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



