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2- normal-butyl-5-substituted amino benzofuran and preparation method thereof

A technology represented by tert-butoxycarbonyl, applied in the field of key intermediates of dronedarone and its preparation

Active Publication Date: 2010-09-22
AVENTIS PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Formula Ⅰ

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  • 2- normal-butyl-5-substituted amino benzofuran and preparation method thereof
  • 2- normal-butyl-5-substituted amino benzofuran and preparation method thereof
  • 2- normal-butyl-5-substituted amino benzofuran and preparation method thereof

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Abstract

The invention discloses an important intermediate of dronedarone, which relates to a dronedarone intermediate shown by a formula I, wherein R is phenylmethoxycarbonyl, or tert-butoxycarbonyl or 9-fluorenylmethoxycarbonyl.

Description

technical field The present invention relates to a key intermediate of dronedarone represented by formula I and a preparation method thereof. Background technique Dronedarone (dronedarone), the chemical name is N-[2-n-butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]-5-benzofuryl] Methylsulfonamide, developed by Sanofi-Aventis of France, can be used to treat atrial fibrillation / flutter. In July 2009, it was approved for marketing by the US Food and Drug Administration (FDA). dronedarone Atrial fibrillation is a complex disease that can increase the risk of stroke by 5 times, worsen the prognosis and triple the mortality rate of patients with cardiovascular risk factors. Atrial flutter is another type of atrial arrhythmia that occurs less frequently but may develop into atrial fibrillation. In the United States, atrial fibrillation is the leading cause of hospitalizations for arrhythmias, and the number of hospitalizations due to atrial fibrillation in the United States ...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/79
Inventor 陈安平刘迎春张志强
Owner AVENTIS PHARMA HAINAN
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