- Metal-free or transition-metal-catalyzed one-pot synthesis of 2-aminobenzothiazoles
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A series of 2-aminobenzothiazoles were synthesized by using 2-halogen-substituted anilines (halogen = Cl, Br, I) and dithiocarbamates in the presence of KOt-Bu. This simple and efficient protocol lets the reactions undergo in a smooth and rapid way to afford the corresponding 2-aminobenzothiazoles in good yields. It is noteworthy that the present process allows the construction of 2-aminobenzothiazoles from a wide range of 2-halogen-substituted aniline derivatives, including substituted 2-iodoanilines, 2-bromoanilines and 2-chloroanilines.
- Xu, Wan,Zeng, Meng-Tian,Liu, Min,Liu, Xing,Chang, Cai-Zhu,Zhu, Hui,Dong, Zhi-Bing
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- Copper-catalyzed tandem reaction of 2-haloanilines with thiocarbamoyl chloride: Synthesis of 2-aminobenzothiazoles
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A simple and efficient protocol for the synthesis of 2-aminobenzothiazoles by a ligand-free copper-catalyzed tandem reaction has been developed. In the presence of CuBr and t-BuOK, a variety of 2-haloanilines (halogen = Br, I) underwent the reaction with thiocarbamoyl chloride efficiently to afford the corresponding 2-aminobenzothiazoles in good yields (83–94%). The features of this method include good yield, cheap catalyst, mild reaction conditions, and broad substrate scope, which make the protocol practical and attractive in the preparation of some potential pharmaceutically active compounds.
- Chang, Cai-Zhu,Xu, Wan,Zeng, Meng-Tian,Liu, Min,Liu, Xing,Zhu, Hui,Dong, Zhi-Bing
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- 1, 3, 4, 5-TETRAHYDRO-2H-PYRIDO[4,3-B]INDOLE DERIVATIVES FOR THE TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH TAU AGGREGATES LIKE ALZHEIMER'S DISEASE
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The present invention relates to novel compounds that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).
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Page/Page column 83
(2019/07/20)
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- TETRAHYDROBENZOFURO[2,3-C]PYRIDINE AND BETA-CARBOLINE COMPOUNDS FOR THE TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH TAU AGGREGATES
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The present invention relates to novel compounds of formula (I) that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).
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Page/Page column 60
(2019/12/28)
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- Copper(II)-Promoted Cascade Synthesis of 2-Aminobenzothiazoles Starting from 2-Iodoanilines and Sodium Dithiocarbamates
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A facile and efficient formation of 2-aminobenzothiazoles by a copper(II)-promoted one-pot cascade process was developed. The desired 2-aminobenzothiazoles were synthesized in good to excellent yields (up to 97 %) in the presence of Cu(OAc)2 an
- Zhu, Hui,Zhang, Shi-Bo,Liu, Xing,Cheng, Yu,Peng, Han-Ying,Dong, Zhi-Bing
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supporting information
p. 5711 - 5716
(2018/10/31)
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- Method for catalytically synthesizing 2-aminobenzothiazole derivative by N, N-dimethylthio carbamoyl chloride under microwave radiation
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The invention discloses a method for catalytically synthesizing a 2-aminobenzothiazole derivative under microwave radiation. A catalytic amount of copper iodide serving as a catalyst, 8-hydroxyquinoline serving as a ligand, potassium hydroxide serving as an auxiliary catalyst, 2-halogenated aniline, a derivative of 2-halogenated aniline, powdered sulfur, an N, N-dimethylthio carbamoyl chloride derivative and pyridine are added into a reaction vessel, the reaction vessel is placed into a microwave reactor, reaction is performed at a certain temperature and under a certain power, vacuum concentration is performed after a certain time, and a product is purified by column chromatography. According to the method, raw materials are novel, operation is simple and convenient, and the 2-aminobenzothiazole derivative is efficiently prepared. Compared with the prior art, the method has the advantages that reaction speed is obviously increased as compared with conventional heating, reaction conditions are mild, and the method is simple in operation, high in yield, safe, low in cost and environmentally friendly.
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Paragraph 0028; 0038
(2018/04/28)
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- Copper catalyzed synthesis of benzoxazoles and benzothiazoles via tandem manner
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A useful protocol for the preparation of substituted 2-aminobenzoxazoles and 2-aminobenzothiazoles was presented. Under the catalysis of copper, 2-aminophenols or 2-aminothiophenols reacted with thiocarbamoyl chlorides via a tandem manner, furnishing a series of 17 benzoheterocycles smoothly with good to excellent yields (70–91%). The broad substrate scope, short reaction time, mild react conditions, easy performance and nice yields make this approach attractive, showing its practical synthetic value for the preparation of some biologically or pharmaceutically active compounds.
- Xu, Wan,Zeng, Meng-Tian,Liu, Sha-Sha,Li, Yue-Sheng,Dong, Zhi-Bing
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supporting information
p. 4289 - 4292
(2017/10/12)
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- Palladium-Catalyzed Synthesis of 2-Aminobenzothiazoles through Tandem Reaction
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A variety of 2-aminobenzothiazoles were synthesized by using 2-chloroanilines and dithiocarbamates through a tandem approach in the presence of Pd(PPh 3) 4 and t -BuOK. The facile and efficient protocol enabled the reaction to proceed at a good rate with excellent yields.
- Xu, Wan,Zeng, Meng-Tian,Liu, Min,Liu, Sha-Sha,Li, Yue-Sheng,Dong, Zhi-Bing
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p. 3084 - 3090
(2017/07/13)
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- Palladium-catalyzed tandem synthesis of 2-aminobenzothiazoles starting from unreactive 2-chloroanilines
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A simple and efficient protocol for the synthesis of 2-aminobenzothiazole derivatives is described. 2-Chloroanilines were treated with thiocarbamoyl chloride in the presence of Pd(dba)2 and t-BuOK to afford the corresponding 2-amino-benzothiazoles in good to excellent yield via a tandem manner.
- Xu, Wan,Zeng, Meng-Tian,Liu, Min,Liu, Xing,Chang, Cai-Zhu,Zhu, Hui,Li, Yue-Sheng,Dong, Zhi-Bing
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supporting information
p. 641 - 643
(2017/09/01)
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