Invention Grant
- Patent Title: Process for the synthesis of lofexidine
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Application No.: US17617598Application Date: 2020-06-19
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Publication No.: US11459303B2Publication Date: 2022-10-04
- Inventor: Monica Donnola , Alessandro Barozza , Jacopo Roletto , Paolo Paissoni
- Applicant: Procos S.P.A.
- Applicant Address: IT Cameri
- Assignee: Procos S.P.A.
- Current Assignee: Procos S.P.A.
- Current Assignee Address: IT Cameri
- Agency: Silvia Salvadori, P.C.
- Agent Silvia Salvadori
- Priority: IT102019000009777 20190621
- International Application: PCT/EP2020/067105 WO 20200619
- International Announcement: WO2020/254580 WO 20201224
- Main IPC: C07D233/22
- IPC: C07D233/22

Abstract:
Disclosed is a process for the synthesis of lofexidine of formula (I) and the hydrochloride salt thereof (II), from ethyl 2-(2,6-dichlorophenoxy)propionate (III) and ethylenediamine in the presence of tetravalent titanium alkoxides, preferably titanium isopropoxide, in an apolar solvent such as toluene. A further object of the present invention is a process for the preparation of the intermediate ethyl 2-(2,6-dichlorophenoxy)propionate (III) from 2,6-dichlorophenol and ethyl 2-chloropropionate in the presence of a polar aprotic solvent and an alkali or alkaline earth carbonate salt, preferably potassium carbonate. Both processes are more cost-effective and more easily industrially scalable than the known procedures, thus enabling the active ingredient to be obtained with high yields at a limited cost.
Public/Granted literature
- US20220204455A1 A PROCESS FOR THE SYNTHESIS OF LOFEXIDINE Public/Granted day:2022-06-30
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