N-(3,6,6-Tриметил-1-пиридин-2-ил- 4,5,6,7-тетрагидро-1Н-индазол-4-ил)амиды карбоновых кислот

Synthesis of tetrahydroindazole derived amides via the Ritter reaction is discussed

A Facile Synthesis of 4-Acylamino-tetrahydroindazoles via the Ritter Reaction

A new route to the title compounds proceeds via reaction of 4-hydroxytetrahydroindazoles with various nitriles

A Facile Synthesis of 4-Acylamino-Tetrahydroindazoles via the Ritter Reaction

A new route toward 4-acylamino- and 4-amino-substituted tetrahydroindazoles is disclosed. The title compounds are obtained in good to excellent yields in the Ritter reaction between 4-hydroxy-tetrahydroindazoles and various nitriles. The reactivity of the tetrahydroindazole-derived carbenium ion is both sufficiently high to react with trichloroacetonitrile and sufficiently selective to resist the azide functionality within its structure. The present approach adds a method to the toolbox of tetrahydroindazole chemistry and facilitates the structural modifications of the scaffold, which has found important applications in medicinal chemistry