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Compound for treating tumor

A technology of compound and solvate, which is applied in the field of drug synthesis, can solve the problems such as few complete cures, achieve excellent anti-tumor activity, excellent application prospects, and the effect of inhibiting new blood vessels

Active Publication Date: 2018-11-02
SICHUAN JINGHUA BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the treatment of cancer can be treated by traditional Chinese medicine, surgical resection, chemotherapy, radiotherapy, immunotherapy, monoclonal antibody therapy or other treatments, but there are few cases of complete cure

Method used

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  • Compound for treating tumor
  • Compound for treating tumor
  • Compound for treating tumor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] The synthesis of embodiment 1, compound 1

[0057] synthetic route:

[0058]

[0059] Preparation:

[0060] (1) Add compound a (10g, 1.0eq) and dichloromethane (100ml) into a three-necked flask, under nitrogen protection, cool down to -78°C, add boron tribromide (10eq) in dichloromethane solution (1g / 3ml). After the addition, keep the reaction for 1 hour, heat up to 25°C and react for 4-6 hours. After the reaction, wash with 10ml of water, dry with anhydrous sodium sulfate, concentrate the organic phase to dryness, and pass through a flash column to obtain 6.97g of compound b. The yield is: 80.5%.

[0061] (2) Compound b (5g, 1.0eq) and pyridine (50ml) were added to a three-necked flask, and under nitrogen protection, acetic anhydride (2.5eq) was added while the temperature was controlled below 20°C. After the addition is complete, heat the reaction for 1 hour, raise the temperature to 25°C and react for 4-6 hours. After the reaction, pour the reaction liquid in...

Embodiment 2

[0069] The synthesis of embodiment 2, compound 2

[0070]

[0071] The benzoyl chloride in step (7) of Example 1 is replaced by 2-fluorobenzoyl chloride, and the same preparation method as in Example 1 can be used to prepare compound 2, 1 H NMR (300MHz, CDCl 3 , 25°C, TMS): δ=2.13-2.38(m, 4H, CH2), 3.29-3.39(m, 4H, CH2), 4.0(s, 1H, NH), 6.79(s, 1H, CH), 7.16( s,1H,CH)7.24(s,1H,CH)7.29(s,1H,CH),7.40(s,1H,CH).7.41(s,1H,CH)7.42(s,1H,CH),8.00 (s, 1H, CH), 8.01 (s, 1H, CH) 8.49 (s, 1H, CH). Molecular formula: C 26 h 19 CIF 2 N 4 o 3 , relative molecular mass: 508.9.

Embodiment 3

[0072] The synthesis of embodiment 3, compound 3

[0073]

[0074] By replacing p-fluorobenzoyl chloride with benzoyl chloride in step (7) of Example 1, and using the same preparation method as in Example 1, compound 3 can be prepared, 1 H NMR (300MHz, CDCl 3 , 25°C, TMS): δ=2.13-2.38(m, 4H, CH2), 3.29-3.39(m, 4H, CH2), 4.0(s, 1H, NH), 6.79(s, 1H, CH), 7.16( s,1H,CH)7.24(s,1H,CH),7.29(s,1H,CH),7.41(s,1H,CH),7.42(s,2H,CH),.8.12(s,2H,CH ), 8.49 (s, 1H, CH). Molecular formula: C 26 h 19 CIF 2 N 4 o 3 , relative molecular mass: 508.9.

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Abstract

The invention discloses a compound as shown in the formula (I) in the description or pharmaceutically acceptable salt thereof or a solvate thereof, wherein R1 is selected from groups shown in the specification; R2 and R3 are independently selected from H, halogen, alkyl, the group as shown in the description respectively, or R2, R3 and carbon atoms to which R2 and R3 are attached constitute a 1-substituted or polysubstituted six-membered aromatic heterocyclic ring with 1 to 2 heteroatoms; R4, R5 and R6 respectively represent a 0 to 3 substitution on a benzene ring; R4, R5, and R6 are independently selected from the H, a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a hydroxy group, an amino group, a carboxy group, a nitro group, CH3O(CH2)nCH2O-, and a group as shown in the description respectively, where n is an integer of 1 to 6. The invention provides the use of the compound in preparing drugs for treating tumors. The compound provided by the invention is definite in pharmacological function.

Description

technical field [0001] The invention belongs to the field of drug synthesis, in particular to a compound for treating tumors. Background technique [0002] In recent years, with the acceleration of the pace of life, people's pressure has further increased. Schizophrenia and cancer have become diseases that cannot be ignored in today's society, seriously affecting the normal development of society and normal public order. Since the 20th century, the number of people infected with cancer has been increasing. Millions of patients die from cancer every year in the world, and most cancer patients are low-income and middle-income groups. At present, the treatment of cancer can be through traditional Chinese medicine treatment, surgical resection, chemotherapy, radiotherapy, immunotherapy, monoclonal antibody treatment or other treatment methods, but there are few cases of complete cure. How to minimize the pain of cancer patients and achieve good prevention and treatment effect...

Claims

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Application Information

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IPC IPC(8): C07D491/20C07D491/113A61P35/00
CPCA61P35/00C07D491/113C07D491/20
Inventor 杨佑喆庄明晨刘乾英郭鹏
Owner SICHUAN JINGHUA BIOTECH CO LTD
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