The last couple of decades has witnessed an incredible development in the progress of catalytic creation of triarylmethane (TRAM) motif. The broad‐spectrum applications of TRAMs in domains like medicinal chemistry, pharmacology, dyes, and functional materials has urged scientists to invent their efficient synthetic strategies. Herein, we have attempted to comprehensively document the catalytic methodologies for the synthesis of triarylmethanes which will satiate the anticipations of the readers who are looking for an update and stimulate the researches for further development.

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Although the synthesis of novel N-heterocyclic molecules is extremely demanding as well as challenging, the involvement of toxic solvents often triggers environmental safety concerns, resulting in process-engineering challenges. Herein, we have demonstrated a rapid, environmentally benign and energy efficient scalable method for the synthesis of 2,3-dihydroquinazolin-4­(1H)-one by grinding in a mortar pestle as well as mechanochemically via ball milling using p-TSA catalyst. The ability to accomplish the reaction in the absence of solvent via grinding or milling with p-TSA catalyst, with an immediate reduction in the cost and operational procedures, features the significant advantages of this protocol. The scalability and significance of the operational parameters during mechanochemical milling in the tubular ball mill were also demonstrated. Excellent yield in short duration, large substrate scope, product scalability, and easy recoverability are the prime features of this mechanochemical solvent-free protocol for the synthesis of 2,3-dihydroquinazolin-4­(1H)-one. The study also demonstrated the significant role of ball diameter to improve the efficiency of the milling operation in this mechanochemical synthesis.

The present work describes the design, synthesis, and evaluation of the anticancer properties of pyrazolone ring appended triarylmethanes by the condensation of diarylmethanols with pyrazolone in presence of a catalytic amount of p-TSA catalyst. The use of an inexpensive catalyst and accessing the desired product in good yields within a short span are the merits associated with this protocol. Furthermore, the in-silico, as well as in-vitro analysis and molecular docking of the designed molecules, were performed followed by their anticancer activity evaluation against cancer cell lines like MCF7, MDA-MB-231, HeLa, and DU-145. Few of the synthesized molecules demonstrated significant anticancer activity and could provide a new direction in the development of anti-cancer molecules.

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