Invention Grant
US08501965B2 Method for producing 3-substituted-4-fluoropyrrolidine derivative
有权
3-取代-4-氟吡咯烷衍生物的制备方法
- Patent Title: Method for producing 3-substituted-4-fluoropyrrolidine derivative
- Patent Title (中): 3-取代-4-氟吡咯烷衍生物的制备方法
-
Application No.: US13700772Application Date: 2011-05-30
-
Publication No.: US08501965B2Publication Date: 2013-08-06
- Inventor: Masashi Suzuki , Muneki Nagao
- Applicant: Masashi Suzuki , Muneki Nagao
- Applicant Address: JP Tokyo
- Assignee: Kyorin Pharmaceutical Co., Ltd.
- Current Assignee: Kyorin Pharmaceutical Co., Ltd.
- Current Assignee Address: JP Tokyo
- Agency: Wenderoth, Lind & Ponack, L.L.P.
- Priority: JP2010-123889 20100531
- International Application: PCT/JP2011/062385 WO 20110530
- International Announcement: WO2011/152354 WO 20111208
- Main IPC: C07D207/04
- IPC: C07D207/04

Abstract:
An inexpensive and industrially advantageous method for producing optically active syn-3-(N-substituted-aminomethyl)-4-fluoropyrrolidine which may be an intermediate for producing pharmaceuticals is provided. The present invention relates a method for producing a syn-1-protected-4-fluoro-3-(N-substituted-N-nitrobenzenesulfonyl)pyrrolidine derivative or it's enantiomer, or their salts comprising the process of fluorinating a compound represented by the general formula (6) (in the formula, PG1 represents a protecting group for an amino group, R1 represents a C1 to C6 alkyl group which may be substituted or a C3 to C8 cycloalkyl group which may be substituted, and Ns represents a 2-nitrobenzenesulfonyl group or a 4-nitrobenzenesulfonyl group) or it's enantiomer using a nucleophilic fluorinating agent and an organic base having an amidine or guanidine structure.
Public/Granted literature
- US20130085282A1 METHOD FOR PRODUCING 3-SUBSTITUTED-4-FLUOROPYRROLIDINE DERIVATIVE Public/Granted day:2013-04-04
Information query