A kind of complex of vitamin D and omeprazole and coupling method thereof

An omeprazole and vitamin technology, which is applied in the field of vitamin D and omeprazole complexes and their coupling, can solve problems such as the poor effect of vitamin D and omeprazole alone, and achieve anti-cancer ulcer healing, The effect of high yield and mild reaction conditions

Active Publication Date: 2017-12-26
CHANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved in the present invention is: to overcome the deficiency that independent effect of vitamin D and omeprazole alone is not good in the prior art, provide a kind of compound of vitamin D and omeprazole and coupling method thereof, further Application of a Novel Compound in the Preparation of Drugs for Anti-gastric Cancer and Healing of Gastric Ulcer

Method used

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  • A kind of complex of vitamin D and omeprazole and coupling method thereof
  • A kind of complex of vitamin D and omeprazole and coupling method thereof
  • A kind of complex of vitamin D and omeprazole and coupling method thereof

Examples

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Embodiment 1

[0028] Example 1 Vitamin D 3 Synthesis, purification and MTT cancer cell toxicity test of a novel drug complex coupled with omeprazole.

[0029] (1) Vitamin D 3 Synthesis of novel drug complex coupled with omeprazole, its synthetic route is as follows:

[0030]

[0031] Weigh 100mg (0.26mmol) vitamin D 3 Dissolve in 3ml of anhydrous dichloromethane solution, under N 2 Add 115mg (0.39mmol) of triphosgene (0.39mmol) and 54μL (0.39mmol) of triethylamine under ambient conditions, and stir the reaction at 0°C for 3-4h until the reaction is complete. The mixed solution is vacuum-dried for 0.5h and dissolved in 3ml of dichloromethane solution, N 2 Add 134mg (0.39mmol) omeprazole dichloromethane solution dropwise under ambient conditions, stir at 0°C for 3-5h, then react overnight at room temperature. Add 20ml NaHCO 3 aqueous solution, extracted three times with dichloromethane, washed with saturated brine, and then washed with anhydrous Na 2 SO 4 Dry, filter and concentrate...

Embodiment 2

[0056] Embodiment 2 Vitamin D 2 Synthesis, purification and MTT cancer cell activity test of a novel drug complex coupled with omeprazole.

[0057] (1) Vitamin D 2 Synthesis and purification of a novel drug complex coupled with omeprazole, the synthesis route is as follows:

[0058]

[0059] Weigh 200mg (0.504mmol) vitamin D 2 Dissolve in 5ml of anhydrous dichloromethane solution, under N 2 Add 115mg (0.756mmol) of triphosgene and 105μL (0.756mmol) of triethylamine under ambient conditions, and stir the reaction at 0°C for 3-4h until the reaction is complete. The mixed solution is vacuum-dried for 0.5h and dissolved in 5ml of dichloromethane solution, N 2 Add 260mg (0.756mmol) omeprazole dichloromethane solution dropwise under ambient conditions, stir at 0°C for 3-5h, then react overnight at room temperature. Add 30ml NaHCO 3 aqueous solution, extracted three times with dichloromethane, washed with saturated brine, and then washed with anhydrous Na 2 SO 4 Dry, filter...

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Abstract

The invention belongs to the filed of pharmaceutical chemistry, and relates to a novel drug composite obtained through a novel drug coupling connection method. Coupling is conducted on fat-soluble vitamin D and omeprazole which serves as a drug for treating gastropathy through triphosgene, on the basis that pharmaceutical activity is not damaged, drug stability detection and activity detection are conducted, and pharmaceutical activity research in gastric epithelial cells, caner cells and living animals can be further conducted; the functions of resisting cancer and facilitating gastric ulcer healing are achieved.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, relates to a novel drug coupling and connection method to obtain a novel drug compound, and specifically relates to the coupling of fat-soluble vitamin D and omeprazole, a drug for treating stomach diseases, through solid phosgene without damaging On the basis of drug activity, drug stability testing and activity testing can be carried out, so that it can be further used for drug activity research in gastric epithelial cells and cancer cells, as well as in vivo animals, and has the effect of anti-cancer and promoting gastric ulcer healing. Background technique [0002] With the improvement of people's living standards, the acceleration of the pace of life in modern society, the change of lifestyle, environmental pollution and many other factors, cancer has become the main killer of human health. In recent years, although great progress has been made in the diagnosis and treatment of tumors, ove...

Claims

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Application Information

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Patent Type & AuthorityPatents(China)
IPC IPC(8): C07D401/12A61P1/04A61P35/00A61P1/00
CPCC07D401/12
Inventor王建浩李进晨曹之宪李明星蒋鹏举邱琳
OwnerCHANGZHOU UNIV