- Synthesis of indoles from aroyloxycarbamates with alkynes: Via decarboxylation/cyclization
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An efficient Pd-catalyzed decarboxylation/cyclization of aroyloxycarbamates to realize substituted indoles has been disclosed. Terminal alkynes as the coupling partners lead to site specific 2-substituted indoles through two pathways, while internal alkynes with aroyloxycarbamates can be transformed to 2,3-disubstituted indoles directly. This protocol is further demonstrated by the efficient synthesis of indoles as well as the success of employing inexpensive aryl acids as starting materials to construct C-N bonds by releasing CO2.
- Ma, Nuannuan,Li, Peihe,Wang, Zheng,Dai, Qipu,Hu, Changwen
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supporting information
p. 2421 - 2426
(2018/04/12)
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- Synthesis of indole-fused heteroacenes by cascade cyclisation involving rhodium(ii)-catalysed intramolecular C-H amination
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Heteroacenes are potentially important materials for organic electronics and their syntheses are of topical interest. Herein we report the development of a catalytic, redox-neutral reaction for the synthesis of the 5,10-dihydroindolo[3,2-b]indole class of
- Matsuda, Takanori,Ito, Hirotaka
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p. 6703 - 6707
(2018/09/29)
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- Diversely Substituted Quinolines via Rhodium-Catalyzed Alkyne Hydroacylation
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The Rh-catalyzed hydroacylative union of aldehydes and o-alkynyl anilines leads to 2-aminophenyl enones, and onward to substituted quinolines. The mild reaction conditions employed in this chemistry result in a process that displays broad functional group
- Neuhaus, James D.,Morrow, Sarah M.,Brunavs, Michael,Willis, Michael C.
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supporting information
p. 1562 - 1565
(2016/05/02)
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- Pyrimidine or pyridine pyridine ketone compound and its preparation method and application (by machine translation)
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The invention discloses a kind of type I of the pyrimidine or pyridine pyridine ketone compound and its preparation and application, which belongs to the technical field of pharmaceutical preparation. The compounds have high-efficient and selectively inhibit the cell cycle dependent kinases (Cdks) CDK4 and CDK6 active, and then by inhibiting CDK4/CDK6 prevent tumor cell division. Therefore, the compounds of this invention can be used for CDK4 and CDK6 the involved in cell cycle control disorders result in various diseases, especially suitable for the treatment of malignant tumors. (by machine translation)
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- Synthesis of 3,4-fused 2-quinolones from an (ortho-aminophenyl)propiolate via sequential cycloaddition/lactam formation
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An N-phthalimide-protected (ortho-aminophenyl)propiolate was prepared by the carboxylation of the corresponding silylalkyne precursor with carbon dioxide. The obtained propiolate was further transformed to various 3,4-fused 2-quinolones via cycloadditions and subsequent deprotection/lactam formation.
- Murayama, Tsukasa,Shibuya, Masatoshi,Yamamoto, Yoshihiko
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supporting information
p. 690 - 694
(2015/03/18)
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- Development of an Efficient Procedure for Indole Ring Synthesis from 2-Ethynylaniline Derivatives Catalyzed by Cu(II) Salts and Its Application to Natural Product Synthesis
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The development of efficient methods for the indole synthesis catalyzed by Cu(II) salts and its applications were investigated. Cu(OAc)2 has been proved to be the best catalyst for the synthesis of various 1-p-tolylsulfonyl or 1-methylsulfonylindoles, which have both electron-withdrawing and electron-donating groups on the aromatic ring and C2 position of indoles. For the primary aniline derivatives, Cu(OCOCF 3)2 showed good activities, while Cu(OAc)2 was a good catalyst for the cyclization of secondary anilines. This methodology could be applied to the sequential cyclization reaction for the compounds which have the electrophilic part in the same molecule. By prior treatment with KH, the sequential cyclization was realized to provide the tricyclic ring systems, but it was limited to five- and six-membered rings for the second cyclization. Finally, formal and total synthesis of hippadine with the Cu(II)-promoted indole synthesis as the key step was accomplished.
- Hiroya, Kou,Itoh, Shin,Sakamoto, Takao
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p. 1126 - 1136
(2007/10/03)
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- A concise synthesis of 7-substituted indoles
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7-Substituted indoles were synthesized by the basic cyclization of 6-substituted tert-butyl 2-(trimethylsilyiethynyl)phenylcarbamates which were derived by the lithiation of tert-butyl 2- (trimethylsilylethynyl)phenylcarbamate and the subsequent reaction with electrophiles.
- Kondo, Yoshinori,Kojima, Satoshi,Sakamoto, Takao
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p. 2741 - 2746
(2007/10/03)
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