公开(公告)号：US20220098216A1

公开(公告)日：2022-03-31

申请号：US17426356

申请日：2020-03-25

Applicant: PROCOS S.P.A.

Inventor： Alberto LENA ,  Antonio TOPPINO ,  Katia MIELE ,  Jacopo ROLETTO ,  Paolo PAISSONI

IPC: C07D498/22

Abstract: A process for the preparation of midostaurin with high purity, particularly a process for the preparation of midostaurin with a content of oxidation impurities lower than 0.1% comprising the treatment of crude midostaurin or staurosporine with strong organic or inorganic acids in a water-immiscible solvent and, optionally, also with reducing silanes is described.

公开(公告)号：US20180319747A1

公开(公告)日：2018-11-08

申请号：US15771050

申请日：2016-10-27

Applicant: PROCOS S.p.A.

Inventor： Matteo MOSSOTTI ,  Alessandro BAROZZA ,  Jacopo ROLETTO ,  Paolo PAISSONI

IPC: C07D213/64

CPC classification number: C07D213/64

Abstract: Disclosed is a process for the synthesis of Pirfenidone (1) from 5-methyl-2(1H)-pyridinone and chlorobenzene in the presence of a catalytic system consisting of a copper salt and an organic ligand, in the presence of a base. The process exploits the high efficiency of the catalytic system consisting of copper(I) salt and an organic ligand in the presence of an inorganic base in the N-amidation reaction of chlorobenzene, a cheap reagent also usable as solvent in this case; reaction conditions at high temperatures, at atmosphere pressure or higher, produce a reaction with good yields.