A new synthetic approach has been developed for efficient access to triarylmethanes by palladium catalyzed decarboxylative cross coupling reactions. The reaction features sp 2 -sp 3 coupling where benzoic acids upon decarboxylation reacted with diaryl methyl iodides having both electron donating and withdrawing functionalities, leading to the synthesis of diverse triarylmethanes. a Reaction conditions: Pd source (0.1 equiv.), ligand (0.2 equiv.), Ag 2 CO 3 (1.5 equiv.), arene carboxylic acid (1.2 equiv.), methyl iodide (1.0 equiv.), 100 C. b Reaction was performed at 65 C. c CuI additive (0.2 eq.) is used. d Pd catalyst (0.2 eq.) was used. e Reaction was performed at 120 C. f Overall isolated yield. g Nd means not determined.
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Tuberculosis (TB) is an infection caused by Mycobacterium tuberculosis (Mtb) and one of the deadliest infectious diseases in the world. Mtb has the ability to become dormant within the host and to develop resistance. Hence, new antitubercular agents are required to overcome problems in the treatment of multi-drug-resistant Tb (MDR-Tb) and extensively drug-resistant Tb (XDR-Tb) along with shortening the treatment time. Several efforts are being made to develop very effective new drugs for Tb, within the pharmaceutical industry, the academia and through public-private partnerships. This review will address the antitubercular activities, biological target, mode of action, synthetic approaches and thoughtful concept for the development of several new drugs currently in the clinical trial pipeline (up to October 2019) for tuberculosis. The aim of this review may be very useful in scheming new chemical entities (NCEs) for Mtb.
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