Discovery and structural optimization of 4-(4-(benzyloxy)phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists
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The Synthesis and Evaluation of Dihydroquinazolin-4-ones and Quinazolin-4-ones as Thyroid Stimulating Hormone Receptor Agonists.
We herein describe the rapid synthesis of a diverse set of dihydroquinazolin-4-ones and quinazolin-4-ones, their biological evaluation as thyroid stimulating hormone receptor (TSHR) agonists, and SAR analysis. Among the compounds screened, 8b was 60-fold more potent than the hit compound 1a, which was identified from a high throughput screen of over 73,000 compounds.
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In this research, one-pot three-component synthesis of 3,4-dihydropyrimidin-2-(1H)-ones havebeen developed using Biginelli reaction from the interaction between ethyl/methyl acetoacetate,aromatic aldehydes, and urea/thiourea in the presence of 4-sulfobenzoic acid as a new, effective,inexpensive, and available bronsted acid. Avoidance of toxic and dangerous solvents, easy isola...
متن کاملpreparation of 3, 4-dihydropyrimidin-2(1H)-ones using quaternary ammonium- treated clay in water
In this study, a variety of 3, 4-dihydropyrimidin-2(1H)-ones derivatives were synthesized via three-component Biginelli reaction. The quaternary ammonium- treated clay -catalyzed process proved to be simple, efficient, and environmentally friendly.
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Different (±)-4-(3/4-acetoxyaryl)-5-ethoxycarbonyl-6-methyl-3,4-dihydropyrimidin-2-ones have been synthesized and subjected to enantioselective deacetylation reactions mediated by different lipases in organic media. Novozyme 435 in tetrahydrofuran:diisopropyl ether was found to be the catalyst of choice for efficient enantioselective deacetylation of dihydropyrimidinones under study. Further, w...
متن کامل1H-Imidazol-4(5H)-ones and thiazol-4(5H)-ones as emerging pronucleophiles in asymmetric catalysis
Asymmetric catalysis represents a very powerful tool for the synthesis of enantiopure compounds. In this context the main focus has been directed not only to the search for new efficient chiral catalysts, but also to the development of efficient pronucleophiles. This review highlights the utility and first examples of 1H-imidazol-4(5H)-ones and thiazol-4(5H)-ones as pronucleophiles in catalytic...
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ژورنال
عنوان ژورنال: Acta Pharmacologica Sinica
سال: 2016
ISSN: 1671-4083,1745-7254
DOI: 10.1038/aps.2016.32