100587-74-4Relevant articles and documents
Preparation method of 5, 6-methylenedioxy indole
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, (2021/03/31)
The invention provides a preparation method of 5, 6-methylenedioxy indole. The preparation method comprises the following steps: reacting 3, 4-methylenedioxy aniline serving as a raw material with benzene sulfonyl chloride to obtain A2, reacting A2 with 2, 2-dimethoxy-1-bromoethane to obtain a precursor A3 of a ring closing reaction, performing ring closing on A3 under the action of Lewis acid toobtain A4, and removing a protecting group of amino by using alkali to obtain the final 5, 6-methylenedioxy indole. according to the invention, 3, 4-methylenedioxy aniline is used as a raw material, nitro is prevented from being reduced into amino, the price of the compound is low, the cyclization reaction can be completed at normal temperature under the action of Lewis acid, and extreme conditions of high temperature or a strong reducing agent are avoided. The whole synthesis operation is simple, the post-treatment is easy, and the generated three wastes are few. The solvent in the reaction process can be reused, so that the cost is reduced, the operation is simple, the yield is higher, and the product with the purity of more than 98% can be obtained. The method is suitable for mass production and has obvious economic benefits.
Topically active carbonic anhydrase inhibitors. 3. Benzofuran- and indole-2-sulfonamides
Graham,Hoffman,Gautheron,Michelson,Scholz,Schwam,Shepard,Smith,Smith,Sondey,Sugrue
, p. 749 - 754 (2007/10/02)
Derivatives of benzofuran- and indole-2-sulfonamide were prepared for evaluation as topically active ocular hypotensive agents. These compounds were found to be excellent inhibitors of carbonic anhydrase and to lower intraocular pressure in a rabbit model