- BENZOPYRAZOLE COMPOUND USED AS RHO KINASE INHIBITOR
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The invention relates to a benzopyrazole compound used as RHO kinase inhibitor, a pharmaceutical composition and uses thereof for preparing an RHO kinase inhibiting drug, and more specifically to said compound of formula (I-1), a pharmaceutically acceptable salt and isomer thereof.
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Paragraph 0156-0157; 0162; 0206-0207; 0211
(2021/02/25)
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- Base-induced Sommelet–Hauser rearrangement of N-(α-(2-oxyethyl)branched)benzylic glycine ester-derived ammonium salts via a chelated intermediate
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The base-induced Sommelet–Hauser (S–H) rearrangement of N-(α-branched)benzylic glycine ester-derived ammonium salts 1 was investigated. When the α-branched substituent was a simple alkyl, such as a methyl or butyl, desired S–H rearrangement product 2 was obtained in low yield with formation of the [1,2] Stevens rearranged 4 and Hofmann eliminated products 5 and 6. However, when the α-branched substituent had a 2-oxy moiety, such as 2-acetoxyethyl or 2-benzoyloxyethyl, the yields of 2 were improved. These results could be explained by formation of chelated intermediate C that stabilizes the carbanionic ylide, and the subsequent initial dearomative [2,3] sigmatropic rearrangement would be accelerated. The existence of C was supported by mechanistic experiments. This enhancement effect is not very strong or effective; however, it will expand the synthetic usefulness of ammonium ylide rearrangements.
- Baba, Souya,Hirano, Kazuki,Tayama, Eiji
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supporting information
(2020/03/13)
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- Site-Specific C(sp3)–H Aminations of Imidates and Amidines Enabled by Covalently Tethered Distonic Radical Anions
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The utilization of N-centered radicals to synthesize nitrogen-containing compounds has attracted considerable attention recently, due to their powerful reactivities and the concomitant construction of C?N bonds. However, the generation and control of N-centered radicals remain particularly challenging. We report a tethering strategy using SOMO-HOMO-converted distonic radical anions for the site-specific aminations of imidates and amidines with aid of the non-covalent interaction. This reaction features a remarkably broad substrate scope and also enables the late-stage functionalization of bioactive molecules. Furthermore, the reaction mechanism is thoroughly investigated through kinetic studies, Raman spectroscopy, electron paramagnetic resonance spectroscopy, and density functional theory calculations, revealing that the aminations likely involve direct homolytic cleavage of N?H bonds and subsequently controllable 1,5 or 1,6 hydrogen atom transfer.
- Fang, Yuanding,Fu, Kang,Shi, Lei,Zhao, Rong,Zhou, Jia
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supporting information
p. 20682 - 20690
(2020/09/07)
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- A convenient synthesis of dihydro- and tetrahydro-1,3-thiazine derivatives from β-aryl-β-amino acids
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A facile synthesis of 2-alkyl-4-aryl-5,6-dihydro-4H-1,3-thiazines and cis-2-alkyl-4-aryl-3,4,5,6-tetrahydro-2H-1,3-thiazines with potential therapeutic interest was achieved starting from readily accessible β-aryl-β-amino acids.
- Leflemme, Nicolas,Dallemagne, Patrick,Rault, Sylvain
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p. 1503 - 1505
(2007/10/03)
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