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A simple and efficient method for synthesizing dinoprost

A dinoprost, high-efficiency technology, applied in the field of pharmaceutical preparation, can solve the problems of high cost, complicated operation, long steps, etc., and achieve the effect of increased reaction yield and simple operation

Active Publication Date: 2018-11-20
厦门欧瑞捷生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, it has many disadvantages: long steps, low yield and high cost; at the same time, intermediate purification methods and impurity control are also barriers to industrialization.
[0006] Chinese patent application-"Synthetic method of trometamol prostaglandin F2α" (public date: June 9, 2017) involves the synthesis and preparation of prostaglandin F2α. When this preparation method is used to prepare prostaglandin F2α, the yield is low. Complicated operation

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  • A simple and efficient method for synthesizing dinoprost
  • A simple and efficient method for synthesizing dinoprost
  • A simple and efficient method for synthesizing dinoprost

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Embodiment

[0060] The specific synthesis steps are as figure 1 Shown:

[0061] Step (1) Preparation of Compound I

[0062] In a 10L three-necked flask equipped with a constant pressure dropping funnel, a thermometer and a mechanical stirrer, respectively add Corinolidediol (500g, 2.907mol), DMN-AZADO (4.93g, 0.02907mol), and potassium bromide KBr (34.59). g, 0.2907mol), n-Bu4NBr (47.8g, 0.1454mol), dichloromethane (5L) and saturated sodium bicarbonate solution (400mL); then use an ice-salt bath for the above-mentioned mixed system, and cool to an internal temperature ≤0℃ , And stir at constant temperature for 10 min; then slowly add NaClO (3.4884 mol, used as oxidant) solution to the reaction system dropwise to control the reaction temperature not to be higher than 5°C; after the dropwise addition, stir at constant temperature for 30 minutes. After the reaction, add saturated Na to the system 2 S 2 O 3 (Neutralize excess oxidant) (1000 mL) The reaction was quenched, and the aqueous phase was...

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Abstract

The invention provides a method for simply and efficiently synthesizing dinoprost. The method comprises synthesis steps as follows: L-corey lactone diol is selectively oxidized to aldehyde-containingcorey lactone monols, namely, a compound I; the compound I and dimethyl(2-oxoheptyl)phosphonate are subjected to a Honel-Wadsworth-Emmons reaction, and a reactive product compound II is produced; lactone is reduced to alcohol, and an intermediate, namely, a compound III, is obtained; the intermediate III selectively oxidizes primary alcohol, and an intermediate, namely, a compound IV, is obtained;the compound IV is subjected to a Witting reaction, and the dinoprost is produced. According to the method for simply and efficiently synthesizing dinoprost, raw materials are simple and easy to obtain, and equipment requirements are simple; the steps are short, and industrial production is easy to realize; no heavy metals or other strong carcinogens are used in the whole process; an intermediatepurification method is simple and impurities are easy to control.

Description

Technical field [0001] The present invention relates to the field of medical preparation, in particular to a method for synthesizing dinoprost simply and efficiently. Background technique [0002] Prostaglandins (PGs for short) are a class of important endogenous products with extensive physiological activities. PGs were first discovered and named by American scholar Von Eluer in 1930. In 1962, Bergstorm extracted two pure PGs (PGFl and PGF2.) and determined their chemical structures. In 1969 Willis first proposed that PGs are an inflammatory mediator in the body. Subsequently, various physiological and pharmacological activities of PGs have been studied in depth. It exists in almost all mammalian tissues and plays an important role in the reproductive system, digestive system, respiratory system, and cardiovascular system. It participates in thermoregulation, inflammation, glaucoma, pregnancy, hypertension, ulcers, asthma and other physiological pathologies. process. The str...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C405/00
CPCC07B2200/07C07C29/147C07C405/00C07D307/935C07C35/06
Inventor 郑飞剑张江平赵欢张立军王萍陈思涵赖育来吴进泉
Owner 厦门欧瑞捷生物科技有限公司