Invention Grant
US08946456B2 Process for the preparation of 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol and (R)-feso-deacyl
有权
制备2-羟基-4-苯基-3,4-二氢-2H-色烯-6-基 - 甲醇和(R) - 壬酰基
- Patent Title: Process for the preparation of 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol and (R)-feso-deacyl
- Patent Title (中): 制备2-羟基-4-苯基-3,4-二氢-2H-色烯-6-基 - 甲醇和(R) - 壬酰基
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Application No.: US13702403Application Date: 2011-04-29
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Publication No.: US08946456B2Publication Date: 2015-02-03
- Inventor: Umberto Ciambecchini , Stefano Turchetta , Lorenzo De Ferra , Maurizio Zenoni
- Applicant: Umberto Ciambecchini , Stefano Turchetta , Lorenzo De Ferra , Maurizio Zenoni
- Applicant Address: IT Cinisello Balsamo (MI)
- Assignee: Chemi S.p.A.
- Current Assignee: Chemi S.p.A.
- Current Assignee Address: IT Cinisello Balsamo (MI)
- Agency: Silvia Salvadori, P.C.
- Priority: ITMI2010A1047 20100610
- International Application: PCT/IB2011/051896 WO 20110429
- International Announcement: WO2011/154854 WO 20111215
- Main IPC: C07D311/20
- IPC: C07D311/20 ; C07C213/10 ; C07C213/00 ; C07C213/02 ; C07C215/54

Abstract:
The present invention regards an improved and industrially advantageous process for the preparation of the 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol intermediates, also called “feso chromenyl” and (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol, also called “(R)-feso deacyl”, which are in turn used in the synthesis of fesoterodine and in particular of fesoterodine fumarate. This process utilises reagents which are non-toxic and manageable at industrial level and enables obtaining a new stable and non-hygroscopic crystalline form of the key intermediate “(R)-feso deacyl”, called form B.
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