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Quinazoline derivative used for cardio cerebrovascular diseases

A technology of compounds and hydrates, applied in the field of quinazoline derivatives such as terazosin, preparation of drugs for cardiovascular and cerebrovascular diseases, and new pharmaceutical applications of quinazoline derivatives, which can solve heavy economic burdens and patients and family issues

Inactive Publication Date: 2014-04-23
刘磊 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition to the blow to patients and families, it also creates a heavy financial burden

Method used

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  • Quinazoline derivative used for cardio cerebrovascular diseases
  • Quinazoline derivative used for cardio cerebrovascular diseases
  • Quinazoline derivative used for cardio cerebrovascular diseases

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0081] Preparation Example 1: Preparation of Co.1

[0082]

[0083] Step 1: Bubble ammonia gas into a solution of compound 1a (50 mmol) in 200 mL THF, and react at 25°C for 36 hours. A large amount of white solids were precipitated in the system, and the resulting white solids were filtered and washed with tetrahydrofuran to obtain the final product 1f. Yield: 63%.

[0084]

[0085] Step 2: 15 mL of acetic anhydride was added to compound 1f (10 mmol), and the reaction was refluxed for 2 hours. After cooling to room temperature, a large amount of white solids were precipitated in the system. The resulting white solids were filtered and washed with tetrahydrofuran to obtain 1 g of the final product. Yield: 63%.

[0086]

[0087] Step 3: To a solution of 1 g (2 mmol) of 1-pentanol was added under argon atmosphere for 1 h (2 mmol). After the reaction system was refluxed for 4.5 hours, it was placed in an environment of 0-5° C. for static crystallization. The obtained...

preparation example 2

[0088] Preparation Example 2: Preparation of Co.2

[0089]

[0090] Step 1: Compound 1b (20 mmol) was added to compound 1a (20 mmol) in 100 mL of methanol solution, and the reaction was carried out at 25° C. for 4 hours. Thin plate chromatography indicated that 1a was completely converted, and 100 mL of diethyl ether was added to the system, mixed evenly, and placed in a -20°C environment for static crystallization. The resulting white solid was recrystallized from petroleum ether / ethyl acetate to obtain the final product 1c. Yield: 41%.

[0091]

[0092] Step 2: To a solution of 1c (2 mmol) in 1-pentanol was added 1d (2 mmol) under argon atmosphere. After the reaction system was refluxed for 4.5 hours, it was placed in an environment of 0-5° C. for static crystallization. The obtained white crystals were washed twice with 10 mL of acetone, and then recrystallized with ether / methanol to obtain the final product 1e, which was compound Co.2. Yield: 62%. 1H NMR (300MHz...

preparation example 3

[0093] Preparation Example 3: Preparation of Co.3

[0094]

[0095] Step 1: Add hydrazine hydrate (20 mmol) to a solution of compound 1a (20 mmol) in 100 mL of methanol, and react at 25° C. for 4 hours. Thin plate chromatography indicated that 1a was completely converted, and 100 mL of diethyl ether was added to the system, mixed evenly, and placed in a -20°C environment for static crystallization. The obtained white solid was recrystallized from petroleum ether / ethyl acetate to obtain the final product 3a. Yield: 61%.

[0096]

[0097] Step 2: To a solution of 3a (2 mmol) in 1-pentanol was added 1d (2 mmol) under argon atmosphere. After the reaction system was refluxed for 4.5 hours, it was placed in an environment of 0-5° C. for static crystallization. The obtained white crystals were washed twice with 10 mL of acetone, and then recrystallized with ether / methanol to obtain the final product 3b, which is compound Co.3. Yield: 31%. 1H NMR(300MHz,DMSO-d6):d1.87(m,2H,...

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Abstract

The invention relates to a quinazoline derivative used for cardio cerebrovascular diseases, and particularly relates to a compound shown as a formula I, or a pharmaceutically acceptable salt, a solvate such as a hydrate, an ester and a prodrug of the compound, wherein substituents are as defined in the specification. The invention also relates to the use of the compound in preparation of drugs for preventing and / or treating cerebrovascular diseases of a mammal (such as people), as well as the use of the compound in preparation of drugs for preventing and / or treating cardiovascular diseases or heart diseases of the mammal (such as people). The compound disclosed by the invention can be advantageously used for cerebral vascular diseases including but not limited to, cerebral thrombosis, cerebral ischemia, cerebral infarction and the like, as well as for cardiovascular diseases including but not limited to, myocardial infarction, myocardial ischemia, myocardial injury, coronary heart disease, angina, heart failure and the like.

Description

technical field [0001] The present invention relates to a class of quinazoline derivatives that can be used for cardiovascular and cerebrovascular diseases, and also relates to new pharmaceutical applications of quinazoline derivatives, in particular to the preparation of quinazoline derivatives such as terazosin for cardiovascular and cerebrovascular diseases. Use in medicine for disease. Background technique [0002] Cardiovascular and cerebrovascular diseases are one of the most extensive diseases affecting human health. Typical cerebrovascular diseases such as cerebral thrombosis, cerebral ischemia, and cerebral infarction, as well as cardiovascular diseases such as myocardial infarction, myocardial ischemia, coronary heart disease, angina pectoris, and heart failure. [0003] Cerebral thrombosis refers to blockage of blood vessels in the brain due to various reasons, resulting in cerebrovascular dysfunction and related symptoms. Due to severe stenosis or occlusion of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/12C07D491/056C07D471/04A61K31/517A61K31/519A61P7/02A61P9/10A61P9/00A61P9/04
CPCC07D405/12C07D471/04C07D491/056A61P7/02A61P9/00A61P9/04A61P9/10
Inventor 刘磊李笑宇官清华
Owner 刘磊
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