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：WO2020148621A1

公开(公告)日：2020-07-23

申请号：PCT/IB2020/050218

申请日：2020-01-13

Applicant: PROCOS S.P.A.

Inventor： COLOMBANO, Giampiero ,  BARBERO, Mauro ,  GIOVENZANA, Giovanni B ,  ROLETTO, Jacopo ,  PAISSONI, Paolo

IPC: C07D401/12

Abstract: Disclosed is a process for the synthesis of gepirone of formula (I) from 8-(pyrimidin-2-yl)-5,8-diazaspiro[4,5]decan-5-ium bromide. The process according to the invention is economically efficient and easily industrially scalable.

公开(公告)号：WO2021023634A1

公开(公告)日：2021-02-11

申请号：PCT/EP2020/071581

申请日：2020-07-30

Applicant: PROCOS S.P.A.

Inventor： COLOMBANO, Giampiero ,  BARBERO, Mauro ,  BOGOGNA, Luigi ,  ROLETTO, Jacopo ,  PAISSONI, Paolo

IPC: C07D295/088 ,  C07D471/10

Abstract: Disclosed is a process for the synthesis of pitolisant HCl of formula (I), from piperidine and 1-bromo-3-chloropropane. The process according to the invention is economically efficient and easily industrially scalable.

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