公开(公告)号：WO2019086434A1

公开(公告)日：2019-05-09

申请号：PCT/EP2018/079675

申请日：2018-10-30

Applicant: PROCOS S.P.A.

Inventor： DONNOLA, Monica ,  MOSSOTTI, Matteo ,  BARBERO, Mauro ,  ROLETTO, Jacopo ,  PAISSONI, Paolo

IPC: C07D453/02

CPC classification number: C07D453/02

Abstract: The present invention discloses a process for the preparation of 2-benzhydryl-3-quinuclidinone (1). (I). The process of the invention allows to obtain the intermediate 2-benzhydryl-3-quinuclidinone (1) by reaction of 2-benzylidene-3-quinuclidinone (2) with the Grignard reagent phenylmagnesium halide, in particular chloride or bromide, in the presence of catalytic amounts of copper (I) salts. Taking advantage of the high efficiency of the catalytic system of the copper (I) salts, 2-benzhydryl-3-quinuclidinone (1) is obtained in higher yields than those of the known processes. Advantageously, since the amounts of copper (I) salts are catalytic, the latter can easily be removed from the reaction mixture, and the process is carried out in the presence of solvents less toxic and expensive than those used in the state of the art.

公开(公告)号：WO2017072216A1

公开(公告)日：2017-05-04

申请号：PCT/EP2016/075899

申请日：2016-10-27

Applicant: PROCOS S.p.A.

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

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 thepresence of a base. The process exploits the high efficiency of the catalytic system consisting of copper(I) salt and an organic ligandin 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 pressureor higher, produce a reaction with good yields.

Abstract translation: 公开了一种由5-甲基-2（1H） - 吡啶酮和氯苯在由铜盐和有机配体组成的催化体系存在下合成吡非尼酮（1）的方法， 在一个基地的存在。 该方法利用在氯苯的N-酰胺化反应中存在无机碱的情况下由铜（I）盐和有机配体组成的催化体系的高效率，在这种情况下，廉价试剂也可用作溶剂; 在高温下，在大气压力或更高温度下的反应条件，产生良好收率的反应。

公开(公告)号：EP3368513A1

公开(公告)日：2018-09-05

申请号：EP16797465.8

申请日：2016-10-27

Applicant: Procos S.p.A.

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

IPC: C07D213/64

CPC classification number: C07D213/64

Abstract: 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.

公开(公告)号：EP3704116A1

公开(公告)日：2020-09-09

申请号：EP18800538.3

申请日：2018-10-30

Applicant: Procos S.p.A.

Inventor： DONNOLA, Monica ,  MOSSOTTI, Matteo ,  BARBERO, Mauro ,  ROLETTO, Jacopo ,  PAISSONI, Paolo

IPC: C07D453/02