- Phosphine-catalyzed sequential (2+3)/(2+4) annulation of γ-vinyl allenoates: Access to the synthesis of chromeno[4,3-: B] pyrroles
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A phosphine-catalyzed cascade (2+3)/(2+4) cyclization reaction of γ-vinyl allenoates with aldimine esters has been developed to provide a series of chromeno[4,3-b]pyrrole derivatives that contain three contiguous stereogenic centers. The method gives a good yield, excellent chemoselectivity and diastereoselectivity under mild conditions.
- Huang, You,Li, Xiaohu
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supporting information
p. 9934 - 9937
(2021/10/12)
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- 3-substituted coumarin derivatives and their use
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The invention provides a 3-substituted coumarin derivative, and pharmaceutically acceptable salts, solvates, hydrates or crystal forms thereof. The above compound has a high calcium flow activity and a very good selectivity on a human derived cannabinoid receptor CB2, and is a specific agonist or inverse agonist of the cannabinoid receptor CB2. The compound is an active ligand of a novel cannabinoid II receptor CB2, and compounds of the above kind and pharmaceutically acceptable salts, solvates, hydrates or crystal forms thereof have high calcium flow activities and a very good selectivity on the human derived cannabinoid receptor CB2. The compound is the specific agonist or inverse agonist of the cannabinoid receptor CB2, and can be applied to the preparation of medicines for treating, preventing and inhibiting CB2 receptor mediated diseases. The structure of the derivative is represented by a general formula A shown in the specification.
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Paragraph 0088; 0089; 0090
(2016/10/08)
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- Design, syntheses, structure - Activity relationships and docking studies of coumarin derivatives as novel selective ligands for the CB2 receptor
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The CB2 receptor has been considered as an inspiring drug target for the treatment of pain and immune-related diseases. In the current manuscript, a novel series of coumarin derivatives is reported to be designed and synthesized by combining the structural features of some known ligands for the cannabinoid receptors based on the CoMFA model of the lead compounds. The compounds were evaluated to be highly selective ligands for the CB2 receptor over the CB1 receptor by calcium mobilization assays. Furthermore, SAR results Therefore, molecular docking simulations were performed to calculate the receptor-ligand interactions of our synthesized compounds binding to the CB2 receptor. The understanding of the binding modes could be advantageous for further development of selective ligands for the CB2 receptor.
- Han, Shuang,Zhang, Fei-Fei,Qian, Hai-Yan,Chen, Li-Li,Pu, Jian-Bin,Xie, Xin,Chen, Jian-Zhong
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- Efficient one-pot synthesis of ethyl [2-(2H-Chromene-3yl)-4-oxo-L,3- thiazolidin-3-yl]acetates
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Ethyl [2-(2H-chromene-3yl)-4-oxo-1,3-thiazolidin-3yl]acetates (6a-e) were synthesized in a single pot by the reaction of 2H-3-chromenecarbaldehydes (3a-e), glycine ethyl ester hydrochloride (4), and mercaptoacetic acid (5) in diisopropylethylamine/benzene under refluxing conditions in a Dean-Stark trap.
- Reddy, S. Satyanarayana,Krupadanam, G. L. David
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body text
p. 1305 - 1311
(2010/06/20)
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- Does the DABCO-catalysed reaction of 2-hydroxybenzaldehydes with methyl acrylate follow a Baylis-Hillman pathway?
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Evidence is presented which supports the intermediacy of dipolar Baylis-Hillman-type adducts in the synthesis of coumarin and chromene derivatives from the reaction of 2-hydroxybenzaldehydes with methyl acrylate in the presence of 1,4-diazabicyclo[2.2.2]octane (DABCO).
- Kaye, Perry T.,Musa, Musiliyu A.,Nocanda, Xolani W.,Robinson, Ross S.
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p. 1133 - 1138
(2007/10/03)
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- A mild and chemoselective dealkylation of alkyl aryl ethers by cerium(III) chloride-NaI
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The alkoxy groups present ortho to carbonyl group in alkoxybenzaldehydes are selectively deprotected in high yields leaving other alkoxy groups unaffected by cerium(III) chloride-NaI in refluxing acetonitrile under neutral reaction conditions.
- Yadav,Subba Reddy,Madan,Riaz Hashim
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p. 738 - 739
(2007/10/03)
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- Substituted benzopyran derivatives for the treatment of inflammation
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A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A1, A2, A3, A4, R, R'', R1 and R2 are as described in the specification.
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