02-8

Upstream product

• 74743-23-0 N-phthalimido-4-amino-L-phenylalanine ethyl ester 
• 36097-39-9 (S)-methyl 2-acetamido-3-(4-nitrophenyl)propanoate 
• 147065-06-3 L-nitrophenylalanine hydrochloride 
• 34276-53-4 ethyl (S)-2-amino-3-(4-nitrophenyl)propionate 
• 17451-67-1 N-phthalimido-4-nitro-L-phenylalanine ethyl ester 
• 555-16-8 4-nitrobenzaldehdye 
• 17451-66-0 N-phthaloyl-3-(4-nitrophenyl)-(S)-alanine 
• 85-44-9 phthalic anhydride 
• 207569-25-3 p-nitro-L-phenylalanine hydrate 
• 75-21-8 oxirane 

Downstream Products

• 792864-20-1 N-phthalimido-4-(bis-2-chloroethyl)amino-L-phenylalanine ethyl ester 

Relevant academic research and scientific papers

A PROCESS FOR THE SYNTHESIS OF MELPHALAN

The invention relates to a process for the preparation of Melphalan (4-[bis(2-5 chloroethyl)amino]-L-phenylalanine of formula (I) said process comprising the reaction of a 4-amino-L-phenylalanine protected at the carboxy and amino aminoacidic groups with an agent able to convert the aromatic amino group into a group of formula: -N(CH2CH2OS(O)nO-)2, wherein n is 1 or 2 followed by conversion of the –-N(CH2CH2OS(O)nO-)2 group into a -N(CH2CH2Cl)2 group. The invention also provides novel intermediates useful for the preparation of Melphalan.

Melphalan intermediate and preparation method thereof

The invention discloses a Melphalan intermediate and a preparation method thereof. The Melphalan intermediate is prepared by acidifying a compound p-nitrobenzaldehyde under the action of methanol, a hydrochloric acid solvent, etc. The preparation method has a route with mild reaction conditions, is higher than an existing preparation method in yield, is economical and effective, and is suitable for large-scale industrial production. The synthesis route is as shown in the description.

Synthesis process of N-paraphthalyl(diethanol)amino-L-phenylalanine ethyl ester

The invention provides a synthesis process of N-paraphthalyl(diethanol)amino-L-phenylalanine ethyl ester. The process includes the first step of amino protection reaction, the second step of esterification reaction, the third step of reduction reaction and the fourth step of substitution reaction. According to the synthesis process, amino is protected by phthalic anhydride, and then esterification, reduction and substitution are conducted obtain the product. The process has the advantages of being low in cost, mild in reaction condition, low in toxicity, convenient to operate, high in yield and suitable for industrial production.