6484-23-7Relevant articles and documents
Method for synthesizing quinazolinone compound through visible light induction
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Paragraph 0077-0082, (2021/11/27)
The method is mild in reaction condition, simple and convenient in post-treatment operation, free of additional additives, high I in reaction efficiency, wide II in substrate adaptability, high in product purity, green and environment-friendly, and the method has III the advantages of mild reaction conditions, no need of additional additives, high reaction efficiency, wide substrate adaptability.
Discovery of Quinazolin-4(3 H)-ones as NLRP3 Inflammasome Inhibitors: Computational Design, Metal-Free Synthesis, and in Vitro Biological Evaluation
Abdullaha, Mohd,Mohammed, Shabber,Ali, Mehboob,Kumar, Ajay,Vishwakarma, Ram A.,Bharate, Sandip B.
, p. 5129 - 5140 (2019/04/16)
NLRP3 inflammasome is an important therapeutic target for a number of human diseases. Herein, computationally designed series of quinazolin-4(3H)-ones were synthesized using iodine-catalyzed coupling of arylalkynes (or styrenes) with O-aminobenzamides. The key event in this transformation involves the oxidative cleavage of the C-C triple/double bond and the release of formaldehyde. The reaction relies on the C-N bond formation along with the C-C bond cleavage under metal-free conditions. The nitro-substituted quinazolin-4(3H)-one 2k inhibited NLRP3 inflammasome (IC50 5 μM) via the suppression of IL-1β release from ATP-stimulated J774A.1 cells.
The mechanochemical synthesis of quinazolin-4(3H)-ones by controlling the reactivity of IBX
Alam, Md Toufique,Maiti, Saikat,Mal, Prasenjit
supporting information, p. 2396 - 2403 (2018/10/15)
Performing any synthesis using several arylamines and hypervalent iodine(V) reagents by direct mixing is unrealistic because of the high exothermic reaction or explosion. Herein we demonstrate, when anilines were substituted with an amide group at the orthoposition, successful chemical reactions could be performed due to intramolecular control. At maximum contact of the reacting substances, i.e., under solvent-free mechanochemical conditions, 2-aminobenzamides, aryl-, alkylaldehydes and the iodine(V) reagent o-iodoxybenzoic acid (IBX) led to substituted quinazolin-4(3H)-one derivatives in fair yields.