- Preparation method of indazole and application of indazole in medicine synthesis
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The invention belongs to the field of chemicals, and relates to a preparation method of indazole and an application of the indazole in medicine synthesis. The invention discloses a preparation method of indazole and an application of the indazole in synthesizing 1H-indazole-3-carboxylic acid, lonidamine, a compound 8, a compound 9, a compound 10, axitinib, YD-3, YC-1 and similar substances thereof.
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Paragraph 0124; 0125; 0132; 0133
(2017/04/21)
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- Copper(I) Oxide-Mediated Cyclization of o-Haloaryl N-Tosylhydrazones: Efficient Synthesis of Indazoles
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An efficient synthesis of indazoles from readily accessible E/Z mixtures of o-haloaryl N-tosylhydrazones has been developed. The thermo-induced isomerization of N-tosylhydrazones is discussed. A series of valuable indazole derivatives are prepared in good yields, and the method has been successfully applied to the synthesis of the bioactive compounds, lonidamine, AF-2785, axitinib, YC-1 and YD-3.
- Tang, Meng,Kong, Yuanfang,Chu, Bingjie,Feng, Dan
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supporting information
p. 926 - 939
(2016/04/05)
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- Efficient palladium-catalyzed C(sp2)-H activation towards the synthesis of fluorenes
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A facile protocol for the synthesis of fluorene derivatives has been developed through palladium-catalyzed cyclization of 2′-halo-diarylmethanes via activation of arylic C-H bonds. The reactions occurred smoothly and allowed both electron-rich and electron-deficient substrates to convert into their corresponding fluorenes in good to excellent yields. Studies revealed that this Pd-catalyzed cyclization was also available for the substrates of 2′-chloro-diarylmethanes and no catalyst poisoning occurred for 2′-iodo-diphenylmethane.
- Song, Juan,Li, Yali,Sun, Wei,Yi, Chenglong,Wu, Hao,Wang, Haotian,Ding, Keran,Xiao, Kang,Liu, Chao
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supporting information
p. 9030 - 9033
(2016/11/11)
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- Bismuth-catalyzed synthesis of anthracenes via cycloisomerization of o-alkynyldiarylmethane
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In this study, anthracenes were efficiently synthesized from o-alkynyldiarylmethane using a novel method that exploits the synergistic effect between Bi(OTf)3 as the catalyst, and trifluoroacetic acid (TFA). Through this reaction, we achieved the rapid and efficient synthesis of anthracenes bearing various functional groups under mild conditions.
- Park, Jungmin,Choi, Hyuck,Lee, Deug-Chan,Lee, Kooyeon
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supporting information
p. 7005 - 7007
(2015/11/27)
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- CuII-catalyzed asymmetric hydrosilylation of diaryl- and aryl heteroaryl ketones: Application in the enantioselective synthesis of orphenadrine and neobenodine
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With certain amounts of sodium tert-butoxide and tert-butanol as additives, catalytic amounts of an inexpensive and easy-to-handle copper source Cu(OAc)2·H2O, a commercially available and air-stable non-racemic dipyridylphosphine ligand, as well as the stoichiometric desirable hydride donor polymethylhydrosiloxane (PMHS), formed a versatile in situ catalyst system for the enantioselective reduction of a broad spectrum of prochiral diaryl and aryl heteroarylketones in air, in high yields and with good to excellent enantioselectivities (up to 96 %). In particular, the practical viability of this process was evinced by its successful applications in the asymmetric synthesis of optically enriched potent antihistaminic drugs orphenadrine and neobenodine. Copyright
- Sui, Yao-Zong,Zhang, Xi-Chang,Wu, Jun-Wen,Li, Shijun,Zhou, Ji-Ning,Li, Min,Fang, Wenjun,Chan, Albert S. C.,Wu, Jing
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supporting information; experimental part
p. 7486 - 7492
(2012/07/27)
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- Fluorenone synthesis by palladacycle-catalyzed sequential reactions of 2-bromobenzaldehydes with arylboronic acids
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Chemical equations presented. A new, anionic four-electron donor-based (type I) palladacycle-catalyzed sequential reaction of 2-bromobenzaldehydes with arylboronic acids based on the addition reaction, cyclization via C-H activation-oxidation sequence is described. Our study provided an efficient access to a variety of substituted fluorenones/indenofluorenediones from readily available arylboronic acids and 2-bromobenzaldehydes.
- Liu, Tao-Ping,Liao, Yuan-Xi,Xing, Chun-Hui,Hu, Qiao-Sheng
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supporting information; experimental part
p. 2452 - 2455
(2011/06/25)
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- A nontransmetalation reaction pathway for anionic four-electron donor-based palladacycle-catalyzed addition reactions of arylborons with aldehydes
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A nontransmetalation reaction pathway for anionic four-electron donor-based (Type I) palladacycle-catalyzed addition reactions of arylborons with aldehydes is described. This new reaction pathway offers new catalysis opportunities for Type I palladacycle-catalyzed addition reactions such as the exceptionally low catalyst loading catalysis, with the catalyst loading as low as 0.0005 mol %. This new pathway may be applicable for other transition metal-catalyzed addition reactions and might lead to the development of new reactions including sequential/tandem reactions.
- Liao, Yuan-Xi,Xing, Chun-Hui,Israel, Matthew,Hu, Qiao-Sheng
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supporting information; experimental part
p. 3324 - 3328
(2011/06/28)
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- Iron-catalyzed, microwave-promoted, one-pot synthesis of 9-substituted xanthenes by a cascade benzylation-cyclization process
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"Chemical Equation Presented" An efficient iron-catalyzed, microwave-promoted cascade benzylation-cyclization of phenols is reported. Benzyl acetates, benzyl bromides, and benzyl carbonates are suitable benzylating reagents. The reactions proceed to afford both 9-aryl and 9-alkyl xanthene derivatives in good to high yields using FeCI3 as the catalyst under MW irradiation conditions
- Xu, Xiaobing,Xu, Xiaolei,Li, Hongfeng,Xie, Xin,Li, Yanzhong
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supporting information; experimental part
p. 100 - 103
(2010/03/04)
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- Orthoplatinated triarylphosphite as a highly efficient catalyst for addition reactions of arylboronic acids with aldehydes: Low catalyst loading catalysis and a new tandem reaction sequence
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(Chemical Equation Presented) Readily available, air/moisture-stable orthoplatinated triarylphosphite catalyzes the addition reactions of arylboronic acids with aldehydes with the catalyst loading as low as 0.01%. It also cataylzes a new tandem reaction of arylboronic acids with α,β- unsaturated aldehydes to form 1,3-diaryl-1-propanols. Our study provides a new paradigm for the application of orthoplatinated triarylphosphites, and may pave the road to develop other Pt(II) catalysts for such addition reactions and other tandem reactions with such addition reactions as part of the reaction sequence.
- Liao, Yuan-Xi,Xing, Chun-Hui,He, Ping,Hu, Qiao-Sheng
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supporting information; experimental part
p. 2509 - 2512
(2009/05/26)
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- Orthobromodiphenylmethane derivatives as starting materials for the total synthesis of anthraquinones
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In this communication we describe the synthesis of four simple anthraquinones by a five-step sequence, using easily available bromobenzaldehydes and phenyllithium derivatives as starting materials.
- Almeida, Wanda P.,Costa, Paulo R.R.
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p. 4507 - 4518
(2007/10/03)
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