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Benzopyran
About: Benzopyran is a research topic. Over the lifetime, 1889 publications have been published within this topic receiving 15235 citations.
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Patent•
17 Dec 2012
TL;DR: The OP-1074 as mentioned in this paper is a pure anti-estrogen when tested in the agonist mode and a complete anti -estrogen in the antagonist mode, which is the only compound known to have antiestrogenic activity.
Abstract: Benzopyran compounds with strong anti-estrogenic activity and essentially no estrogenic activity are provided, which are OP- 1038, which is 3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-l-yl]ethoxy}phenyl)-2H-chromen-7-ol, and OP-1074, which is (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin- 1 -yl]ethoxy}phenyl)-2H-chromen-7-ol. OP-1074 is a pure anti-estrogen when tested in the agonist mode and a complete anti-estrogen when tested in the antagonist mode. These compounds are useful for the treatment or prevention of a variety of conditions that are modulated through the estrogen receptor in mammals including humans.
11 citations
TL;DR: In this article, a short synthetic method for 3-substituted 9H-pyrido[3,4-b]indoles and isoquinolines was proposed using cycloaddition-elimination reactions between 3Hpyrano[3.4]-indol-3-ones 1 or 3H-2-benzopyran-3 -ones 6 and electron-poor nitriles as ethyl cyanoformate and p-toluenesulfonyl cyanide.
Abstract: A short synthetic method for 3-substituted 9H-pyrido[3,4-b]indoles 3 and isoquinolines 7 is proposed using cycloaddition-elimination reactions between 3H-pyrano[3,4-b]indol-3-ones 1 or 3H-2-benzopyran-3-ones 6 and electron-poor nitriles as ethyl cyanoformate and p-toluenesulfonyl cyanide. Extension of the method is possible neither with benzoyl cyanide nor with imines. The diene system undergoes cycloaddition with the carbonyl function of the former compound
11 citations
TL;DR: A mild and efficient protocol for the synthesis of the benzopyran ring has been described and a series of chromans compounds are reported, the yield is from 72% to 95% as mentioned in this paper.
Abstract: A mild and efficient protocol for the synthesis of the benzopyran ring has been described and a series of chromans compounds is reported, the yield is from 72% to 95%. The diadduct tended to angular product and showed good regioselectivity. This strategy was applied for the benzopyran derived natural products (±)-xyloketals and (±)-alboatrin. The crystal of compound 9 exhibited centro-symmetric space group, containing two isomers in one unit. The relative configurations were 1R,10R,15S and 34S,22R,30S, respectively.
11 citations
TL;DR: Out of all the compounds screened, compounds 16, 17, and 18 were found to be active against the virulent strain M. tubercolosis H37Rv displaying MIC in the range of 6.25–1.56 μg/ml against.
Abstract: A series of hybrid molecules (7–9, 12, 13, and 14–18) consisting of chromans and pyrolidines or cyclic amines were prepared either by (3 + 2) cycloaddition of nitrostyrenes and azomethine ylide or by three component reactions of chromanyl aldehydes, acetylenes, and cyclic amines. All the synthesized compounds were evaluated against both avirulent (H37Ra) and virulent (H37Rv) strains of Mycobacterium tuberculosis. Out of all the compounds screened, compounds 16, 17, and 18 were found to be active against the virulent strain M. tubercolosis H37Rv displaying MIC in the range of 6.25–1.56 μg/ml against.
11 citations
TL;DR: In this article, the unusual behavior of aryl 2-deoxy-D-galactopyranosides yielding two different products with BF 3 ·Et 2 O under different concentrations was reported.
11 citations