- 5, 10-dihydroindolo [3, 2-b] indole derivative and synthesis method and application thereof
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The invention discloses a synthesis method of a 5, 10-dihydroindolo [3, 2-b] indole derivative, the method comprises the following steps: mixing a 2-((2-halogen phenyl) ethynyl)-N, N-dimethylaniline derivative (II), N, N-di-tert-butyl diazacycloketone (III), a palladium catalyst, a monophosphine ligand, alkali and a first organic solvent, and carrying out a diamidation reaction under the protection of inert gas to realize the synthesis of the 5, 10-dihydroindolo [3, 2-b] indole derivative(I). The method is easy to operate, mild in reaction condition and high in reaction yield, and the synthesized 5, 10-dihydroindolo [3, 2-b] indole derivative can be used for preparing an organic light-emitting device.
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Paragraph 0071; 0073-0074
(2021/07/17)
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- 1-heterocyclyl-2-(heteroarylthio) benzene derivative and use method and application
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The present invention discloses a 1-heterocyclyl-2-(heteroarylthio) benzene derivative and a use method and application, and in particular, relates to a novel 1-heterocyclyl-2-(heteroarylthio) benzene derivative and a pharmaceutical composition containing the novel 1-heterocyclyl-2-(heteroarylthio) benzene derivative, and the novel 1-heterocyclyl-2-(heteroarylthio) benzene derivative and the pharmaceutical composition can be used to inhibit 5-hydroxytryptamine reuptake. The present invention also relates to a preparation method of the novel 1-heterocyclyl-2-(heteroarylthio) benzene derivative and the pharmaceutical composition, and application of the novel 1-heterocyclyl-2-(heteroarylthio) benzene derivative and the pharmaceutical composition in the treatment of central nervous system functional disorders, particularly affective disorders.
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Paragraph 0386; 0387; 0388
(2016/10/09)
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- Palladium-catalyzed three-component approach to promazine with formation of one carbon-sulfur and two carbon-nitrogen bonds
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(Chemical Presented) Zip it up! The use of a Pd/dppf catalyst gives access to the tricyclic phenothiazine scaffold starting from 1-bromo-2-iodobenzenes, aliphatic or aromatic amines, and 2-bromothiophenols in a single reaction flask (see scheme; dppf=1,1′-bis(diphenylphosphanyl) ferrocene; dba=dibenzylidineacetone). This transformation involves thioether formation and subsequent intermolecular and intramolecular aryl amination reactions. The reaction occurs in good overall yield and selectivity.
- Dahl, Troels,Tornoe, Christian W.,Bang-Andersen, Benny,Nielsen, Poul,Jorgensen, Morten
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supporting information; experimental part
p. 1726 - 1728
(2009/02/06)
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- 4-(2-PHENYLSULFANYL-PHENYL)-PIPERIDINE DERIVATIVES AS SEROTONIN REUPTAKE INHIBITORS
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The invention provides compounds represented by the general formula (I) wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general
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Page/Page column 40
(2010/02/08)
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- Fluoro- or trifluoromethyl-substituted benzyl and phenethyl alcohols: Substrates for metal-mediated site-selective functionalization
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It was possible to functionalize the three fluorobenzyl alcohols and the three 2-(fluorophenyl)ethanols by metalation and subsequent carboxylation, the prototype electrophilic trapping reaction. Triisopropylsilyl (TIPS) outperformed methoxymethyl (MOM) as an O-protective group making seven new fluorobenzoic acids accessible in 63% average yield. Moreover, the TIPS group tolerates weakly basic and acidic media and, therefore, may facilitate further structural elaboration. The unprotected alcohols reacted more sluggishly and were unable to provide two of the targeted products (acids 1 and 2). The yield averaged only 46% in the five other cases (acids 3-7). The direct metalation of fluorinated benzyl and phenethyl alcohols remains nevertheless an attractive option because of its operational simplicity. All three (trifluoromethyl)benzyl alcohols and two of the three (trifluoromethyl)phenethyl alcohol isomers were successfully submitted to the metalation/functionalization sequence. These five starting materials gave rise to a total of nine new benzoic acids or lactones (compounds 8-14 and 17-18). Despite the poor yields (31% on average), the organometallic methods employed are, in general, extremely selective, economical and easy to perform. Wiley-VCH Verlag GmbH, 69451 Weinheim, Germany, 2002.
- Marzi, Elena,Spitaleri, Andrea,Mongin, Florence,Schlosser, Manfred
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p. 2508 - 2517
(2007/10/03)
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- Generation of functionalized asymmetric benzynes with TMP-zincates. Effects of ligands on selectivity and reactivity of zincates
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We have developed new methods for preparing functionalized benzynes through deprotonative zincation as a key reaction using R2Zn(TMP)Li, and we also describes dramatic ligand effects on the benzyne formation. Deprotonative zincation of various meta-substituted bromobenzenes with Me2Zn(TMP)Li proved effective for the one-pot generation of various 3-functionalized benzynes, particularly those electrophilic substituents such as ester, amide, and cyano. On the other hand, zincation with tBu2Zn(TMP)Li, followed by electrophilic trapping (with I2) proved a powerful tool for the preparation of 1,2,3-trisubstituted aromatic compounds.8 The resultant 1,2,3-trisubstituted benzenes are available as precursors for generation of 3-substituted benzynes by halogen-zinc exchange reactions with Me3ZnLi. These methods offer far greater generality than previous methods for the synthesis of functionalized asymmetric benzynes, and should be of value in new syntheses of various natural products and functional materials. In addition, these results underline the utility of spectator ligands on the central metal of ate complexes as a tunable functionality in the development of new ate complex-promoted reactions. Copyright
- Uchiyama, Masanobu,Miyoshi, Tomoko,Kajihara, Yumiko,Sakamoto, Takao,Otani, Yuko,Ohwada, Tomohiko,Kondo, Yoshinori
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p. 8514 - 8515
(2007/10/03)
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