A Library of 3-Aryl-4,5-dihydroisoxazole-5-carboxamides

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• 作者：Melissa R. Jeddeloh ; Jason B. Holden ; Dustin H. Nouri ; Mark J. Kurth
• 刊名：Journal of Combinatorial Chemistry
• 出版年：2007
• 出版时间：November 2007
• 年：2007
• 卷：9
• 期：6
• 页码：1041 - 1045
• 全文大小：740K
• 年卷期：v.9,no.6(November 2007)
• ISSN：1520-4774

文摘

Parallel solution phase methods for the preparation of a 72-membered 3-aryl-4,5-dihydroisoxazole-5-carboxamide library is reported. The reaction order (nitrile oxide 1,3-dipolar cycloaddition followed by amide formation, or vice versa) was investigated both experimentally and computationally to determine which route would result in the highest yields, minimize purification efforts, and give higher 1,3-dipolar cycloaddition regioselectivity. Automated preparative HPLC was used to purify the final products to ≥90% purity on a 10+ mg scale.