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Reaction of 1,3,5-Triazinanes with Phosphoryl Diazomethanes: Access to 5-Phosphoryl-1,2,3,4-tetrahydropyrimidines

Wenlai Xie, Chengzhuo Wang, Jiaxi Xu

2024Organic Letters19 citationsDOI

Abstract

Conversion of 1,3,5-triazinanes into 5-phosporyl-1,2,3,4-tetrahydropyrimidines is achieved efficiently through the microwave-assisted reaction with phosphoryl diazomethanes. Both trialkyl and triaryl 1,3,5-triazinanes were converted by diazomethyldiarylphosphine oxides, dialkyl diazomethylphosphonates, and alkyl diazomethyl(aryl)phosphinates and functionalized simultaneously in good to excellent yields. The reaction is a sequence of 1,3,5-triazinane fragmentation, tandem nucleophilic addition of the generated formaldimines and phosphoryl diazomethanes, and final N, N -acetalization.

Topics & Concepts

ChemistryNucleophileAlkylArylMedicinal chemistryTandemFragmentation (computing)Reaction conditionsPhosphoryl chlorideMicrowave irradiationSequence (biology)Combinatorial chemistryOrganic chemistryCatalysisBiochemistryMaterials scienceComputer scienceOperating systemComposite materialSynthesis and Catalytic ReactionsClick Chemistry and ApplicationsChemical Synthesis and Analysis
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