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Methods of preparing pimecrolimus

A technology for pimecrolimus and ascomycin, which is applied in the field of pure pimecrolimus and can solve the problems of low total yield and the like

Inactive Publication Date: 2007-11-07
TEVA GYOGYSZERGYAR RESVENYTARSASAG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, the overall yield of the process disclosed in EP 427 680 may be expected to be low from the number of reaction steps and the number of chromatographic purifications required

Method used

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  • Methods of preparing pimecrolimus
  • Methods of preparing pimecrolimus

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Abstract

The present invention provides a process for the preparation of pimecrolimus from ascomycin in which ascomycin is reacted with a conversion reagent that converts ascomycin to its activated derivative at C-32. The activated ascomycin is then reacted with chloride ion. The process of the invention requires fewer process steps than prior art processes, and does not require the protection of the ascomycin C-24 hydroxyl group or the purification of the activated ascomycin derivative.

Description

[0001] related application [0001] This application claims the benefit of the following U.S. provisional patent applications: 60 / 632,372 filed December 1, 2004; 60 / 633,926 filed December 6, 2004; 60 / 641,697 filed January 5, 2005; 60 / 641,868 filed January 5, 60 / 641,869 filed January 5, 2005, 60 / 662,440 filed March 16, 2005, 60 / 705,681 filed August 3, 2005, and August 2005 60 / 709,160 filed on the 17th, the entire contents of which are hereby incorporated by reference in their entirety. field of invention [0002] The present invention relates to a process for the preparation of the anti-inflammatory compound pimecrolimus and to pure pimecrolimus. Background of the invention [0003] Pimecrolimus is an anti-inflammatory compound derived from the macrolide natural product ascomycin produced by certain strains of Streptomyces. Pimecrolimus is sold in the United States under the trade name ELTJDEL(R) and is approved for the treatment of atopic dermatitis. The systematic design...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D498/18A61K31/70C07H19/01A61P17/00A61K31/395
Inventor V·捷莱C·绍博
Owner TEVA GYOGYSZERGYAR RESVENYTARSASAG
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