- Discovery and Development of a Series of Pyrazolo[3,4- d]pyridazinone Compounds as the Novel Covalent Fibroblast Growth Factor Receptor Inhibitors by the Rational Drug Design
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Alterations of fibroblast growth factor receptors (FGFRs) play key roles in numerous cancer progression and development, which makes FGFRs attractive targets in the cancer therapy. In the present study, based on a newly devised FGFR target-specific scorin
- Wang, Yulan,Dai, Yang,Wu, Xiaowei,Li, Fei,Liu, Bo,Li, Chunpu,Liu, Qiufeng,Zhou, Yuanyang,Wang, Bao,Zhu, Mingrui,Cui, Rongrong,Tan, Xiaoqin,Xiong, Zhaoping,Liu, Jia,Tan, Minjia,Xu, Yechun,Geng, Meiyu,Jiang, Hualiang,Liu, Hong,Ai, Jing,Zheng, Mingyue
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- 5-MEMBERED HETEROCYCLE FUSED WITH [3,4-D]PYRIDAZINONE, AND MANUFACTURING METHOD, PHARMACEUTICAL COMPOSITION, AND APPLICATION THEREOF
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The present invention provides a compound comprising a 5-membered heterocycle fused with a pyridazinone, wherein the compound is used as an FGFR kinase inhibitor, and a manufacturing method and application thereof. The invention specifically provides a co
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Paragraph 0102; 0103
(2019/04/29)
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- New One-Pot Synthesis of Polysubstituted Benzofurans and Benzo-1,4-dioxines
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It has been revealed that the copper(II) triflate catalyzed reaction of ethyl-2-diazo-3-oxobutanoate with phenols followed by cyclization of the intermediate enol in the presence of polyphosphoric acid is a simple and efficient method of synthesis of polysubstituted benzofurans. The use of pyrocatechol leads to the corresponding substituted 1,4-benzodioxine-2-carboxylates as major products.
- Sakhabutdinova,Raskil’dina,Zlotskii,Sultanova
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p. 233 - 236
(2018/11/21)
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- Benzofuran Derivatives. Part 4. Synthesis of Benzofurans and 2,3,4,5-Tetrahydro-1-benzoxepin-3,5-diones
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By treatment of ethyl 4- or 5-substituted 2-acetylphenoxyacetates 1 with potassium hydroxide in dry dioxane, benzofurans 2-7 and 2,3,4,5-tetrahydro-1-benzoxepin-3,5-diones 8 were obtained.The relative yields of benzofurans 2-7 and 2,3,4,5-tetrahydro-1-benzoxepin-3,5-diones 8 varied with the types of 4- or 5-substituents.The electron-donating 4-methoxyl group favored the formation of benzoxepins.On the other hand, electron-withdrawing substituents such as the 4-nitro group favored the formation of benzofurans.When esters 1 were treated with sodium amide,2,3-dihydrobenzofurans 2 were obtained exclusively regardless of 4- or 5-substituents.
- Suzuki, Tsuneo,Tanemura, Kiyoshi,Horaguchi, Takaaki,Shimimizu, Takahachi,Sakakibara, Tohru
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p. 423 - 429
(2007/10/02)
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