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Benzisoxazole compound and application thereof
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A compound, isoxazole technology, applied in the field of medicine, can solve problems affecting the DA function of the substantia nigra-striatum and tubercle-infundibulum system
Active Publication Date: 2014-04-02
SHENYANG PHARMA UNIVERSITY
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Specifically, the drug exerts pharmacological effects by blocking dopamine D2 receptors in the midbrain-cerebral cortex and midbrain-limbic system, but because it also affects the DA function of the substantia nigra-striatum and tubercle-infundibulum system, so Can cause extrapyramidal reactions (EPS), as well as adverse reactions such as endocrine and metabolic changes
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Embodiment 1
[0052] Example 1: 3-{1-[3-(3,4-dihydro-2H-chromen-7-yloxy)propyl]pyridin-4-yl}-6-fluorobenzo[d]isox Preparation of azole
[0054] Example 2: Preparation of 6-{3-[4-(6-fluorobenzo[d]isoxazol-3-yl)pyridin-1-yl]propoxy}chroman-4-one
[0055] According to the method of Example 1, a white solid was obtained with a yield of 54.5%, mp.135-136°C. 1 H-NMR (CDCl 3 ,600MHz)δ(ppm):7.33(1H,d,J=3.0Hz),7.25(1H,s),7.10(1H,d,J=3.0Hz),7.08(1H,d,J=3.0Hz) ,6.92(1H,d,J=9.0Hz),4.50(2H,t,J 1 =J 2 =6.6Hz), 4.05(2H,t,J 1 =J 2 =6.0Hz), 2.80(4H,m), 2.20(6H,m); ESI-MS: m / z425([M+H] + ),446.9([M+Na] + );IR,ν(cm -1 ):2952,2824,2773,1675,1613,1519,1434,1346,1282,1234,1122,1037,957,849,786,709.
Embodiment 3
[0056] Example 3: Preparation of 7-{3-[4-(6-fluorobenzo[d]isoxazol-3-yl)pyridin-1-yl]propoxy}chroman-4-one
[0057] According to the method of Example 1, a white solid was obtained with a yield of 59.7%, mp.122-123°C. 1 H-NMR (CDCl 3 ,600MHz)δ(ppm):7.83(1H,d,J=9.0Hz),7.70(1H,s),7.24(1H,q,J 1 =8.4Hz,J 2 =2.4Hz),7.05(1H,m,J 1 =8.4Hz,J 2 =8.4Hz,J 3 =2.4Hz),6.59(1H,q,J 1 =8.4Hz,J 2 =2.4Hz),6.43(1H,d,J=2.4Hz),4.51(2H,t,J 1 =J 2 =6.6Hz), 4.09(2H,t,J 1 =J 2 =6.6Hz), 3.08(3H,s), 2.75(2H,t,J 1 =J 2 =6.6Hz), 2.57(2H,s), 2.21(2H,m), 2.07(4H,m), 2.04(2H,m); ESI-MS: m / z425([M+H] + ),446.9([M+Na] + );IR,ν(cm -1 ):2957,2917,2849,2759,1675,1612,1578,1518,1495,1441,1257,1233,1197,1169,1122,1059,957,907,830,620.
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Abstract
The invention relates to a benzisoxazole compound and application thereof, in particular relates to the benzisoxazole compound, a stereisomer and pharmaceutically acceptable salt of the benzisoxazole compound, and application of the benzisoxazole compound, belonging to the technical field of medicines. The compound is characterized in that 6-fluorine-3-(4-piperidyl)-1,2-benzisoxazole hydrochloride containing an antipsychotic active structural segment is respectively connected with 6-hydroxychroman, 7-hydroxychroman, 6-hydroxy-4-chromanone, 7-hydroxy-4-chromanone, a flavonoids compound and an isoflavones compound through 1,3-dibromo chloropropane to synthesize nine benzisoxazole compounds based on the bioisosteres and splicing principle; the benzisoxazole compounds as shown in the structural formula below have high application value and wide development and application prospect. The benzisoxazole compounds and pharmaceutically acceptable acid addition salt of the benzisoxazole compound can be combined or individually used as 5-HT2 / D2 receptor antagonists for treating schizophrenia.
Description
Technical field: [0001] The invention belongs to the technical field of medicine, and relates to benzisoxazole compounds and applications thereof, in particular to benzisoxazole compounds, stereoisomers and pharmaceutically applicable salts of the compounds and applications thereof. The compound is 5-HT 2 / D 2 Receptor antagonists are the first personalized psychiatric drugs and the first gene-targeted drugs for the treatment of schizophrenia. Background technique: [0002] The cause of schizophrenia is due to the excessive activation of dopamine neurons in the patient's brain. Antipsychotic drugs produce antipsychotic effects mainly by blocking dopamine (DA) receptors in the brain. Specifically, the drug exerts pharmacological effects by blocking dopamine D2 receptors in the midbrain-cerebral cortex and midbrain-limbic system, but because it also affects the DA function of the substantia nigra-striatum and tubercle-infundibulum system, so It can cause extrapyramidal rea...
Claims
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Application Information
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