6142-11-6Relevant academic research and scientific papers
Synthesis of 2-aminothiazoles via rhodium-catalyzed carbenoid insertion/annulation of sulfoxonium ylides with thioureas
Chen, Yuncan,Lv, Shan,Lai, Ruizhi,Xu, Yingying,Huang, Xin,Li, Jianglian,Lv, Guanghui,Wu, Yong
, p. 2555 - 2558 (2021/03/17)
Sulfoxonium ylides as carbene precursors couple smoothly with thioureas in the presence of 5 mol% of rhodium(II) acetate dimmer via carbenoid insertion to afford the corresponding 2-aminothiazoles with high chemoselectivity, providing a facile and efficient approach to access a variety of 2-aminothiazole derivatives with good functional groups tolerance.
Novel green synthesis method for efficiently synthesizing aminothiazole derivatives through transition metal catalyzed carbene insertion/cyclization reaction
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Paragraph 0035-0036, (2020/11/01)
The invention relates to a novel green synthesis method for efficiently synthesizing aminothiazole derivatives through transition metal catalyzed carbene insertion/cyclization reaction. According to the method, sulfur ylide serves as a carbene donor, carbene is catalyzed by a transition metal to be subjected to an insertion/cyclization reaction, a C-S bond is efficiently formed, and the 2-aminothiazole derivative is constructed. Compared with the traditional method, the method has the advantages that the raw materials are easy to obtain, the steps are simple, the mild sulfur ylide reagent is used for replacing a halogenating reagent required in the traditional synthesis method, and the method is a mild, quick, simple, convenient, effective and environment-friendly method for preparing the2-aminothiazole and the derivative thereof and has a wide application prospect.
SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF NUCLEASES
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Page/Page column 14; 61-62, (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.
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.
Synthesis of 2-aminothiazoles from styrene derivatives mediated by 1,3-dibromo-5,5-dimethylhydrantoin (DBH)
Ma, Chunhua,Miao, Yuqi,Zhao, Minghao,Wu, Ping,Zhou, Jianglu,Li, Zhi,Xie, Xilei,Zhang, Wei
, p. 3602 - 3607 (2018/05/26)
An efficient procedure for the synthesis of 2-aminothiazoles via DBH-mediated oxidative cyclization of styrenes and thioureas is reported. Various alkenes were successfully transformed to the corresponding 2-aminothiazoles in yields of 10–81% via a two-step one-pot manner using DBH as both the bromine source and oxidant. The method can be readily carried out in gram-scale and successfully applied to the synthesis of anti-inflammatory drug fanetizole using styrene as starting material.
Method of synthesizing 2-aminothiazole ring compound from ethylbenzene compound
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Paragraph 0056; 0057; 0058, (2018/12/13)
The invention discloses a method of synthesizing 2-aminothiazole ring compound from ethylbenzene compound, and belongs to the technical field of thiazole ring derivative synthesis. The technical scheme of the invention is characterized by adding the ethylbenzene compound, a phase transfer catalyst, N-bromosuccinimide (NBS) and azodiisobutyronitrile (AIBN) into water in sequence, reacting at 60 DEGC, cooling after the reaction, adding inorganic base and a thiourea compound, and reacting at 80 DEG C to obtain the target product. The synthesis method has the advantages of high yield, mild reaction, low cost and environment friendliness.
Method for synthesizing novel 2-aminothiazole ring derivatives
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Paragraph 0054; 0055; 0056, (2018/11/27)
The invention discloses a method for synthesizing 2-aminothiazole ring derivatives and belongs to the technical field of organic synthesis. The method comprises that an ethylbenzene compound, dibromohydantoin DBH and t-butyl hydroperoxide TBHP are sequentially added to water, the solution undergoes a reaction at 60 DEG C, the reaction product is cooled, an inorganic base and a thiourea compound are orderly added into the reaction product and the mixture undergoes a reaction at 80 DEG C to produce desired product 2-aminothiazole ring derivatives. The method has the advantages of high yield, mild reaction, low cost and environmental friendliness.
CYANOPYRROLIDINES AS DUB INHIBITORS FOR THE TREATMENT OF CANCER
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Page/Page column 65, (2017/02/09)
The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C- terminal hydrolase L1 (UCHL1) and ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of cancer and conditions involving mitochondrial dysfunction. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1,R2,R3,R4,R5,R6,R7,R8 and R9 are as defined herein.
Method for synthesizing 1,3-substituted thiazole ring compound by styrene compound
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Paragraph 0064; 0065; 0066; 0067, (2018/01/12)
The invention discloses a method for synthesizing a 1,3-substituted thiazole ring compound by a styrene compound, and belongs to the technical field of synthesis of thiazole ring compounds. The method is characterized by comprising the following steps: dissolving the styrene compound and a phase transfer catalyst into water, adding dibromohydantoin DBH, carrying out a reaction at 60 DEG C, spin-drying after the reaction and dissolving into an organic solvent, adding a thiourea compound and performing reflux reaction to prepare a target product 1,3-substituted thiazole ring compound. The synthesis method provided by the invention is high in yield, mild in reaction, low in cost and environmentally friendly.
Nanochitosan: A biopolymer catalytic system for the synthesis of 2-aminothiazoles
Safari, Javad,Abedi-Jazini, Zahra,Zarnegar, Zohre,Sadeghi, Masoud
, p. 108 - 112 (2016/02/05)
A convenient and efficient method is described for the synthesis of 2-aminothiazoles by one-pot reaction of ketone and thiourea using chitosan nanoparticles under mild condition. Nanochitosan was used as a biodegradable and green catalyst for this reaction in satisfactory yields. The attractive advantages of the present process include easy isolation of products, milder and cleaner conditions, higher purity and yields and easier work-up procedure.
