Title:
PROCESS FOR PREPARING ALPHA-CARBOXAMIDE PYROLIDINE DERIVATIVES
Document Type and Number:
WIPO Patent Application WO/2019/071162
Kind Code:
A3
Abstract:
The invention relates to a novel process for preparing a-carboxamide pyrrolidine derivatives, in particular (2S, 5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxamide, and to novel intermediates for use in said process along with processes for preparing said intermediates.
Inventors:
CHEN WEIRONG (US)
COUMING VINNY (US)
IRDAM ERWIN (US)
KIESMAN WILLIAM (US)
KWOK DAW-LONG (US)
MACK TAMERA (US)
OPALKA SUZANNE (US)
PATIENCE DANIEL (US)
WALKER DONALD (US)
LIANG WENLI (US)
COUMING VINNY (US)
IRDAM ERWIN (US)
KIESMAN WILLIAM (US)
KWOK DAW-LONG (US)
MACK TAMERA (US)
OPALKA SUZANNE (US)
PATIENCE DANIEL (US)
WALKER DONALD (US)
LIANG WENLI (US)
Application Number:
PCT/US2018/054661
Publication Date:
March 26, 2020
Filing Date:
October 05, 2018
Export Citation:
Assignee:
BIOGEN INC (US)
International Classes:
A61K31/401; C07D207/16
Domestic Patent References:
| WO2016102967A1 | 2016-06-30 | |||
| WO2012063252A2 | 2012-05-18 |
Foreign References:
| US4981996A | 1991-01-01 |
Other References:
XU ET AL.: "Asymmetric Synthesis of cis-2,5-disubsituted pyrrolidine, the core scaffold of b3- AR agonists", ORGANIC LETTERS, vol. 15, no. 6, 15 March 2013 (2013-03-15), pages 1342 - 1345, XP055172096, ISSN: 1523-7060, DOI: 10.1021/ol400252p
MURRAY ET AL.: "Continuous Flow-Processing of Organometallic Reagents Using an Advanced Peristaltic Pumping System and the Telescoped Flow Synthesis of (E/Z).Tamoxifen", ORGANIC PROCESS RESEARCH AND DEVELOPMENT, vol. 17, no. 9, 15 August 2013 (2013-08-15), pages 1192 - 1208, XP055695268, ISSN: 1083-6160, DOI: 10.1021/op4001548
FINELLI ET AL.: "Expanding the Toolbox of Asymmetric Organocatalysis by Continuous-flow Process", CHEMICAL COMMUNICATIONS, vol. 51, no. 18, 1 January 2015 (2015-01-01), pages 3708 - 3722, XP055695276, ISSN: 1359-7345, DOI: 10.1039/C4CC08748H
ANGELINI ET AL.: "Multistep Flow Procedure for the Waste-Minimized Preparation of N-Boc-beta -Amino Ketones", JOURNAL OF FLOW CHEMISTRY, vol. 41, no. 1, 23 March 2015 (2015-03-23), pages 40 - 43, XP055695281, ISSN: 2062-249X, DOI: 10.1556/JFC-D-13-00027
DA CHAO-SHAN ET AL.: "Highly Catalytic Asymmetric Addition of Deactivated Alkyl Grignard Reagents to Aldehydes", ORGANIC LETTERS, vol. 11, no. 24, 12 November 2009 (2009-11-12), pages 5578 - 5581, XP055695286, ISSN: 1523-7060, DOI: 10.1021/ol9020942
MURRAY ET AL.: "Continuous Flow-Processing of Organometallic Reagents Using an Advanced Peristaltic Pumping System and the Telescoped Flow Synthesis of (E/Z).Tamoxifen", ORGANIC PROCESS RESEARCH AND DEVELOPMENT, vol. 17, no. 9, 15 August 2013 (2013-08-15), pages 1192 - 1208, XP055695268, ISSN: 1083-6160, DOI: 10.1021/op4001548
FINELLI ET AL.: "Expanding the Toolbox of Asymmetric Organocatalysis by Continuous-flow Process", CHEMICAL COMMUNICATIONS, vol. 51, no. 18, 1 January 2015 (2015-01-01), pages 3708 - 3722, XP055695276, ISSN: 1359-7345, DOI: 10.1039/C4CC08748H
ANGELINI ET AL.: "Multistep Flow Procedure for the Waste-Minimized Preparation of N-Boc-beta -Amino Ketones", JOURNAL OF FLOW CHEMISTRY, vol. 41, no. 1, 23 March 2015 (2015-03-23), pages 40 - 43, XP055695281, ISSN: 2062-249X, DOI: 10.1556/JFC-D-13-00027
DA CHAO-SHAN ET AL.: "Highly Catalytic Asymmetric Addition of Deactivated Alkyl Grignard Reagents to Aldehydes", ORGANIC LETTERS, vol. 11, no. 24, 12 November 2009 (2009-11-12), pages 5578 - 5581, XP055695286, ISSN: 1523-7060, DOI: 10.1021/ol9020942
Attorney, Agent or Firm:
HALSTEAD, David, P. et al. (US)
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