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Propofol ester derivative containing amino carboxylic acid amide structure, its preparation method and its purpose

A technology of aminocarboxylic acid amide and propofol, which is applied to the preparation of carboxylic acid amide, the preparation of organic compounds, and medical preparations containing active ingredients, etc. It can solve the problems of poor water solubility, achieve stable aqueous solution, and have cheap and easy-to-obtain raw materials , reducing the effect of the first-pass effect

Active Publication Date: 2015-01-21
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The propofol ester derivatives can overcome the disadvantage of poor water solubility of propofol, and after entering the body, except propofol can be released quickly, the rest of the released components are mostly endogenous nutrients of the human body without obvious toxicity

Method used

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  • Propofol ester derivative containing amino carboxylic acid amide structure, its preparation method and its purpose
  • Propofol ester derivative containing amino carboxylic acid amide structure, its preparation method and its purpose
  • Propofol ester derivative containing amino carboxylic acid amide structure, its preparation method and its purpose

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Solk the 20 G propyphenol (type Ⅱ) in 50 mL triamine, add 14 G amber acidic anhydride and 0.02 G ditrobyl pyridine, stir at room temperature for 16 h, remove the reactor decompression distillation and remove excessive triamines with excessive amounts of totoramine, Remnant into 100 ml of water, adjust the pH value of 6 n n N nn nnid hydrochloric acid to 1, and precipitate a large amount of white precipitation.Acetate ethyl acetic crystals obtained a needle-shaped crystal 23.5 g, the reaction production rate was 75.4%, and MP: 103-104 ° C.

Embodiment 2

[0041] Solk the 20 G propyphenols in 100 ml of dichloromethane, add 13.3 g -b -t -t -t -methalic acid and 0.02 g di metrophic pyridine, then add 23.2 G DCC to the room temperature for 6 h, and then filter out the white solid in the reaction solution., Wash the filtrate with 150 ml 6N hydrochloric acid once, separate the organic layer, reduce the stamina and steam the solvent, obtain the light yellow solid of the propyel picoline monoclodine (Ⅲ).The white needle-shaped crystal is 26.6 g, the yield is 85%, MP: 102-103 ° C.

Embodiment 3

[0043] Called 1 g of proper phenols (Ⅲ), a propylene phenolic acid single ester (Ⅲ) in 25 mL mono bottle, add 10 ml of dry dichloroblyne, and quickly add 2 G new steamed strawlllchriumThe atmosphere reacts at the room temperature by 2 h. After the HCL is released, it is steamed to dry the solvent and low volatile substances on the rotary evaporator, that is, the propylene phenol ambercotate is single -chloride, and it is directly used.

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Abstract

The invention relates to a propofol ester derivative containing an amino carboxylic acid amide structure, its preparation method and its purpose. The derivative has a following formula (I), in the formula, M is H, NH4 or pharmaceutically acceptable alkali metal element or alkali earth metal element, n=1-3, m=1-7, x=1 / 2-1. 2,6-diisopropyl phenol (II) is taken as a raw material, reacted with diacid or the corresponding anhydride to obtain a 2,6-diisopropyl phenol monoester intermediate, and continuously reacted with amino carboxylic acid to obtain the corresponding product (I). The propofol ester derivative can be used for preparing injection type central inhibition medicaments for generating effects of calmness, hypnosis and / or anaesthesia on animals and human, and is capable of improving the water-solubility of propofol, reducing the toxic and side effects of original drug and analogous prodrug, increasing the stability of profrug in vitro and increasing the application scope. The preparation method is simple which has industrial application value.

Description

Technical field [0001] The present invention involves a derivative of a 2,6-diopropyl phenol (propyphenol) and its preparation methods, as well as injection central inhibitory drugs that can produce sedatives and / or anesthesia that can produce animals / people.The purpose. Background technique [0002] Propofol (chemical name: 2,6-binary propionine) is currently widely used in drugs that are widely used in systemic anesthesia induction, maintenance, and ICU sedation.It has the characteristics of fast results, fast metabolism, and light anesthesia. Since the first clinical report was made in 1977, it has gradually been promoted and applied worldwide.Because the solubility of propyphenols in water is only 146mg / L in water, the preparations that are still widely used in clinical clinical clinical in the world are 1%propyphenol, 10%soybean oil, 2.25%glycerin and 1.2%refined egg yolk lecithinPreparation of O / W emulsion.0.005%of sodium in the United States is also added as inhibitors for...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C233/47C07C231/02A61K31/222A61P25/20A61P23/00
Inventor 郑虎翁玲玲刘进张文胜杨俊
Owner SICHUAN UNIV
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