- "TRPV1 VANILLOID RECEPTOR ANTAGONISTS WITH A BICYCLIC PORTION"
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The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active
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Page/Page column 111; 132
(2011/10/13)
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- NON NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
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The invention relates to compounds of formula (I) wherein Ar, X, R1, R2, R3 and R4 are as defined herein and, pharmaceutical compositions thereof useful, either alone or in combination with other therapeutic agents as reverse transcriptase inhibitors against wild type and single or double mutant strains of HIV for the treatment or prophylaxis of HIV infection
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Page/Page column 79
(2008/06/13)
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- Efficient reagents for the synthesis of 5-, 7-, and 5,7-substituted indoles starting from aromatic amines: Scope and limitations
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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.
- Ezquerra, Jesus,Pedregal, Concepcion,Lamas, Carlos,Barluenga, Jose,Perez, Marta,Garcia-Martin, Miguel Angel,Gonzalez, Jose M.
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p. 5804 - 5812
(2007/10/03)
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