10.1021/jo061541v.s001 Takashi Emura Takashi Emura Toru Esaki Toru Esaki Kazutaka Tachibana Kazutaka Tachibana Makoto Shimizu Makoto Shimizu Efficient Asymmetric Synthesis of Novel Gastrin Receptor Antagonist AG-041R via Highly Stereoselective Alkylation of Oxindole Enolates American Chemical Society 2006 oxindole enolates Efficient Asymmetric Synthesis AG Gastrin stereoselective alkylation reactions tetrasubstituted chiral intermediates core oxindole stereochemistry bromoacetic acid esters 2006-10-27 00:00:00 Dataset https://acs.figshare.com/articles/dataset/Efficient_Asymmetric_Synthesis_of_Novel_Gastrin_Receptor_Antagonist_AG_041R_via_Highly_Stereoselective_Alkylation_of_Oxindole_Enolates/3051307 An efficient method for asymmetric synthesis of the potent Gastrin/CCK-B receptor antagonist AG-041R was developed. Core oxindole stereochemistry was established by asymmetric alkylation of oxindole enolates with bromoacetic acid esters, using <i>l</i>-menthol as a chiral auxiliary. The key alkylation reaction of the oxindole enolates generated tetrasubstituted chiral intermediates with high diastereoselectivity. The stereoselective alkylation reactions are described in detail.