Considering that DHPM substrates were easily synthesized by Biginelli three component coupling reaction of aryl aldehyde, β-ketoester, and thiourea, the present method provides a direct access toward diverse 2-arylthiopyrimidines which have been used as a prominent substructure of drug molecules. This cascade reaction of DHPM with aryl iodide proceeds presumably via sequential tautomerization, C–S cross-coupling, and oxidative dehydrogenation (oxidation followed by elimination). We have developed a Cu- catalyzed cascade reaction for the synthesis of fully substituted 2-arylthiopyrimidines from 3,4-dihydropyrimidine-2(1H)-thiones (DHPMs) under aerobic conditions. In the reactions, the aspects of no need of ligands has been particular advantage over other metal catalysis. Lee, Ok Suk Kim, Hyeji Sohn, Jeong-Hun [Chungnam National University, Daejeon (Korea, Republic of) Lee, Hee-Seung [KAIST, Daejeon (Korea, Republic of) Shin, Hyunik [Yonsung Fine Chemicals R and D Center, Suwon (Korea, Republic of)Ĭopper-catalyzed C–S cross-coupling reactions have been considered as powerful tools in synthetic chemistry and utilized for diverse heterocycle syntheses. Synthesis of Arylthiopyrimidines by Copper-catalyzed Aerobic Oxidative C-S Cross-couplingĮnergy Technology Data Exchange (ETDEWEB) Preliminary mechanistic studies distinguish this reaction from previously reported Cu-mediated reactions. A two-step copper-catalyzed decarboxylative protocol for converting allylic alcohols to trifluoromethanes is reported. However, this transformation typically requires four-step processes, specialty chemicals, and/or stoichiometric metals to access the trifluoromethyl-containing product. Given the prevalence and accessibility of alcohols, methods to convert alcohols to trifluoromethanes are desirable. The development of new synthetic fluorination reactions has important implications in medicinal, agricultural, and materials chemistries. Copper-catalyzed decarboxylative trifluoromethylation of allylic bromodifluoroacetates.
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