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2-(Amino) methylquinazolin-4(3H)-one compound and preparation method and application thereof

A technology of methylquinazoline and ketone compounds, which can be used in organic chemistry, drug combination, and pharmaceutical formulation, etc., and can solve the problems of hypoglycemia drug efficacy reduction, weight gain, etc.

Inactive Publication Date: 2016-10-26
XIANGTAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Traditional hypoglycemic drugs mainly fall into three categories: insulin sensitizers, insulin secretagogues, and α-glucosidase inhibitors, and these drugs have some adverse reactions, mainly manifested in weight gain, hypoglycemia, and gradual decrease in drug efficacy, etc. , so there is an urgent need to develop new hypoglycemic drugs

Method used

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  • 2-(Amino) methylquinazolin-4(3H)-one compound and preparation method and application thereof
  • 2-(Amino) methylquinazolin-4(3H)-one compound and preparation method and application thereof
  • 2-(Amino) methylquinazolin-4(3H)-one compound and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0091] Example 1 Preparation of 2-(amino)methyl-6-fluoroquinazolin-4(3H)-one

[0092]

[0093] 1) Preparation of intermediate 5-fluoroisatoic anhydride

[0094]2-Amino-5-fluorobenzoic acid (13.30g, 85.73mmol) was dissolved in 100mL THF, pre-cooled for 0.5h, stirred in ice bath for 2h, and then bis(trichloromethyl)carbonate (12.72 g, 42.86mmol), sealed, continued to stir and react under ice bath for 1.5h, then transferred to 100°C oil bath to reflux for 6h. Concentrate the reaction solution with a rotary evaporator, add 150 mL of ether, and filter with suction. The filter cake was washed 4 times with THF-diethyl ether (1:10), and dried under vacuum to obtain 14.85 g of 5-fluoroisatoic anhydride as a white powder, with a yield of 95.62%. 1 H NMR (400MHz, DMSO-d 6 )δ(ppm):11.80(s,1H),7.66~7.63(m,2H),7.20~7.17(m,1H).MALDI-TOF-MS:m / z 182([M+H] + ).

[0095]

[0096] 2) Preparation of intermediate 2-amino-5-fluorobenzamide

[0097] Dissolve 5-fluoroisatoic anhydride (4.4...

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Abstract

The invention relates to 2-(amino) methylquinazolin-4(3H)-one compound, a preparation method of the compound and application of the compound as DPP-4 inhibitor. The compound can be used for treating diabetics, diabetic complications or other related diseases. The 2-(amino) methylquinazolin-4(3H)-one compound has a structure shown as in the following formula (I), or its salts, hydrates, solvates and stereoisomers are also disclosed.

Description

technical field [0001] The invention relates to a class of 2-(amino)methylquinazolin-4(3H)-one compounds and a preparation method thereof, as well as a DPP-4 inhibitor for the preparation of antidiabetic and other disease medicines. Background technique [0002] Diabetes mellitus is a chronic comprehensive disease mainly caused by the disorder of glucose metabolism caused by absolute or relative insulin deficiency or decreased sensitivity of target cells to insulin. There are 415 million diabetics in the world, that is, 1 in every 11 people has diabetes, and 318 million people in the world are at risk of developing diabetes. It is expected to reach 642 million people by 2040, an increase of more than 50% compared with the current data, and become the third largest non-communicable disease after cardiovascular and malignant tumors, seriously endangering human health and social development. Among them, type 2 patients account for 90% to 95% of the total number of diabetic pat...

Claims

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Application Information

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IPC IPC(8): C07D239/90A61K31/517A61P3/10A61P3/00A61P3/08A61P3/04A61P3/06A61P3/12A61P35/00A61P25/00A61P37/00
CPCC07D239/90
Inventor 彭圣明易立成邹晓青
Owner XIANGTAN UNIV
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