- Construction of 2-Arylbenzo[4,5]thieno[2,3-d]thiazole Skeleton via CuCl/S-Mediated Three-Component Reaction
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An exclusive thiophene-fused polycyclic I-conjugated 2-arylbenzo[4,5]thieno[2,3-d]thiazole skeleton was constructed via a one-pot CuCl-mediated three-component reaction, using 2-(2-bromophenyl)acetonitrile and aromatic aldehydes as substrates and elementa
- Zhang, Wei,Tao, Shanqing,Ge, Huaibin,Li, Qiao,Ai, Zhenkang,Li, Xiaoxian,Zhang, Beibei,Sun, Fengxia,Xu, Xiaqing,Du, Yunfei
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supporting information
p. 448 - 452
(2020/02/04)
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- Direct synthesis of diverse 2-aminobenzo[b]thiophenes via palladium-catalyzed carbon-sulfur bond formation using Na2S2O3 as the sulfur source
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A novel and direct synthesis of various 2-aminobenzo[b]thiophenes has been developed. The reactions were catalyzed by a combination of Pd(dppf)Cl2 and dppf using odorless and cheap Na2S2O3 as the sulfur source. This strategy allowed us to synthesize important 2-aminobenzo[b]thiophene scaffold more efficiently and conveniently.
- Hou, Chuanwei,He, Qian,Yang, Chunhao
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supporting information
p. 5040 - 5043
(2014/12/11)
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- Methods for inhibiting protein kinases
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The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim-1 kinase, and tyrosine kinase using imidazo[1,2-a]pyrazine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.
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Page/Page column 193
(2010/11/27)
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- Imidazopyrazines as protein kinase inhibitors
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In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.
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Page/Page column 125
(2010/11/27)
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- General preparation of primary, secondary, and tertiary aryl amines by the oxidative coupling of polyfunctional aryl and heteroaryl amidocuprates
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(Chemical Equation Presented). A tolerant reaction: Functionalized tertiary amines have been prepared by the oxidative coupling of amidocuprates with chloranil used as the oxidant (see Scheme). A high tolerance of functional groups and insensitivity to steric hindrance characterize this general amination reaction.
- Del Amo, Vicente,Dubbaka, Srinivas Ready,Krasovskiy, Arkady,Knochel, Paul
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p. 7838 - 7842
(2007/10/03)
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- REVERSED PYRIMIDINONE COMPOUNDS AS CALCILYTICS
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Calcilytic compounds and methods of preparing them are disclosed. Methods of using the calcilytic compounds are also provided.
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Page/Page column 38
(2010/11/08)
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- Electrophilic Amination of Higher Order Cuprates with N,O-Bis(trimethylsilyl)hydroxylamine
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In the reaction of higher order cyanocuprates with N,O-bis(trimethylsilyl)hydroxylamine delivery of the NHSiMe3 moiety to one of the anionic ligands in the cuprate takes place even in the absence of external bases according to an "electrophilic amination" protocol.Details of the methodology are given, and the reaction mechanism is analyzed in terms of interception by a mixed bis-metal cluster of a lithium N-silyl-N-siloxyamide, followed by intramolecular C-N coupling.This method is applicable to cyanocuprates bearing aromatic, heteroaromatic, and saturated aliphatic ligands.A number of 2-amino-substituted heterocycles, not easily accesible by normal routes, can be obtained with the aid of a stabilizing silylation at the nitrogen atom.
- Casarini, Antonella,Dembech, Pasquale,Lazzari, Dario,Marini, Elisabetta,Reginato, Gianna,et al.
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p. 5620 - 5623
(2007/10/02)
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- THERMAL REACTIVITY OF 2-AZIDO- AND 3-AZIDO-BENZOTHIOPHENE WITH DIALKYLAMINES AND ALKANETHIOLS
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On thermolysis in diethyl- or dimethyl-amine both 3-azido- and 2-azidobenzothiophene afford the appopriate 3-(dialkylamino)-2-aminobenzothiophene in good yield, whereas in ethyl or butyl mercaptan at room temperature, these azides smoothly lead to 2-(alkylthio)-3-amino- and 3-(alkylthio)-2-amino-benzothiophene, respectively.
- Toselli, Maurizio,Spagnolo, Piero,Zanirato, Paolo
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p. 411 - 414
(2007/10/02)
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