Quinazolinone vasoinhibitors, and preparation method and medical application thereof

A pharmaceutical and compound technology, applied in the field of quinazolinone vascular inhibitors, can solve the problem of tumor blood vessels being sensitive to drugs and vulnerable to damage

Inactive Publication Date: 2013-01-16
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, tumor blood vessels are more sens

Method used

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  • Quinazolinone vasoinhibitors, and preparation method and medical application thereof
  • Quinazolinone vasoinhibitors, and preparation method and medical application thereof
  • Quinazolinone vasoinhibitors, and preparation method and medical application thereof

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specific Embodiment approach

[0050] The specific embodiment (described embodiment is only used to illustrate the present invention, is not used to limit the present invention)

Embodiment 1

[0054] Preparation of 3-methoxy-4-benzyloxybenzaldehyde (2)

[0055] Dissolve 3-methoxy-4-hydroxybenzaldehyde 1 (10g, 65.8mmol) in 120mL ethanol, add K 2 CO 3 (11.8g, 85.5mmol), benzyl chloride (11.4mL, 98.7mmol), reflux for 5 hours. The reaction solution was filtered to remove the filter residue, concentrated to dryness, and the crude product was recrystallized from ethanol to obtain a white solid 2 (13.6 g, 85.5%). m.p.56-57℃ (literature m.p.59℃); EI-MSm / z: 242(M+).

Embodiment 2

[0057] Preparation of 3-methoxy-4-benzyloxy-6-nitrobenzaldehyde (3)

[0058] 3-Methoxy-4-benzyloxybenzaldehyde 2 (13.6 g, 41 mmol) was slowly added into concentrated nitric acid (95 mL) at 10°C. After the addition was complete the reaction was stirred at 15°C for two hours. The reaction solution was poured into ice water, stirred, and filtered to obtain yellow solid 3 (12.9 g, 80%). m.p.: 127-130°C (literature m.p.131°C). EI-MS m / z: 287(M+).

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Abstract

The invention relates to the field of pharmaceutical chemistry, in particular to quinazolinone vasoinhibitors with general formulas I and II, and a preparation method and a medical application thereof, particularly use of the quinazolinone vasoinhibitors as medicines for preventing or treating tumors, retinopathy, rheumatic arthritis, diabetes, lupus erythematosus, chronic inflammation and other vascular proliferation diseases. The general formulas I and II are shown in the specifications.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry, in particular to a series of quinazolinone vascular inhibitors, their preparation methods and their medical use, especially as a method for preventing or treating tumors, retinopathy, diabetes, rheumatoid arthritis, lupus erythematosus , chronic inflammatory response and other vascular proliferative disease drugs. Background technique [0002] Angiogenesis refers to the process in which endothelial cells proliferate and migrate to form new blood vessels through budding or embedding on the basis of existing blood vessels. Angiogenesis can occur under both physiological and pathological conditions. Under normal physiological conditions, physiological stimuli during wound healing, embryonic development, and reproductive processes can induce local angiogenesis. However, pathological angiogenesis is related to many diseases, such as tumor growth and invasion, retinopathy, diabetes, rheumat...

Claims

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Application Information

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IPC IPC(8): C07D239/90A61K31/517A61P3/10A61P9/10A61P19/02A61P29/00A61P35/00A61P37/02
Inventor 向华司文博辛敏行刘元元肖红严明尤启冬张陆勇廖清江
Owner CHINA PHARM UNIV
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