N鈥揘 Bond-Forming Cyclization for the One-Pot Synthesis of N-Aryl[3,4-d]pyrazolopyrimidines

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• 作者：Lindsay E. Evans ; Matthew D. Cheeseman ; Keith Jones
• 刊名：Organic Letters
• 出版年：2012
• 出版时间：July 6, 2012
• 年：2012
• 卷：14
• 期：13
• 页码：3546-3549
• 全文大小：234K
• 年卷期：v.14,no.13(July 6, 2012)
• ISSN：1523-7052

文摘

An efficient one-pot synthesis of N-aryl[3,4-d]pyrazolopyrimidines in good yield and under mild reaction conditions is described. By exploiting electron-deficient hydroxylamines, the substituted oxime products were formed with very high E-diastereoselectivity. The key step utilizes a cyclization reaction upon an oxime derived from hydroxylamine-O-sulfonic acid to form the N鈥揘 bond of the product.