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The stereoselective synthesis of 1,3‐diaminotruxillic acid derivatives has been achieved in high yields and short reaction times. The procedure starts from simple 5(4H)‐ oxazolones and is based on an efficient combination of CH orthopalladation, [2+2]‐photocycloaddition on continuous flow microreactors using visible light from LED sources, and hydrogenation to selectively afford the epsilon isomer...
The stereoselective synthesis of ε‐isomers of dimethyl esters of 1,3‐diaminotruxillic acid in three steps is reported. The first step is the ortho‐palladation of (Z)‐2‐aryl‐4‐aryliden‐5(4H)‐oxazolones 1 to give dinuclear complexes 2 with bridging carboxylates. The reaction occurs through regioselective activation of the ortho‐CH bond of the 4‐arylidene ring in carboxylic acids. The second step is...
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