180624-11-7Relevant articles and documents
MANNOSE DERIVATIVES FOR TREATING BACTERIAL INFECTIONS
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Paragraph 000188, (2016/12/26)
The compounds represented by Formula (I) or pharmaceutically acceptable salts thereof: with U, W, X, Y, Z, p and ring A as defined in claim 1. Those compounds are useful for the treatment or prevention of bacteria infections. The variables of Formula (I) are as described herein. Pharmaceutically acceptable compositions comprise the compounds of Formula (I) or pharmaceutically acceptable salts thereof and pharmaceutically acceptable carriers, adjuvants, or vehicles. Methods of treating bacteria infections employ such compounds or pharmaceutically acceptable salts thereof.
Efficient reagents for the synthesis of 5-, 7-, and 5,7-substituted indoles starting from aromatic amines: Scope and limitations
Ezquerra, Jesus,Pedregal, Concepcion,Lamas, Carlos,Barluenga, Jose,Perez, Marta,Garcia-Martin, Miguel Angel,Gonzalez, Jose M.
, p. 5804 - 5812 (2007/10/03)
Upon reaction with IPy2BF4, 4-substituted anilines give regioselectively the corresponding o-iodoanilines in nearly quantitative yield, in a process that can be carried out on a multigram scale. Palladium-catalyzed coupling of the resulting 2-iodoanilines with (trimethylsilyl)acetylene (TMSA), followed by efficient CuI-mediated nitrogen cyclization onto alkynes with concurrent elimination of the TMS substituent, allows a straightforward elaboration of 5-mono- and 5,7-disubstituted indoles from aromatic amines. This new approach to the aforementioned indoles does not requires protective groups on nitrogen at any step and can be adapted for preparing related 7-monosubstituted indoles. Moreover, examples iterating the process are given, allowing bis-annulation and sequential double annulation and resulting in synthesis of benzodipyrroles. Additionally, suitable conditions for iodination of some of the target indoles with IPy2BF4 are discussed.
