Novel process for the preparation of vorinostat

A vorinostat, stand-alone technology for the preparation of active pharmaceutical ingredients vorinostat that addresses issues that limit the feasibility of commercial production scale, reduce overall yield, etc.

Inactive Publication Date: 2011-01-05
GENERICS UK LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This reduces the overall yield and severely limits the viability of the method for commercial production scale

Method used

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  • Novel process for the preparation of vorinostat
  • Novel process for the preparation of vorinostat
  • Novel process for the preparation of vorinostat

Examples

Experimental program
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Embodiment

[0079] Vorinostat

[0080]Suberic acid (1.0 eq) was dissolved in tetrahydrofuran (15 vol), and the clear solution was cooled to 0-5°C. Methyl chloroformate (1.1 eq) and triethylamine (1.1 eq) were added to the solution at the same temperature and the mixture was stirred for 15 minutes. The formed triethylamine hydrochloride was filtered off, then aniline (1 eq) was added to the reaction mixture at 0-5°C and stirring was continued for 15 minutes. Methyl chloroformate (1.1 eq) and triethylamine (1.1 eq) were added to the clear solution and stirring was continued for a further 15 minutes at 0-5°C. The cooled reaction mixture was added to fresh methanolic solution of hydroxylamine (*see below) cooled to 0-5°C and stirred at 0-5°C for 15 minutes. The solvent was removed under vacuum at 40°C, the obtained residue was taken up in dichloromethane and the organic solution was washed with water and dried over anhydrous sodium sulfate. The dichloromethane was removed under vacuum at 4...

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PUM

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Abstract

The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient, vorinostat. In particular it relates to an efficient process for the preparation of vorinostat of high purity without the requirement to isolate any synthetic intermediate compounds.

Description

technical field [0001] The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient vorinostat. In particular it relates to an efficient process for the preparation of high-purity vorinostat without isolating any synthetic intermediate compounds. Background technique [0002] Vorinostat, also known as suberoylanilide hydroxamic acid (SAHA) or N-hydroxy-N'-phenylsuberamide, is represented by structural formula (I). [0003] [0004] Vorinostat is a histone deacetylase (HDAC) inhibitor currently marketed for the treatment of cutaneous T-cell lymphoma (CTCL), a type of skin cancer. Since vorinostat is considered to be able to selectively induce late differentiation of tumor cells and thereby inhibit the proliferation of such cells under suitable conditions, vorinostat is used for the treatment of patients with tumors characterized by continuous proliferation of tumor cells. tumor patients. [0005] Processes for the prep...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C259/06A61K31/167
CPCC07C259/06A61P35/00
Inventor 阿沛·盖顿德巴拉蒂·乔杜里
Owner GENERICS UK LTD
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