Invention Grant
- Patent Title: Process for the synthesis of melphalan
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Application No.: US18320326Application Date: 2023-05-19
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Publication No.: US12077484B2Publication Date: 2024-09-03
- Inventor: Pietro Allegrini , Andrea Bonetti , Marco Molinari , Andrea Gambini
- Applicant: Indena S.P.A.
- Applicant Address: IT Milan
- Assignee: Indena S.P.A.
- Current Assignee: Indena S.P.A.
- Current Assignee Address: IT Milan
- Agency: Silvia Salvadori, P.C.
- Agent Silvia Salvadori
- Priority: IT 2019000025348 2019.12.23
- The original application number of the division: US17757830
- Main IPC: C07C227/20
- IPC: C07C227/20
Abstract:
The invention relates to a process for the preparation of Melphalan (4-[bis(2-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.
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.
Public/Granted literature
- US20230286901A1 PROCESS FOR THE SYNTHESIS OF MELPHALAN Public/Granted day:2023-09-14
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