The invention relates to the technical field of organic
chemical synthesis, in particular to a 2-
sulfonyl aminopyrrole derivative and a preparation method thereof, and the preparation method comprises the following steps: in the presence of a
copper compound, performing one-pot reaction on an alpha-amino
acetophenone compound as shown in a formula (II), a terminal acetylenic
ketone compound as shown in a formula (III) and a
sulfonyl azide compound as shown in a formula (IV) to obtain the 2-
sulfonyl aminopyrrole derivative. The 2-sulfonyl aminopyrrole derivative as shown in the formula (I) is obtained. A
copper compound is used as a catalyst, no
oxidizing agent or
reducing agent needs to be added, under the promotion of alkali, an alpha-amino
acetophenone compound, terminal
alkyne ketone and a sulfonyl
azide compound are subjected to a one-pot reaction in an
organic solvent, and the 2-sulfonyl aminopyrrole derivative which is a diastereoisomer is obtained in one step. The preparation method has the advantages of one-pot reaction, simple and efficient reaction, diversified three-dimensional structure of the product, high yield, wide substrate application range, easiness in separation and purification of the product, good purity and wide industrial application prospect.