6318-74-7Relevant academic research and scientific papers
A one-pot synthesis of 2-aminothiazoles via the coupling of ketones and thiourea using I2/dimethyl sulfoxide as a catalytic oxidative system
Zhang, Qian,Wu, Jiefei,Pan, Zexi,Zhang, Wen,Zhou, Wei
, p. 89 - 94 (2020/06/17)
A series of 2-aminothiazoles is prepared in moderate-to-good yields by the direct coupling of ketones and thiourea using I2/dimethyl sulfoxide as a catalytic oxidative system. This method avoids the preparation of lachrymatory and toxic α-haloketones and the use of an acid-binding agent, thus providing a more convenient approach to 2-aminothiazoles compared to the Hantzsch reaction.
Method for preparing 2-aminothiazole compound
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Paragraph 0114-0119, (2020/03/09)
The invention discloses a method for preparing a 2-aminothiazole compound. The method comprises the following steps: in an organic solvent, carrying out a condensation reaction on thiourea representedby a formula (II) and a ketone compound represented by a formula (III) at 50-120 DEG C for 6-24 h under the catalysis of elemental iodine, and after the reaction is finished, carrying out post-treatment on the reaction solution to obtain the 2-aminothiazole compound represented by a formula (I). According to the invention, the method has characteristics of cheap and easily available reaction rawmaterials, mild reaction conditions, simpleness, no requirement of transition metal catalysts and a stoichiometric halogenating reagents and cost reducing, and can be used for synthesizing a series of2-aminothiazole derivatives, and the prepared products can be used as important intermediates for synthesizing thiazole structure-containing drugs or bioactive compounds.
2-Amino-4-arylthiazoles through One-Pot Transformation of Alkylarenes with NBS and Thioureas
Shibasaki, Kaho,Togo, Hideo
, p. 2520 - 2527 (2019/04/04)
Treatment of alkylarenes with N-bromosuccinimide in a mixture of ethyl acetate and water at 60 °C, a mixture of acetonitrile and water at 80 °C, or a mixture of diethyl carbonate and water under irradiation with a tungsten lamp, followed by a reaction with thioureas or arenethioamides provided the corresponding 2-amino- 4-arylthiazoles or 2,4-diarylthiazoles in good to moderate yields, respectively, in one pot. The present reaction is an efficient one-pot transformation method of alkylarenes into 2-amino-4-arylthiazoles and 2,4-diarylthiazoles directly under mild and transition-metal-free conditions.
SUBSTITUTED PROPANAMIDES AS INHIBITORS OF NUCLEASES
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, (2019/11/12)
The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3, R4, R5, R6 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF NUCLEASES
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, (2019/11/12)
The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3, R4, R5, R6 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
Efficient and facile strategy to substituted 2-aminothiazoles via ring opening of α-nitroepoxides
Zhu, Yue,Wang, Qilin,Luo, Haofan,Zhang, Guolin,Yu, Yongping
supporting information, p. 7143 - 7147 (2018/11/10)
A novel and efficient reaction has been developed to synthesize a set of substituted 2-aminothiazoles from α-nitroepoxides and ammonium thiocyanate. This reaction could proceed smoothly at mild condition, to afford products for a wide range of substrates with good to excellent yields. A possible mechanism has also been proposed.
Method for performing driving synthesis of 4-alkyl or aryl-2-aminothiazole by visible light
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Paragraph 0111; 0112; 0113; 0114; 0115; 0116, (2018/04/02)
The invention relates to a method for performing driving synthesis of 4-alkyl or aryl-2-aminothiazole by visible light. The method comprises the following steps: adding an olefin azide compound, ammonium thiocyanate and copper acetate into a solvent acetonitrile separately, performing driving reaction by using visible light with wavelength of 450 to 460 nm at the temperature of 25 DEG C for 20 to36 hours to obtain reaction liquid, and spin-drying the reaction liquid to obtain concentrate; and performing silica-gel column chromatography on the concentrate to obtain the 4-alkyl or aryl-2-aminothiazole. The method is high in yield, mild in condition and low in environmental pollution.
Synthesis of 5-Phenylthiazolamines by Using Thiourea as an α-Bromination Shuttle
Roslan, Irwan Iskandar,Ng, Kian-Hong,Chuah, Gaik-Khuan,Jaenicke, Stephan
, p. 704 - 709 (2017/02/05)
A straightforward synthesis of 5-phenylthiazolamines by coupling thiourea with phenylacetones, phenylacetophenones, and β-tetralone has been developed. Thiourea acts as a substrate and an α-bromination shuttle by transferring a Br atom from CBrCl3/s
Synthesis and antibacterial screening of novel 2-(4-(aryl) thiazol-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-ethanoisoindole-1,3(2H)-dione derivatives
?zbek, Oguz,Usta, Necibe Canan,Gürdere, Meliha Burcu,Aslan, Osman Nuri,Budak, Yakup,Ceylan, Mustafa
, p. 1153 - 1157 (2017/09/06)
A series of novel 2-(4-(aryl)thiazol-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-ethanoisoindole-1,3(2H)-dione derivatives were synthesized and evaluated for their antimicrobial activity. The structures of the synthesized derivatives (9a-j) were confirmed by means of IR, 1H-NMR, 13C-NMR and elemental analyses. All the compounds 9a-j showed activity against all microorganisms. Compounds 9a, 9c-d, and 9j exhibit potent antibacterial activity against tested S. pyogenes. Compounds 9c showed higher activity than standards against C. perfringes. 9a-e, 9j and 9i possess good activity against A. tumefacen.
