97338-02-8Relevant articles and documents
A PROCESS FOR THE SYNTHESIS OF MELPHALAN
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Page/Page column 16, (2021/07/02)
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.
Synthesis process of N-paraphthalyl(diethanol)amino-L-phenylalanine ethyl ester
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, (2017/10/28)
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.