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Novel butadiene derivatives, process for preparation of the same and intermediates for the synthesis thereof

A technology of butadiene and derivatives, which is applied in the field of new butadiene derivatives, can solve problems such as not being clearly disclosed, and achieve high safety, low toxicity, and significant toxicity

Inactive Publication Date: 2004-08-18
MITSUBISHI TANABE PHARMA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] WO97 / 36864 discloses (1Z,3E)-1-methyl-1-(3,5-dimethoxyphenyl)-2-methoxycarbonyl-3-[N-(4-pyridyl)aminocarbonyl] -4-(3,4-methylenedioxyphenyl)-butadiene, (1Z,3E)-1-methyl-1-(3,4,5-trimethoxyphenyl)-2-methyl Oxycarbonyl-3-[N-(4-pyridyl)aminocarbonyl]-4-(3,4-methylenedioxyphenyl)butadiene, etc.; Compounds containing a carboxyl group on the benzene ring at the -position or compounds containing a 2-lower alkyl-pyridyl substituent on the carbamoyl group at the 3-position of butadiene, and these compounds will be disclosed in the patent application

Method used

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  • Novel butadiene derivatives, process for preparation of the same and intermediates for the synthesis thereof
  • Novel butadiene derivatives, process for preparation of the same and intermediates for the synthesis thereof
  • Novel butadiene derivatives, process for preparation of the same and intermediates for the synthesis thereof

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Embodiment 1

[0071] (1) Suspend 4-acetylbenzoic acid (100 g) in 500 ml of dichloromethane. To the suspension were added 64 ml of oxalyl chloride and 4.7 ml of N,N-dimethylformamide at room temperature, and the mixture was stirred at room temperature for 2 hours. The reaction solution was concentrated under reduced pressure, and the residue was dissolved by adding 250 ml of chloroform and 175 ml of tert-butanol. 156 ml of pyridine were then added dropwise to the solution under ice-cooling (12°C). The reaction mixture was stirred at room temperature for 30 minutes and concentrated under reduced pressure. The residue was dissolved in toluene, and the solution was washed successively with 2M hydrochloric acid, saturated aqueous sodium bicarbonate and brine. The organic layer was dried over sodium sulfate and concentrated under reduced pressure. Hexane was added to the residue, and the mixture was stirred under ice-cooling. The precipitated crystals were collected by filtration, washed with...

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Abstract

A butadiene derivative having an excellent inhibitory activity on the PAI-1, which is represented by the general formula [I]: wherein R<1 >is a hydrogen atom or a lower alkyl group, R<2 >is a lower alkyl group, R<3 >is a lower alkoxy group, R<4 >is a hydrogen atom or a lower alkyl group, R<5 >is a lower alkyl group, or a pharmaceutically acceptable salt thereof, a process a process for preparing the same and an intermediate thereof.

Description

technical field [0001] The present invention relates to a novel butadiene derivative, a method for preparing it and an intermediate for synthesizing it. technical background [0002] Fibrinolysis (fibrinolytic system) plays an important role in activities such as thrombus dissolution, tissue destruction and repair, and cell migration in a living body. Fibrinolysis is activated when plasminogen is converted to plasmin by plasminogen activator (PA). Type I plasminogen activator inhibitor (PAI-1) controls fibrinolysis in the initial stage, and according to analysis, it is involved in the formation and development of various pathologies, such as thrombosis, diabetes, and arteriosclerosis. Therefore, compounds capable of inhibiting the production of PAI-1 are useful for the treatment or prevention of thrombosis, diabetic complications, arteriosclerosis, and the like. [0003] On the other hand, EP-A-563798 discloses (1E,3E)-1-(3,4,5-trimethoxyphenyl)-2-methoxycarbonyl-3-[N-(4-p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P7/02A61P9/10A61P29/00A61P31/04A61P35/04A61P37/06A61P43/00C07C63/66C07C69/76C07C69/94C07D213/75
CPCC07C63/66C07C69/76C07C69/94C07D213/75A61P7/02A61P9/10A61P29/00A61P31/04A61P35/04A61P37/06A61P43/00
Inventor 大谷章雄大菊钢山田泰弘
Owner MITSUBISHI TANABE PHARMA CORP
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