Emura, Takashi Esaki, Toru Tachibana, Kazutaka Shimizu, Makoto Efficient Asymmetric Synthesis of Novel Gastrin Receptor Antagonist AG-041R via Highly Stereoselective Alkylation of Oxindole Enolates 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. oxindole enolates;Efficient Asymmetric Synthesis;AG;Gastrin;stereoselective alkylation reactions;tetrasubstituted chiral intermediates;core oxindole stereochemistry;bromoacetic acid esters 2006-10-27
    https://acs.figshare.com/articles/journal_contribution/Efficient_Asymmetric_Synthesis_of_Novel_Gastrin_Receptor_Antagonist_AG_041R_via_Highly_Stereoselective_Alkylation_of_Oxindole_Enolates/3051301
10.1021/jo061541v.s002