Synthesis of pyrimido[4,5-c]azepine- and pyrimido[4,5-c]oxepine-based γ-secretase modulators

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• 作者：Yong-Jin Wu ; ^{Yong-Jin.wu@bms.com" class="auth_mail" title="E-mail the corresponding author} ; Yunhui Zhang ; Jeremy H. Toyn ; John E. Macor ; Lorin A. Thompson
• 关键词：γ-Secretase modulator (GSM) ; 2-Chloro-pyrimido[4 ; 5-c]azepin-4-amine ; 2-Chloro-pyrimido[4 ; 5-c]oxepin-4-amine ; Ring-closing metathesis (RCM)
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 March 2016
• 年：2016
• 卷：26
• 期：6
• 页码：1554-1557
• 全文大小：889 K

文摘

This Letter describes an efficient ring-closing metathesis approach to 2-chloro-4-amino-pyrimido[4,5-c]azepines and 2-chloro-4-amino-pyrimido[4,5-c]oxepines. These chlorides were applied to the synthesis of several potent γ-secretase modulators (GSMs).