公开(公告)号：US12077484B2

公开(公告)日：2024-09-03

申请号：US18320326

申请日：2023-05-19

申请人： Indena S.P.A.

发明人： Pietro Allegrini ,  Andrea Bonetti ,  Marco Molinari ,  Andrea Gambini

IPC分类号： C07C227/20

CPC分类号： C07C227/20

摘要： 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.

公开(公告)号：US20230286901A1

公开(公告)日：2023-09-14

申请号：US18320326

申请日：2023-05-19

申请人： Indena S.P.A.

发明人： Pietro Allegrini ,  Andrea Bonetti ,  Marco Molinari ,  Andrea Gambini

IPC分类号： C07C227/20

CPC分类号： C07C227/20

摘要： 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.

公开(公告)号：US20230094970A1

公开(公告)日：2023-03-30

申请号：US17757830

申请日：2020-12-21

申请人： Indena S.P.A.

发明人： Pietro Allegrini ,  Andrea Bonetti ,  Marco Molinari ,  Andrea Gambini

IPC分类号： C07C227/20

摘要： 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.

公开(公告)号：US11787761B2

公开(公告)日：2023-10-17

申请号：US17757830

申请日：2020-12-21

申请人： Indena S.P.A.

发明人： Pietro Allegrini ,  Andrea Bonetti ,  Marco Molinari ,  Andrea Gambini

IPC分类号： C07C227/20

CPC分类号： C07C227/20

摘要： 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.