- Cedar camphor derivative as well as preparation method and application thereof
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The invention relates to the technical field of synthetic drugs, in particular to a cedar camphor derivative as well as a preparation method and an application thereof. The cedar camphor derivative isany one of compounds shown in the following structural formula, tautomers, hydrates, solvates or pharmaceutically acceptable salts thereof, and the cedar camphor derivative has a good treatment effect on viruses, especially influenza viruses, so that the application range of the cedar camphor and the derivatives thereof is expanded, and the variety of the cedar camphor derivatives is expanded.
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- Scalable and sustainable electrochemical allylic C-H oxidation
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New methods and strategies for the direct functionalization of C-H bonds are beginning to reshape the field of retrosynthetic analysis, affecting the synthesis of natural products, medicines and materials. The oxidation of allylic systems has played a prominent role in this context as possibly the most widely applied C-H functionalization, owing to the utility of enones and allylic alcohols as versatile intermediates, and their prevalence in natural and unnatural materials. Allylic oxidations have featured in hundreds of syntheses, including some natural product syntheses regarded as € classics €. Despite many attempts to improve the efficiency and practicality of this transformation, the majority of conditions still use highly toxic reagents (based around toxic elements such as chromium or selenium) or expensive catalysts (such as palladium or rhodium). These requirements are problematic in industrial settings; currently, no scalable and sustainable solution to allylic oxidation exists. This oxidation strategy is therefore rarely used for large-scale synthetic applications, limiting the adoption of this retrosynthetic strategy by industrial scientists. Here we describe an electrochemical C-H oxidation strategy that exhibits broad substrate scope, operational simplicity and high chemoselectivity. It uses inexpensive and readily available materials, and represents a scalable allylic C-H oxidation (demonstrated on 100 grams), enabling the adoption of this C-H oxidation strategy in large-scale industrial settings without substantial environmental impact.
- Horn, Evan J.,Rosen, Brandon R.,Chen, Yong,Tang, Jiaze,Chen, Ke,Eastgate, Martin D.,Baran, Phil S.
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- Functionalisation of Saturated Hydrocarbons. Part IX. Oxidation of Cedrol, β- and γ-Eudesmol, Sclareol, Manoyl Oxide, 1,9-Dideoxyforskolin, Methyl trans-Dihydrojasmonate, and Tetrahydrolinalool by the 'Gif System'
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The oxidation of cedrol (1), β- and γ-eudesmol (6 and 7, resp.), sclareol (14), manoyl oxide (15), 1,9-dideoxyforskolin (22) (+/-)-methyl trans-dihydrojasmonate (28), and tetrahydrolinalool (32), nearly all of natural terpenoid origin, by the 'Gif system' has afforded a number of novel products (3, 11, and 12, 16/17, 18/19, 26, 29-31, and ketones corresponding to 34-35, resp.).The structures of these compounds were established by spectroscopic techniques including 2D-NMR and, where appropriate, by comparison with authentic samples.
- Barton, Derek H. R.,Beloeil, Jean-Claude,Billion, Annick,Boivin, Jean,Lallemand, Jean-Yves,et al.
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p. 2187 - 2200
(2007/10/02)
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