Indena S.p.a.

Marco Molinari

Pietro Allegrini

Andrea Gambini

Andrea Bonetti

The invention relates to a process for the preparation of Melphalan (4-[bis(2-chloroethyl)amino]-L-phenylalanine of formula (I) The invention also provides novel intermediates useful for the preparation of Melphalan.

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: &#x2014;N(CHCHOS(O)O&#x2014;), wherein n is 1 or 2 followed by conversion of the &#x2192;N(CHCHOS(O)O&#x2014;)group into a &#x2014;N(CHCHCl)group. The invention also provides novel intermediates useful for the preparation of Melphalan.

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Milan, Italy

Marco Molinari