Abstract

A straightforward one-pot approach to the synthesis of challenging 12-arylindolo[1,2-c]quinazolin-6(5H)-ones is described. Starting from readily available o-(o-aminophenylethynyl)trifluoroacetanilides, palladium-catalyzed aminoarylation of the triple bond with ArI, ArBr, and ArN₂ ⁺BF₄ ^– is followed by cyclization of the resulting N-trifluoro­acetyl-2-(o-aminophenyl)-3-aryl indole. This sequential reaction provides the title compounds by means of a rare elimination of trifluoromethane.

A straightforward one-pot approach to the synthesis of challenging 12-arylindolo[1,2-c]quinazolin-6(5H)-ones is described. Starting from readily available o-(o-aminophenylethynyl)trifluoroacetanilides, palladium-catalyzed aminoarylation of the triple bond with ArI, ArBr, and ArN₂ ⁺BF₄ ^– is followed by cyclization of the resulting N-trifluoro­acetyl-2-(o-aminophenyl)-3-aryl indole. This sequential reaction provides the title compounds by means of a rare elimination of trifluoromethane.

中文翻译：

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钯催化级联法合成12-（芳基）吲哚并[1,2-c]喹唑啉-6（5H）-ones

摘要

描述了一种简单的一锅法，用于合成具有挑战性的12-芳基吲哚并[1,2 - c ]喹唑啉-6（5 H）-。从容易获得的起始ø - （ø -aminophenylethynyl）trifluoroacetanilides，具有的Ar1，ARBR和ARN三键的钯催化aminoarylation ₂ ⁺ BF ₄ ^-之后的所得环化Ñ -三氟乙酰基-2-（ø氨基苯基）-3-芳基吲哚。该顺序反应通过罕见地消除三氟甲烷来提供标题化合物。

描述了一种简单的一锅法，用于合成具有挑战性的12-芳基吲哚并[1,2 - c ]喹唑啉-6（5 H）-。从容易获得的起始ø - （ø -aminophenylethynyl）trifluoroacetanilides，具有的Ar1，ARBR和ARN三键的钯催化aminoarylation ₂ ⁺ BF ₄ ^-之后的所得环化Ñ -三氟乙酰基-2-（ø氨基苯基）-3-芳基吲哚。该顺序反应通过罕见地消除三氟甲烷来提供标题化合物。