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A kind of 3,4-dibenzamidobenzamide derivative and its preparation method and application
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A dibenzamide-based benzamide and benzamide-based technology, which is applied in the field of medicinal chemistry and can solve problems such as use restrictions
Active Publication Date: 2019-02-01
NANJING ZHONGRUI PHARMA
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Problems solved by technology
However, due to obvious adverse reactions such as bleeding and thrombocytopenia, blood monitoring of patients is required, so the use of these anticoagulants in clinical practice is subject to certain restrictions.
Method used
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[0075] Preparation of 4-(2-oxopyridin-1(2H)-yl)benzoic acid
[0076]
[0077] Add 400mL of absolute ethanol dried over 3A molecular sieves, 33.0g (0.2mol) of 4-carboxyphenylboronic acid, 8mL of concentrated sulfuric acid, reflux at 105-110°C for 24h, and TLC (CHCl 3 / MeOH=10 / 1) detects that there are very few raw materials, and the ethanol is evaporated under reduced pressure to obtain a white solid, which is added to 500 mL of water, filtered, and saturated with NaHCO 3 The solution was washed with 250 mL, washed with water until neutral, and dried to obtain 33.5 g of 4-ethoxycarbonylphenylboronic acid (yield 86.3%).
[0078] Sequentially add dry CH 2 Cl 2 200mL, 9.5g (0.1mol) of 2-hydroxypyridine, 20.0g (0.1mol) of copper acetate monohydrate, add Et 3 N 100mL, 19.7g (0.1mol) of 4-ethoxycarbonylphenylboronic acid, 20.0g of powdered 4A mol...
Embodiment 2
[0095] Embodiment 2: the preparation of compound 2
[0096] With 3,4-dimethoxybenzoic acid instead of 4-methoxybenzoic acid, it was prepared according to the method of Example 1: N-(5-carbamoyl-2-(4-(2-oxopyridine- 1(2H)-yl)benzamido)phenyl)-3,4-dimethoxybenzamide (compound 2, mp: 278-282°C; ESI-MS: m / z 513 [M+1 ] + ).
Embodiment 3
[0097] Embodiment 3: the preparation of compound 3
[0098] With 3,4,5-trimethoxybenzoic acid instead of 4-methoxybenzoic acid, it was prepared according to the method of Example 1: N-(5-carbamoyl-2-(4-(2-oxopyridine -1(2H)-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide (compound 3, mp: 265-267°C; ESI-MS: m / z 543 [M +1] + ).
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Abstract
The invention discloses a 3,4-dibenzamido benzamide derivative (I), wherein R1, R2 and R3 are respectively and individually hydrogen, fluorine, chlorine, bromine, hydroxyl groups, alkoxy groups, amino groups or substituted amino groups. The alkoxy groups are a C1-C4 alkoxy groups. The substituted amino groups include amino-NR5R6, acylamino-NHCOR7 and sulfoamino-NHSO2R8. The R5, R6, R7 and R8 are respectively and individually C1-C4 alkyl groups and C1-C4 halogenated alkyl groups. The R4 is a five-membered to seven-membered N-heterocyclic group. The invention also discloses a preparation method of the compound, and an application of the compound as an FXa inhibitor in preparation of medicines for preventing or treating cardiovascular and cerebrovascular diseases.
Description
technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a kind of blood coagulation factor Xa inhibitor 3,4-dibenzamidobenzamide derivatives, a preparation method thereof and an application in preparation of drugs for treating or preventing cardiovascular and cerebrovascular diseases. Background technique [0002] The key factor in the occurrence of myocardial infarction, unstable angina pectoris and pulmonary embolism (pulmonary embolism, PE) and other diseases is the formation of thrombus in human blood vessels. Therefore, blocking the coagulation chain and preventing the formation of thrombus is one of the most effective means of treating and preventing these thrombotic diseases. Arterial and venous thrombosis remains a leading cause of death despite tremendous efforts in recent years to prevent and treat blood clots. Current drugs for the prevention and treatment of thrombosis include aspirin, warfarin, clopidogrel,...
Claims
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