A practical synthetic approach to the construction of a library of three isomeric/homologous β‐trifluoromethyl‐substituted pyrrolidines is disclosed. All products were prepared in multigram quantities from a common precursor. The key synthetic step was a [3+2] cycloaddition reaction. The influence of the trifluoromethyl group on the physicochemical characteristics of the pyrrolidine fragment was studied.
3,4,5,10,е][1,4]diazepin-1-ones are obtained by reaction of 3-(2-aminophenylamino)cyclohex-2-en-1-ones with arylglyoxal hydrates in 2-propanol. Also, several of their chemical properties (alkylation, acetylation, nitrosation) were investigated.
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