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：US20130261308A1

公开(公告)日：2013-10-03

申请号：US13852234

申请日：2013-03-28

Applicant: PROCOS. S.P.A.

Inventor： Piergiorgio BETTONI ,  Jacopo ROLETTO ,  Paolo Paissoni

IPC: C07D413/04

CPC classification number: C07D413/04

Abstract: Disclosed is a process for the synthesis of iloperidone starting from 4-hydroxy-3-methoxy acetophenone (acetovanillone), 1-chloro-3-bromo propane and 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride, using a one-pot method. Said process is performed without any intermediate isolation, and is particularly advantageous from the environmental standpoint and in terms of yields, productivity and the purity of the product obtained, both in the reaction mixture and in the crystal isolated.

Abstract translation: 公开了从4-羟基-3-甲氧基苯乙酮（乙腈），1-氯-3-溴丙烷和6-氟-3-（4-哌啶基）-1,2-苯并异恶唑盐酸盐合成起始的方法 ，使用一锅法。 所述方法在没有任何中间分离的情况下进行，并且在环境方面以及在反应混合物和分离的晶体中获得的产物的产率，生产率和纯度方面都是特别有利的。

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.