Fluorinated alcohol mediated N,N'-dialkylation of amino acid derivatives via cascade [1,5]-hydride transfer/cyclization for concise synthesis of tetrahydroquinazoline.,Organic & Biomolecular Chemistry

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Fluorinated alcohol mediated N,N'-dialkylation of amino acid derivatives via cascade [1,5]-hydride transfer/cyclization for concise synthesis of tetrahydroquinazoline.
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020-01-09 , DOI: 10.1039/c9ob02498k
Hongjin Shi ₁ , Lubin Xu ₁ , Didi Ren ₁ , Liang Wang ₂ , Weisi Guo ₃ , Shuai-Shuai Li ₂

Affiliation

Structurally diverse amino acids and their ester derivatives were conveniently N,N'-dialkylated via a TFE-promoted cascade condensation/[1,5]-hydride transfer/cyclization for straightforward construction of pharmeutically significant tetrahydroquinazolines incorporating various amino acids, which featured broad substrate scope, the use of TFE as a sole solvent, additive-free and mild conditions.

中文翻译：

氟化醇通过级联的[1,5]-氢化物转移/环化作用介导氨基酸衍生物的N，N'-二烷基化，以简化四氢喹唑啉的合成。

通过TFE促进的级联缩合/ [1,5]-氢化物转移/环化反应，可以方便地将结构多样的氨基酸及其酯衍生物进行N，N'-二烷基化，以直接构建结合了多种氨基酸，具有广泛底物的药学上重要的四氢喹唑啉。范围，使用TFE作为唯一溶剂，无添加剂且条件温和。

更新日期：2020-02-13

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