2,3-Disubstitutedindoles can be prepared in moderate to excellent yields by reacting readily available o-alkynyltrifluoroacetanilides with aryl chlorides in MeCN at 120 °C in the presence of Pd2(dba)3 and Xphos.
<b>Preparation of Indoles from </b>
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<b>-Alkynyltrifluoroacetanilides Through the Aminopalladation-Reductive Elimination Process</b>
作者:Sandro Cacchi、Giancarlo Fabrizi、Luca Parisi
DOI:10.1055/s-2004-815993
日期:——
The functionalized pyrrole nucleus contained in the indole system has been assembled via the palladium-catalyzed reaction of o-alkynyltrifluoroacetanilides with organic halides/triflates or allyl carbonates. In the presence of carbon monoxide, a three-component reaction can take place and indole derivatives incorporating a molecule of carbon monoxide have been obtained.
2-Substituted 3-Aryl- and 3-Heteroarylindoles by the Palladium-Catalyzed Reaction of<i>o</i>-Trifluoroacetanilides with Aryl Bromides and Triflates.
作者:Sandro Cacchi、Giancarlo Fabrizi、Doriano Lamba、Fabio Marinelli、Luca M. Parisi
DOI:10.1055/s-2003-38079
日期:——
The palladium-catalyzed reaction of aryl and heteroaryl bromides and triflates with o-alkynyltrifluoroacetanilides affords 2-substituted 3-aryl- and heteroarylindoles usually in excellent yield. The procedure can be applied to the synthesis of 2-substituted indole-3-carboxaldehydes.
Benzodiazepine analogs for treating panic syndrome and for directly inducing analgesia
申请人:MERCK & CO. INC.
公开号:EP0434364A2
公开(公告)日:1991-06-26
Benzodiazepine analogs of the formula:
are disclosed which are antagonists of gastrin and cholecystokinin (CCK) and have properties useful for treating panic syndrome and for directly inducing analgesia.
The invention relates to compounds of formula (1) which are suitable for use in electronic devices, and to electronic devices, in particular organic electroluminescent devices, containing said compounds.