57056-90-3Relevant academic research and scientific papers
Synthesis of Difluoroalkylated Benzofuran, Benzothiophene, and Indole Derivatives via Palladium-Catalyzed Cascade Difluoroalkylation and Arylation of 1,6-Enynes
Zhang, Pengbo,Wang, Chen,Cui, Mengchao,Du, Mengsi,Li, Wenwu,Jia, Zexin,Zhao, Qian
, p. 1149 - 1154 (2020)
A novel and efficient method for the synthesis of difluoroalkylated benzofuran, benzothiophene, and indole derivatives via palladium-catalyzed aryldifluoroalkylation of 1,6-enynes with ethyl difluoroiodoacetate and arylboronic acids has been established.
Visible-Light-Induced Cyclization/Aromatization of 2-Vinyloxy Arylalkynes: Synthesis of Thio-Substituted Dibenzofuran Derivatives
Chen, Hui,Chen, Yanyan,Mo, Zuyu,Xu, Yanli,Yan, Yunyun,Zhang, Niuniu
supporting information, p. 376 - 381 (2021/01/13)
A visible-light-induced cascade reaction of 2-vinyloxy arylalkynes with thiosulfonates was developed and provided unexpected thio-substituted dibenzofuran derivatives in moderate yields. Mechanistic studies revealed the thiosulfonylation product of 2-vinyloxy arylalkyne was the key intermediate, and the additive disulfide played the role of hydrogen abstraction in the aromatization process to offer the desired product. This reaction presents a new reaction mode for the construction of polycyclic oxygen heterocycles.
SPIROCYCLIC TETRAHYDROQUINAZOLINES
-
Paragraph 0595; 0601-0603, (2021/07/17)
Provided are compounds represented by Formula I, wherein R3, A, A1, A2, A3, E, E1, E2, L, Q, Z, and (aa) are as defined in the specification, and the pharmaceutically acceptable salts and solvates thereof. Compounds of Formula (I) are KRAS inhibitors and are thus useful to treat cancer and other diseases.
Spirocyclic tetrahydroquinazolines
-
Paragraph 0882; 0890-0892, (2021/07/11)
The invention discloses spirocyclic tetrahydroquinazolines , and particularly provide compounds represented by Formula I shown in the specification, and pharmaceutically acceptable salts and solvates thereof. In the formula, R3, A, A1, A2, A3, E, E1, E2, L, Q, Z and a structure shown in the specification are as defined in the specification,. The compounds of formula I are KRAS inhibitors and are therefore useful in the treatment of cancer and other diseases.
Synthesis of 2-isoxazolyl-2,3-dihydrobenzofuransviapalladium-catalyzed cascade cyclization of alkenyl ethers
Zhou, Fei,Li, Can,Li, Meng,Jin, Yangbin,Jiang, Huanfeng,Zhang, Yingjun,Wu, Wanqing
supporting information, p. 4799 - 4802 (2021/05/25)
A novel palladium-catalyzed cascade cyclization reaction of alkenyl ethers with alkynyl oxime ethers for the construction of poly-heterocyclic scaffolds has been developed, in which the electron-rich alkene moiety functions as a three-atom unit, simultaneously dealing well with the coordination and regioselectivity of electron-rich olefins under metal catalysis. The strategy features excellent regio- and chemoselectivities as well as good functional group tolerance. Moreover, the newly formed 2-isoxazolyl-2,3-dihydrobenzofuran products can be further transformed to diverse complex heterocycles, demonstrating their potential applications in organic synthesis and medicinal chemistry.
Polysubstituted benzodihydrofuro heterocyclic compound and preparation method and application thereof
-
Paragraph 0047; 0049, (2020/06/16)
The invention belongs to the technical field of organic synthesis, and discloses a polysubstituted benzodihydrofuro heterocyclic compound and a preparation method and application thereof. The preparation method comprises the following steps: adding a palladium salt catalyst, an oxidizing agent, an additive and alkali into a reactor, performing dissolving into an organic solvent, performing stirring to react at 50-70 DEG C, and separating and purifying the reaction product to obtain the polysubstituted benzodihydrofuro heterocyclic compound, the reaction formula of the preparation method is shown as a formula (I). According to the method, the alkyne ketoxime ether and the o-iodophenyl alkenyl ether which are simple and easy to obtain are used as reaction raw materials to synthesize a seriesof polysubstituted benzodihydrofuro heterocyclic compounds, and the method has the characteristics of simple and easy-to-obtain raw materials, convenience in operation, mild conditions, high step economy, wide substrate applicability, good functional group tolerance and the like.
Ag-Catalyzed Oxidative Cyclization Reaction of 1,6-Enynes and Sodium Sulfinate: Access to Sulfonylated Benzofurans
Wu, Wanqing,Yi, Songjian,Huang, Wei,Luo, Di,Jiang, Huanfeng
supporting information, p. 2825 - 2828 (2017/06/07)
A convenient protocol for the synthesis of sulfonylated benzofurans via Ag-catalyzed oxidative cyclization has been established. Chemically stable and easily available sodium sulfinates were used as the sulfonylation reagents and building block for the heterocycle construction. With this novel strategy, various benzofurans bearing dual functional groups could be obtained in good yields with high chemo- and regioselectivities under mild conditions.
The Pd-catalyzed synthesis of benzofused carbo- and heterocycles through carbene migratory insertion/carbopalladation cascades with tosylhydrazones
Paraja, Miguel,Carmen Pérez-Aguilar,Valdés, Carlos
supporting information, p. 16241 - 16243 (2015/11/10)
The Pd-catalyzed reaction between o-iodoallylbenzene and tosylhydrazones gives rise to indene derivatives through a process that involves a carbene migratory insertion followed by an intramolecular carbopalladation, with the formation of two C-C bonds on
Rhodium-catalyzed intramolecular cyclization of naphthol- or phenol-linked 1,6-enynes through the cleavage and formation of sp2 C-O bonds
Sakiyama, Norifumi,Noguchi, Keiichi,Tanaka, Ken
supporting information; experimental part, p. 5976 - 5980 (2012/07/03)
Put a ring on it: A cationic rhodium(I)/binap complex catalyzes the intramolecular cyclization reactions of naphthol- or phenol-linked 1,6-enynes to produce vinylnaphtho- or vinylbenzofurans and vinylnaphtho- or vinylbenzopyrans through the cleavage and f
