Method for preparing prostaglandin derivative

The technology of a compound and structural formula is applied in the field of synthesis of prostaglandin derivatives, which can solve the problems of small aortic effect and lower blood pressure.

Inactive Publication Date: 2011-05-11
沈阳万爱普利德医药科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] However, if a large amount of prostaglandin E1 is injected into blood vessels at one time, it acts not only in the peripheral peripheral circulation but also in the aorta, so there is a concern that blood pressure will be seriously lowered
To avoid this problem, prostaglandin E1 should be infused in controlled doses so that it acts in the peripheral peripheral circulation but to a lesser extent in the aorta

Method used

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  • Method for preparing prostaglandin derivative
  • Method for preparing prostaglandin derivative
  • Method for preparing prostaglandin derivative

Examples

Experimental program
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Effect test

Embodiment Construction

[0028] 1. Preparation of 10,12,12,12-tetrachlorododecanoic acid (IV):

[0029] Put 400g of undecylenic acid, 640ml of dry carbon tetrachloride and 20g of benzoyl peroxide into a 2000ml round bottom flask, and heat to reflux for 15 hours. After the reaction was completed, it was naturally cooled to room temperature and stirred for 6 hours. The remaining carbon tetrachloride was recovered, and the carbon tetrachloride was removed by rotary evaporation under reduced pressure below 30°C to obtain 690 g of a yellow oily product. The yield was 94.0%. It can be directly used in the next reaction without further purification.

[0030] 2, the preparation of 3-chlorododecanedioic acid (V):

[0031] Put 690g of 10,12,12,12-tetrachlorododecanoic acid into a 2000ml three-neck bottle, add 1017ml of fuming nitric acid dropwise at room temperature, and control the temperature at 25-30°C. There is a little yellow gas shrouded on it, and the dripping is completed in about 6 hours. At room ...

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Abstract

The invention relates to a method for preparing a compound with a structural formula (I). The compound with the formula (I) is a derivative of prostaglandin E1, and the chemical stability of the derivative is superior to that of the prostaglandin E1. The synthesis process disclosed by the invention is a complete synthesis method of the compound with the formula (I), and the method is simple and feasible.

Description

technical field [0001] The present invention relates to a synthetic method for producing a prostaglandin derivative. The compound is a prodrug of prostaglandin E1. [0002] Prostaglandin E1 is represented by the following structural formula: [0003] Background technique [0004] Since prostaglandin E1 has various physiological properties, especially blood pressure lowering, vasodilation, increased blood flow in blood vessels, and antiplatelet effects, it has been used in medicine. Clinically, it is mainly used to treat peripheral peripheral arterial occlusive disease, thrombosis anginetic obliterence, etc., to maintain blood flow after repairing vascular surgery, to maintain low blood pressure during surgery, and to be used as an anesthetic. [0005] However, the use of prostaglandin E1 to treat peripheral peripheral circulation diseases has the following two problems: [0006] (1) Prostaglandin E1 has many physiological properties. Therefore, if one biological activ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C405/00C12P9/00C12P31/00
CPCY02P20/55
Inventor 张青李淑斌
Owner 沈阳万爱普利德医药科技有限公司
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