827-46-3Relevant academic research and scientific papers
Enantioselective Construction of Spiro[chroman-thiazolones]: Bifunctional Phosphonium Salt-Catalyzed [2+4] Annulation between 5-Alkenyl Thiazolones and ortho-Hydroxyphenyl-Substituted para-Quinone Methides
Tan, Jian-Ping,Zhang, Hongkui,Jiang, Zhiyu,Chen, Yuan,Ren, Xiaoyu,Jiang, Chunhui,Wang, Tianli
supporting information, p. 1058 - 1063 (2020/01/02)
The enantioselective formal [2+4] annulation of 5-alkenyl thiazolones with hydroxyl-substituted para-quinone methides was disclosed by dipeptide-based phosphonium salt catalysts. A wide range of functionalized spiro-chroman-thiazolone molecules bearing three contiguous 3° and/or 4° stereocenters were readily constructed in high yields with excellent stereoselectivities (>20:1 dr and up to >99.9% ee) under low catalyst loading and mild reaction conditions. The practicality and utility of this protocol were demonstrated by the scaled-up preparation and elaborations of product. (Figure presented.).
Organophosphane-catalyzed direct β-acylation of 4-arylidene pyrazolones and 5-arylidene thiazolones with acyl chlorides
Khairnar, Pankaj V.,Su, Yin-Hsiang,Chen, Yung-Chang,Edukondalu, Athukuri,Chen, Yi-Ru,Lin, Wenwei
supporting information, p. 6868 - 6872 (2020/09/15)
An efficient method for the direct β-acylation of arylidene pyrazolones and thiazolones with acyl chlorides in the presence of a base catalyzed by organophosphanes is reported. A variety of functionalized 4-arylidene pyrazolone and 5-arylidene thiazolone derivatives were prepared under metal-free and mild conditions via a tandem phospha-Michael addition/O-acylation/intramolecular cyclization/rearrangement sequence. Our mechanistic investigations revealed that the reaction is highly stereospecific to provide exclusively cis-isomers, and the methodology can also be scaled up with similar efficacy.
Thiazolo [2,3-b] oxazolone compound and preparation method and application thereof
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Paragraph 0084-0086, (2019/12/10)
The invention provides a compound shown in a formula I, or a salt thereof, or a stereoisomer thereof; R1 is selected from 3 and 8-element unsaturated cycloalkyl and 3 and 8-element unsaturated heterocyclic group; R2 is selected from hydrogen, C1-C8 alkyl
Dihydopyranothiazole ring compound as well as preparation method and application thereof
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Paragraph 0035; 0036; 0109; 0110, (2018/03/24)
The invention provides a dihydopyranothiazole ring compound shown as a formula (I) and further provides a preparation method for preparing the previous compound. The compound disclosed by the invention is simple and convenient in preparation method, mild
Crystal form of dihydropyranothiazole compound and preparation method thereof
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Paragraph 0024-0025, (2018/04/03)
The invention provides a crystal form I of a compound shown by formula (A). The crystal form I is characterized in that the crystal form is a triclinic system, wherein the space group is P1, and the cell parameters are shown in the description. The invent
Oxidative N-heterocyclic carbene catalyzed stereoselective annulation of simple aldehydes and 5-alkenyl thiazolones
Lin, Li,Yang, Yuhong,Wang, Mei,Lai, Luhao,Guo, Yarong,Wang, Rui
supporting information, p. 8134 - 8137 (2015/05/20)
A highly diastereoselective annulation of simple aldehydes and 5-alkenyl thiazolones, via oxidative NHC catalysis has been developed. This strategy provides facile access to a diverse library of functionalized chiral thiazolo pyrones. Aerobic oxygen can a
4-Hydroxythiazole Inhibitors of 5-Lipoxygenase
Kerdesky, Francis A. J.,Holms, James H.,Moore, Jimmie L.,Bell, Randy L.,Dyer, Richard D.,et al.
, p. 2158 - 2165 (2007/10/02)
4-Hydroxythiazoles have been identified as potent inhibitors of 5-lipoxygenase in vitro exhibiting IC50's of less than 1 μM.An investigation of structure-activity relationships showed that the most potent inhibitors of this series are the 5-phenyl derivatives.The corresponding thiazolidin-4-one analogues were found to be relatively inactive.The 4-hydroxythiazoles were active inhibitors against 5-lipoxygenase in both intact rat polymorphonuclear leukocytes and human whole blood.The compounds were also selective inhibitors of 5-lipoxygenase, displaying only weak activity against other related enzymes, cyclooxygenase and 12- and 15-lipoxygenase.
A NOVEL ONE-POT SYNTHESIS OF SUBSTITUTED 4-t-BUTYLDIMETHYLSILYLOXY-THIAZOLES
Kopka, Ihor E.
, p. 3765 - 3768 (2007/10/02)
The reaction of 2-halo-acylimidazolides or halides with primary thioamides in base give 2-halo-N-acylthioamides, which cyclize to the substituted 4-thiazolones and are trapped as the novel 4-t-butyldimethylsilyloxythiazoles in fair to good yield.The 2-ary
A facile preparation of 4-thiazolone derivatives from thioamides and various haloacyl halides in a biphase system
Okawara,Kashihara,Furukawa
, p. 3479 - 3483 (2007/10/02)
The reaction of thioamides (1) with various haloacyl halides (2, 7, 11, 14, 17, and 19) was carried out in sat. NaHCO3-CH2Cl2 and 5% NaOH-CH2C12 to give several kinds of 4-thiazolones (3-5, 10, 12 and
