A series of highly substituted tetrahydrofurans (THFs), decorated with modifiable 2 aryl, 3 carboxy and 4 amino substituents, has been prepared for biological evaluation within the European Lead Factory. Diastereoselective reductive amination of pre functionalised 4 oxofurans, readily prepared from cinnamate esters via oxa Michael/Dieckmann annulation, provided the requisite THF cores on gram scale with three Yeezy Discount contiguous stereocentres, including full substitution at C 3. In a second series, a pyrrolidine ring was fused to the same oxofuran scaffold via an intramolecular New Jordan Shoes 2020 reductive amination, inverting the configuration at C 4 relative to the other ring substituents.
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A series of highly substituted tetrahydrofurans (THFs), decorated with modifiable 2 aryl, 3 carboxy and 4 amino substituents, has been prepared for biological evaluation within the European Lead Factory. Diastereoselective reductive amination of pre functionalised 4 oxofurans, readily prepared from cinnamate esters via oxa Michael/Dieckmann annulation, provided the requisite THF cores on gram scale with three Yeezy Discount contiguous stereocentres, including full substitution at C 3. In a second series, a pyrrolidine ring was fused to the same oxofuran scaffold via an intramolecular New Jordan Shoes 2020 reductive amination, inverting the configuration at C 4 relative to the other ring substituents.
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