The Formation of Seven-Membered Heterocycles under Mild Pictet–Spengler Conditions: A Route to Pyrazolo[3,4]benzodiazepines

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• 作者：Timothy A. Katte ; Tristan A. Reekie ; William T. Jorgensen ; Michael Kassiou
• 刊名：Journal of Organic Chemistry
• 出版年：2016
• 出版时间：June 3, 2016
• 年：2016
• 卷：81
• 期：11
• 页码：4883-4889
• 全文大小：345K
• 年卷期：0
• ISSN：1520-6904

文摘

Reported is a method for the synthesis of seven-membered heterocycles via a Pictet–Spengler condensation reaction under very mild conditions. High substrate scope allows for use of aldehydes using catalytic amounts of acetic acid yielding 39–90% and ketones using catalytic amounts of trifluoroacetic acid yielding 25–83%.