2,2,2-Trifluoroethyl Oxalates in the One-Pot Parallel Synthesis of Hindered Aliphatic Oxamides

Andrey V. Bogolubsky,Yurii S. Moroz,Pavel K. Mykhailiuk,Sergey E. Pipko,Alexander V. Grishchenko,Anton V. Zhemera,Anzhelika I. Konovets,Roman A. Doroschuk,Yurii V. Dmytriv,Olga A. Zaporozhets,Andrey Tolmachev

European Journal of Organic Chemistry（2016）

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摘要

A simple parallel synthesis approach to unsymmetrical N1,N2-substituted aliphatic oxamides using methyl (2,2,2-trifluoroethyl) oxalate and bis(2,2,2-trifluoroethyl) oxalate was developed. The method was validated on a 52-membered set of the oxamides, derived mainly from hindered primary and secondary aliphatic amines, and gave the products with a high overall success rate in moderate yields.

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关键词

Synthetic methods,Combinatorial chemistry,Amides,Amines,Esters,Aminolysis,Steric hindrance

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