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Substituted fused pyrimidinone compounds
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A compound and alkyl technology, applied in the field of fused pyrimidinone derivatives, can solve problems such as no effective treatment
Inactive Publication Date: 2018-12-21
TORRENT PHARMA LTD
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[0012] Despite known targets and pathways to control inflammation, there are currently no drugs that address the mechanisms underlying the effective treatment of disease conditions including COPD and asthma
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[0146] To 4-amino-2,2-dimethyl-2,3-dihydro-1-benzofuran-7-ol (30g, 167mmol) and bis(pinacolate) diboron (51gm, 201mmol) in To a stirred solution in acetonitrile (300ml) was added a catalytic amount of benzoyl peroxide at room temperature. The reaction mixture was cooled to 0 °C, and tert-butyl nitrite (30 ml, 251 mmol) was added dropwise to the reaction mixture. The reaction mixture was stirred at room temperature for 5 to 6 h. The reaction mixture was poured into water and extracted with ethyl acetate. The ethyl acetate layer was separated, dried over sodiumsulfate and concentrated under vacuum to obtain a crude solid. The crude product was further purified by silica gelcolumn chromatography (hexane / ethyl acetate=90:10) to obtain 26.0 gm of the title compound as a white solid.
[0152] For 2,2-dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)- A similar procedure described for 2,3-dihydro-1-benzofuran-7-ol, from 7-amino-2,3-dihydro-1H-inden-4-ol and bis(pinacolate)diboron Synthesis of the title compound.
[0157] To a stirred solution of 2-amino-6-methylbenzoic acid (25 g, 165 mmol) in toluene (375 ml) was added chloroacetyl chloride (26 ml, 326 mmol) dropwise at room temperature. The reaction mixture was heated at 100 °C for 6 h. The reaction mixture was cooled to room temperature and poured into ice-cold water; the solid thus precipitated was filtered and dried under vacuum to afford 30.0 gm of the title compound as a brown solid.
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Abstract
Provided herein are novel fused pyrimidinone derivatives of Formula (I) and synthetic intermediates that are useful in preparing the compounds of formula (I). Further provided herein is a method for preparation of a compound of formula (I) or intermediates, a pharmaceutical composition comprising a compound of formula (I), and use of a compound of formula (I).
Description
technical field [0001] The present invention relates to fused pyrimidinone derivatives, pharmaceutically acceptable salts thereof, and metabolites, isomers, stereoisomers, atropisomers, conformers, tautomers, polymorphs thereof , hydrates and solvates. The invention also includes pharmaceutical compositions of the compounds and methods of preparing the novel compounds. The invention further relates to the use of the aforementioned compounds for the preparation of medicaments for use as medicine. Background technique [0002] Despite therapeutic advances, the prevalence of tracheal disease has increased in recent decades. Among airway diseases, asthmaexacerbation and chronic obstructive pulmonary disease (COPD) are the leading causes of hospitalization. Both asthma and COPD involve chronic inflammation of the airways. COPD is the term for a large group of lung diseases characterized by airflow obstruction that interferes with normal breathing. Emphysema and chronic bron...
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