928118-80-3

Upstream product

• 110-89-4 piperidine 
• 36746-07-3 2-chloro-4-methyl-6-phenylpyrimidine-5-carboxylic acid ethyl ester 
• 123237-03-6 ethyl 6-methyl-4-phenyl-3,4-dihydropyrimidin-2(1H)-one-5-carboxylate 
• 69207-36-9 ethyl 6-methyl-4-phenylpyrimidin-2(1H)-one-5-carboxylate 
• 69207-36-9 ethyl 2-hydroxy-4-methyl-6-phenylpyrimidine-5-carboxylate 
• 123043-88-9 5-ethoxycarbonyl-4-phenyl-6-methyl-3,4-dihydropyrimidine-2(1H)-thione 
• 1245716-47-5 ethyl 4-methyl-6-phenyl-2-(tosyloxy)pyrimidine-5-carboxylate 

Relevant academic research and scientific papers

Cu-Catalyzed Direct Amination of Cyclic Amides via C-OH Bond Activation Using DMF

Herein, we describe a Cu-catalyzed approach to directly accessing aromatic heterocyclic amines from cyclic amides. The most-reported methods for cyclic amide conversions to aromatic heterocyclic amines use an activating group, such as a halogen atom or a

Copper(i) chloride promoted Csp2-N cross-coupling of 1,2-di(pyrimidin-2-yl) disulfides with amines: An efficient approach to obtain C2-amino functionalized pyrimidines

The copper(i)-promoted cross-coupling of 1,2-di(pyrimidin-2-yl) disulfides with aromatic amines and aliphatic amines to deliver C-N coupling products in moderate to good yields is reported in this paper. Central to this strategy is the conversion of disulfides into aryl- and alkyl amines by a copper-promoted chemoselective C-S bond cleavage.

Nucleophilic Substitution Reaction of Pyrimidin-2-yl Phosphates Using Amines and Thiols as Nucleophiles Mediated by PEG-400 as an Environmentally Friendly Solvent

A metal-free synthesis of C2-functionalized pyrimidines via the reaction of pyrimidin-2-yl phosphates with amines and thiophenols in PEG-400 has been developed. The desired products can be generated in good to excellent yields in the environmentally friendly PEG-400, without any catalysts or other additives.

Molecular iodine-mediated S-N and C-N cross-coupling and oxidative aromatization of 3,4-dihydropyrimidin-2(1H)-thiones with secondary amines

A domino S-N and C-N coupling/oxidative aromatization process to synthesize 2-aminothio-phenylpyrimidines and 2-amino-phenylpyrimidines by S-N and C-N cross-coupling reactions is described. This methodology couples 3,4-dihydropyrimidine-2-thiones and secondary amines catalyzed by molecular iodine. Remarkably the C-N coupled product was obtained via a desulfitative coupling-aromatization reaction in one-pot reaction.

Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity

A series of pyrimidine derivatives bearing amine substituents at C-2 position were obtained from Biginelli 3,4-dihydropyrimidin-2(1H)-ones and the effect of structural variation on anti-TB activity against Mycobacterium tuberculosis H37Rv strai

Synthesis of C2-functionalized pyrimidines from 3,4-dihydropyrimidin-2(1H)- ones by the Mitsunobu coupling reaction

The Biginelli 3,4-dihydropyrimidin-2(1H)-one was converted to various C2-multifunctionalized pyrimidines via the dehydrogenation and Mitsunobu reaction using amines, alcohols, phenols and carboxylic acids as nucleophiles. A possible mechanism was also proposed to rationalize the formation of products.

Synthesis of 2-substituted pyrimidines via cross-coupling reaction of pyrimidin-2-yl sulfonates with nucleophiles in polyethylene glycol 400

A mild and rapid procedure to the synthesis of 2-substituted pyrimidines was developed via sequential functionalization of easily available Biginelli 3,4-dihydropyrimidine-2(1H)-ones via oxidation, esterification, followed by cross-coupling reaction of pyrimidin-2-yl sulfonates with N, S, and O nucleophiles in PEG-400 as a green reaction medium at room temperature. Georg Thieme Verlag Stuttgart New York.