公开(公告)号：US11286254B2

公开(公告)日：2022-03-29

申请号：US16760324

申请日：2018-10-30

Applicant: Procos S.P.A.

Inventor： Monica Donnola ,  Matteo Mossotti ,  Mauro Barbero ,  Jacopo Roletto ,  Paolo Paissoni

IPC: 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 phenyl-magnesium 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：US20220098170A1

公开(公告)日：2022-03-31

申请号：US17422865

申请日：2020-01-13

Applicant: Procos S.P.A.

Inventor： Giampiero Colombano ,  Mauro Barbero ,  Giovanni Battista Giovenzana ,  Jacopo Roletto ,  Paolo Paissoni

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：US20200339561A1

公开(公告)日：2020-10-29

申请号：US16760324

申请日：2018-10-30

Applicant: Procos S.P.A.

Inventor： Monica Donnola ,  Matteo Mossotti ,  Mauro Barbero ,  Jacopo Roletto ,  Paolo Paissoni

IPC: 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 phenyl-magnesium 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.