U.S. patents available from 1976 to present.
U.S. patent applications available from 2005 to present.

Process for preparing ethyl (S)-2-ethoxy-4-[N-[1-(2-piperidinophenyl)-3-methyl-1-butyl]aminocarbonyl methyl]benzoate and use thereof for the preparation of Repaglinide

Patent 8101769 Issued on January 24, 2012. Estimated Expiration Date: Icon_subject February 14, 2028. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

Phenylacetic acid benzylamides
Patent #: 5312924
Issued on: 05/17/1994
Inventor: Grell, et al.

Process for the preparation of repaglinide Patent #: 7148355
Issued on: 12/12/2006
Inventor: Ray, et al.

Inventors

Assignee

Application

No. 12031184 filed on 02/14/2008

US Classes:

546/234Plural carbocyclic rings containing

Examiners

Primary: Chang, Celia

Attorney, Agent or Firm

Foreign Patent References

  • 9300337 WO 01/01/1993
  • 03027072 WO 04/01/2003
  • 2004103983 WO 12/01/2004

International Class

C07D 211/22

Abstract

Described herein is an improved, commercially viable and industrially advantageous process for the preparation of Repaglinide intermediate, ethyl (S)-2-ethoxy-4-[N-(1-(2-piperidino-phenyl)-3-methyl-1-butyl)-aminocarbonylmethyl]-benzoate. The process provides the Repaglinide intermediate in higher yield and purity compared to the previously disclosed processes, thereby providing for production of Repaglinide and its pharmaceutically acceptable salts in high purity and in high yield.

Other References

  • International Search Report and Written Opinion; International Application No. PCT/IS2008/000825; International Filing Date Feb. 15, 2008; Date of Mailing Aug. 4, 2008; 13 pages.
  • Tang et al. “Boric acid . . . . . ” Organic syn. v.81p. 262-267 (2005).
  • Ray et al. “Industrial process . . . . . . ” CA138:287529 (2003).
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