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Efficient Asymmetric Synthesis of Novel Gastrin Receptor Antagonist AG-041R via Highly Stereoselective Alkylation of Oxindole Enolates

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NIAID Data Ecosystem2026-03-06 收录
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https://figshare.com/articles/dataset/Efficient_Asymmetric_Synthesis_of_Novel_Gastrin_Receptor_Antagonist_AG_041R_via_Highly_Stereoselective_Alkylation_of_Oxindole_Enolates/3051307
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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 l-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.
创建时间:
2006-10-27
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