Title:
PIPERIDINE DERIVATIVE AND PROCESS FOR PRODUCING THE SAME
Document Type and Number:
WIPO Patent Application WO/2006/062063
Kind Code:
A1
Abstract:
A piperidine derivative represented by the formula (I) or a salt thereof is used as an intermediate. Due to this, a 2-cyano-4-fluoropyrrolidine derivative useful as a medicine, especially a DPP-IV inhibitor, can be efficiently produced. In particular, use of the intermediate enables the target compound to be produced through a smaller total number of steps than in conventional processes and improves the overall yield. The 2-cyano-4-fluoropyrrolidine derivative can be produced without using an ultralow-temperature reaction or a reaction necessitating strict control of water in the reaction system, which are unsuitable for industrial production. (I) [In the formula, Ms represents methanesulfonyl, Me represents methyl, and R1 represents -H, halogeno, or -OH.]
Inventors:
SUGIMORI TOSHIYUKI (JP)
SANO KUNIYUKI (JP)
KOMENOI KOUSUKE (JP)
SANO KUNIYUKI (JP)
KOMENOI KOUSUKE (JP)
Application Number:
PCT/JP2005/022299
Publication Date:
June 15, 2006
Filing Date:
December 05, 2005
Export Citation:
Assignee:
ASTELLAS PHARMA INC (JP)
SUGIMORI TOSHIYUKI (JP)
SANO KUNIYUKI (JP)
KOMENOI KOUSUKE (JP)
SUGIMORI TOSHIYUKI (JP)
SANO KUNIYUKI (JP)
KOMENOI KOUSUKE (JP)
International Classes:
C07D211/58; A61K31/454; A61P3/04; A61P3/10; A61P43/00; C07D401/12
Domestic Patent References:
| WO2004009544A1 | 2004-01-29 |
Foreign References:
| JPH07165754A | 1995-06-27 | |||
| JPH10237071A | 1998-09-08 |
Other References:
GREENE T W AND WUTS P G M.: "Protective groups in organic synthesis.", 1991, JOHN WILEY & SONS, INC, pages: 382, XP002995757
MICOVIC I V.: "The Synthesis and preliminary pharmacological evaluation of 4-Methyl fentanyl.", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS., vol. 10, no. 17, September 2000 (2000-09-01), pages 2011 - 2014, XP004214158
MICOVIC I V.: "The Synthesis and preliminary pharmacological evaluation of 4-Methyl fentanyl.", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS., vol. 10, no. 17, September 2000 (2000-09-01), pages 2011 - 2014, XP004214158
Attorney, Agent or Firm:
Morita, Hiroshi c/o Astellas Pharma Inc. (Intellectual Property 3-11, Nihonbashi-Honcho 2-chom, Chuo-ku Tokyo 11, JP)
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