Best Daniel, Burns David J, Lam Hon Wai
School of Chemistry, University of Nottingham, University Park, Nottingham, NG7 2RD (UK).
Angew Chem Int Ed Engl. 2015 Jun 15;54(25):7410-3. doi: 10.1002/anie.201502324. Epub 2015 May 8.
A commercially available rhodium(II) complex catalyzes the direct arylation of 5-diazobarbituric acids with arenes, allowing straightforward access to 5-aryl barbituric acids. Free N-H groups are tolerated on the barbituric acid, with no complications arising from N-H insertion processes. This method was applied to the concise synthesis of a potent matrix metalloproteinase (MMP) inhibitor.
一种市售的铑(II)配合物催化5-重氮巴比妥酸与芳烃的直接芳基化反应,可直接制得5-芳基巴比妥酸。巴比妥酸上的游离N-H基团可耐受,不会因N-H插入过程而产生并发症。该方法应用于一种强效基质金属蛋白酶(MMP)抑制剂的简洁合成。