A highly selective H/D exchange reaction of 1,4-dihydropyridines
A highly selective H/D exchange reaction of 1,4-dihydropyridines
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1,4-二氢吡啶的高选择性H/D交换反应
DOI：
10.1039/c9ob00575g
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发表时间：
2019
影响因子：
3.2
通讯作者：
Liang Feng
中科院分区：
文献类型：
--
作者：
Wang Kaiqian;Chen Xiaoping;Peng Xiao;Wang Ping;Liang Feng
在此，我们报道了一种简单、经济、有效的酸介导方法，用于原位氘化Hantzsch酯及其4-取代衍生物，包括一些构成重要钙通道阻滞剂的药物，这些药物对高血压治疗有效。氢同位素交换选择性地发生在2,6取代基α-烷基C-H键上。
Herein, we report a simple, economical, and effective acid-mediated method for the in situ deuteration of Hantzsch esters and their 4-substituted derivatives, including some drugs that constitute important calcium channel blockers which are effective for hypertension treatment. Hydrogen isotope exchange occurred selectively at α-alkyl C–H bonds in the 2,6-substituents.