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2-pyridinemethanol copper complex and its preparation method and application

A technology of pyridinemethanol and copper complexes, which is applied in the direction of copper organic compounds, drug combinations, antineoplastic drugs, etc., can solve the problem that the anticancer activity of 2-pyridylmethanol has not been reported, and achieve low cost, high anticancer activity, Good fat solubility

Inactive Publication Date: 2016-03-09
LIAOCHENG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on the anticancer activity of copper compounds of 2-pyridinemethanol

Method used

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Experimental program
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Embodiment 1

[0017] 1mmolCu(OAc) 2 ·H 2 Dissolve O in a mixed solution of 10mL ethanol and 10mL acetonitrile, add 1.5mmol 2-pyridinemethanol under stirring, add 1mmol triethylamine after 15 minutes, add 0.5mmol sodium azide after 1 hour, and continue stirring at room temperature for 5-6 hours . Green crystals were obtained by solution cultivation. The melting point is 256°C, and the highest yield of this compound is 63.5%;

[0018] The copper complex of the present invention is analyzed by X-single crystal diffraction, and the crystallographic data are as follows: the complex belongs to the monoclinic crystal system, and the space group is P2 1 / c , the cell parameters are: a =10.1982(9)?, b =13.7631(13)?, c =14.6278(13)?, α =90°, β =104.8940(10)°, gamma =90°, V =1984.2(3)? 3 , Z =2, D =1.665Mg·m -3 , mu =2.189mm -1 , F(000) =1016, 2.54R 1 =0.0371, wxya 2 =0.0936.

Embodiment 2

[0020] 1.1mmolCu(OAc) 2 ·H 2 O was dissolved in a mixed solution of 10mL ethanol and 10mL acetonitrile, 1.65mmol 2-pyridinemethanol was added under stirring, 1.1mmol triethylamine was added after 15 minutes, 0.55mmol sodium azide was added after 1 hour, and stirring continued at room temperature for 5-6 Hour. Green crystals were obtained by solution cultivation. The melting point is 256°C, and the highest yield of this compound is 62.1%;

Embodiment 3

[0022] 1.2mmolCu(OAc) 2 ·H 2 O was dissolved in a mixed solution of 10mL ethanol and 10mL acetonitrile, 1.8mmol 2-pyridinemethanol was added under stirring, 1.2mmol triethylamine was added after 15 minutes, 0.6mmol sodium azide was added after 1 hour, and stirring continued at room temperature for 5-6 Hour. Green crystals were obtained by solution cultivation. The melting point is 256°C, and the highest yield of this compound is 62.3%;

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Abstract

The invention discloses a 2-pyridinemethanol copper compound and a preparation method thereof. Cu(OAc)2.H2O is dissolved in a mixed solution of ethanol and acetonitrile, 2-pyridinemethanol is added under stirring, triethylamine is added, and Sodium Nitrate, continue stirring at room temperature and culture with solution to obtain green crystals. The melting point is 256-258°C. The highest yield of this compound was 63.5%. The copper compound of the present invention has higher anticancer activity, and it can be used as a raw material to prepare medicines for treating human lung cancer and human colon cancer. Compared with platinum anticancer drugs commonly used at present, the copper complex of the present invention has higher anticancer activity. High fat solubility, low cost, simple preparation method and so on. It provides a new way for the development of anticancer drugs.

Description

technical field [0001] The invention belongs to the field of chemical synthesis, and in particular relates to a 2-pyridinemethanol copper complex, a preparation method and an application. Background technique [0002] Metal complexes have been widely used in the field of medicine in recent years, although their reaction mechanism is not fully understood (V.Milacic, D.Chen, L.Ronconi, K.R.Landis-Piwowar, D.Fregona, Q.P.Dou, CancerRes .2006;66:10478.). It is well known that the addition of metal ions can not only accelerate the action of drugs but also improve the effectiveness of organic ligands (Z.A.Siddiqi, M.Khalid, S.Kumar, M.Shahid, S.Noor, Eur.J.Med.Chem.2010 ;45:264.). In 1912, Germany used a mixture of copper chloride and lecithin to treat patients with facial cancer. The success of this treatment suggests that copper compounds have anticancer properties. In conclusion, the necessity of copper in living organisms and its anticancer activity attracted us to synthes...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F1/08A61P35/00
Inventor 吕红美李大成窦建民
Owner LIAOCHENG UNIV
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