公开(公告)号：US20210246123A1

公开(公告)日：2021-08-12

申请号：US16972856

申请日：2019-06-13

申请人： OLON S.P.A.

发明人： Giorgio Bertolini ,  Lazzaro Feliciani ,  Davide Longoni ,  Mara Sada ,  Matteo Valli

IPC分类号： C07D405/06

摘要： The invention relates to a process for the preparation of Lifitegrast of formula (I), which comprises: a) condensation of the compound of formula (II) with the compound of formula (III) to give the compound of formula (IV) wherein R1, R2 and R3 are independently selected from straight or branched C1-C6 alkyl groups; b) chlorination of compound (IV) in the presence of a chlorinating agent (IV), (V), c) condensation of compound (V) with amino acid (VI) to give compound (I), c) condensation of compound (V) with amino acid (VI) to give compound (I), d) optional purification of the crude Lifitegrast in mixtures of polar aprotic solvents and water.

公开(公告)号：US11325922B2

公开(公告)日：2022-05-10

申请号：US16926370

申请日：2020-07-10

申请人： OLON S.P.A.

发明人： Federico Gassa ,  Lazzaro Feliciani ,  Alberto Mazza ,  Marco Quaroni ,  Mara Sada ,  Giorgio Bertolini

IPC分类号： C07F5/02

摘要： The present invention relates to a process for the preparation of crisaborole of formula (I): by preparing intermediates of formulas (II) and (III):

公开(公告)号：US11498917B2

公开(公告)日：2022-11-15

申请号：US16972856

申请日：2019-06-13

申请人： OLON S.P.A.

发明人： Giorgio Bertolini ,  Lazzaro Feliciani ,  Davide Longoni ,  Mara Sada ,  Matteo Valli

IPC分类号： C07D405/06

摘要： The invention relates to a process for the preparation of Lifitegrast of formula (I), which comprises: a) condensation of the compound of formula (II) with the compound of formula (III) to give the compound of formula (IV) wherein R1, R2 and R3 are independently selected from straight or branched C1-C6 alkyl groups; b) chlorination of compound (IV) in the presence of a chlorinating agent (IV), (V), c) condensation of compound (V) with amino acid (VI) to give compound (I), c) condensation of compound (V) with amino acid (VI) to give compound (I), d) optional purification of the crude Lifitegrast in mixtures of polar aprotic solvents and water.

公开(公告)号：US10329311B1

公开(公告)日：2019-06-25

申请号：US15927264

申请日：2018-03-21

申请人： OLON S.p.A.

发明人： Federico Gassa ,  Lazzaro Feliciani ,  Alberto Mazza ,  Marco Quaroni ,  Mara Sada ,  Giorgio Bertolini

IPC分类号： C07F5/02 ,  C07C39/205 ,  B01J27/053 ,  B01J23/44 ,  B01J23/42 ,  C07C39/15 ,  C07C37/02 ,  B01J27/232

CPC分类号： C07F5/027 ,  B01J23/42 ,  B01J23/44 ,  B01J27/053 ,  B01J27/232 ,  C07B47/00 ,  C07C37/02 ,  C07C39/15 ,  C07C39/205 ,  C07C255/50 ,  C07F5/025

摘要： The present invention relates to a process for the preparation of crisaborole of formula (I): by preparing intermediates of formulas (II) and (III):