On February 29, 2008, Bellezza, Francesca; Cipiciani, Antonio; Ruzziconi, Renzo; Spizzichino, Sara published an article.Recommanded Product: 141940-37-6 The title of the article was Nucleus- and side-chain fluorinated 3-substituted indoles by a suitable combination of organometallic and radical chemistry. And the article contained the following:
Regioselectively fluoro-, trifluoromethyl- and trifluoromethoxy-substituted 3-methyleneindolines e.g., I, have been prepared using a four-step procedure involving metalation/bromination of fluorinated Boc-protected anilines, N-propargylation of the resulting o-bromoarylcarbamate and reductive radical cyclization of the product with tributyltin hydride/AIBN. 3-Methyleneindolines, as valuable, versatile intermediates, can be transformed into highly functionalized 3-substituted indoles by ene-type reactions using different enophiles. Thus, fluoro-, trifluoromethyl- and trifluoromethoxy-substituted di-Et 2-hydroxy-2-[(1H-indol-3-yl)methyl]malonates, e.g., II, Et 2-hydroxy-3-(1H-indol-3-yl)propionates, e.g. III, and Et 2-hydroxy-3-(1H-indol-3-yl)-2-trifluormethylpropionates, e.g., IV, were obtained in 77-86% yield by simply heating the corresponding tert-Bu 3-methyleneindoline-1-carboxylate with an equimolar amount of di-Et ketomalonate, Et glyoxalate and Et 3,3,3-trifluoropyruvate, resp., at 100 °C, without solvent, for 0.5-4 h. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Recommanded Product: 141940-37-6
The Article related to aniline butyllithium carbon tetrabromide lithiation bromination, ortho bromo aniline preparation base propargyl bromide alkylation, propargyl aniline preparation aibn tributyltin hydride radical cyclization, indoline preparation enophile carbonyl ene reaction, indole hydroxy propionate derivative preparation, hydroxy malonate indole derivative preparation and other aspects.Recommanded Product: 141940-37-6
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