1122-74-3

Usage

Uses

4-iodo-2-(methylthio)pyrimidine is a useful research chemical.

InChI:InChI=1/C5H5IN2S/c1-9-5-7-3-2-4(6)8-5/h2-3H,1H3

Upstream product

• 49844-90-8 4-Chloro-2-methylthiopyrimidine 
• 823-09-6 2-(methylsulfanyl)pyrimidine 

Downstream Products

• 823-09-6 2-(methylsulfanyl)pyrimidine 
• 123061-49-4 2-(methylthio)-4-(tributylstannyl)pyrimidine 
• 136547-20-1 2-(methylthio)-4-(trifluoromethyl)pyrimidine 
• 16879-42-8 4-iodo-6-methyl-2-methylsulfanyl-pyrimidine 
• 234767-03-4 2,5-diphenyl-1-(methoxymethyl)-5-<4-(2-(methylthio)pyrimidinyl)>imidazole 
• 1074-68-6 4-formyl-2-(methylthio)pyrimidine 
• 250726-39-7 ethyl-2-methylsulfanylpyrimidine-4-carboxylate 
• 337902-89-3 2-(4-Fluorophenyl)-1-(2-methylthio-4-pyrimidinyl)-5-(4-tert-butoxycarbonyl-1-piperazinyl)imidazo[4,5-b]pyridine 
• 471844-88-9 2-(4-fluoro-phenyl)-5-(4-methoxy-benzyloxymethyl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-6,7-dihydro-5H-pyrrolo[1,2-a]imidazole 
• 471845-18-8 2-(4-fluoro-phenyl)-5-(4-methoxy-benzyloxymethyl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-6,7-dihydro-5H-pyrrolo[1,2-a]imidazole 
• 918870-23-2 (2-fluoro-phenyl)-(2-methylsulfanyl-pyrimidin-4-yl)-methanol 
• 895636-77-8 N-{3-[(2-methylthio-4-pyrimidinyl)ethynyl]phenyl}-2,6-difluorobenzamide 
• 234767-04-5 2,5-diphenyl-5-<4-(2-(methylthio)pyrimidinyl)>imidazole 
• 234767-06-7 2,5-diphenyl-5-<4-(2-(methylsulfonyl)pyrimidinyl)>imidazole 

Relevant academic research and scientific papers

Studies toward the total synthesis of the variolins: Rapid entry to the core structure

The pyrido[3′,2′:4,5]pyrrolo[1,2-c]pyrimidine core structure of the variolins has been synthesized in three steps from commercially available materials. The key reaction involves the deoxygenation and concomitant cyclization of a triarylmethanol using the

Structure–Activity Relationships of 2-Sufonylpyrimidines as Quorum-Sensing Inhibitors to Tackle Biofilm Formation and eDNA Release of Pseudomonas aeruginosa

Drug-resistant Pseudomonas aeruginosa (PA) strains are on the rise, making treatment with current antibiotics ineffective. Hence, circumventing resistance or restoring the activity of antibiotics by novel approaches is of high demand. Targeting the Pseudomonas quinolone signal quorum sensing (PQS-QS) system is an intriguing strategy to abolish PA pathogenicity without affecting the viability of the pathogen. Herein we report the structure–activity relationships of 2-sulfonylpyrimidines, which were previously identified as dual-target inhibitors of the PQS receptor PqsR and the PQS synthase PqsD. The SAR elucidation was guided by a combined approach using ligand efficiency and ligand lipophilicity efficiency to select the most promising compounds. In addition, the most effective inhibitors were rationally modified by the guidance of QSAR using Hansch analyses. Finally, these inhibitors showed the capacity to decrease biofilm mass and extracellular DNA, which are important determinants for antibiotic resistance.

In vitro identification of imidazo[1,2-a]pyrazine-based antileishmanial agents and evaluation of L. major casein kinase 1 inhibition

Leishmaniasis constitutes a severe public health problem, with an estimated prevalence of 12 million cases. This potentially fatal disease has a worldwide distribution and in 2012, the fatal Visceral Leishmaniasis (VL) was declared as new emerging disease in Europe, mainly due to global warming, with expected important public health impact. The available treatments are toxic, costly or lead to parasite resistance, thus there is an urgent need for new drugs with new mechanism of action. Previously, we reported the discovery of CTN1122, a potent imidazo[1,2-a]pyrazine-based antileishmanial hit compound targeting L-CK1.2 at low micromolar ranges. Here, we described structurally related, safe and selective compounds endowed with antiparasitic properties, better than miltefosine, the reference therapy by oral route. L-CK1.2 homology model gave the first structural explanations of the role of 4-pyridyl (CTN1122) and 2-aminopyrimidin-4-yl (compound 21) moieties, at the position 3 of the central core, in the low micromolar to nanomolar L-CK1.2 inhibition, whereas N-methylpyrazole derivative 11 remained inactive against the parasite kinase.

Pyrimidine-containing tri-substituted imidazole compound and application thereof

The invention relates to a pyrimidine-containing tri-substituted imidazole compound and application thereof. The compound has a structure shown as a formula (I). The compound can be used for effectively inhibiting EGFR (epidermal growth factor receptor) C797S mutation including EGFR ex19del/T790M/C797S and L858R/T790M/C797S; meanwhile, the compounds also have high inhibitory activity on single-point mutation L858R, ex19del and double-point mutation such as L858R/T790M, ex19del/T790M and the like, and moreover, the compounds have a weak inhibitory effect on wild EGFR (epidermal growth factor receptor), namely, the compounds have very good selectivity. The compound has potential to become a drug for treating malignant tumors carrying EGFR C797S mutation, especially non-small cell lung cancer(NSCLC), and has great application value.

Azine and Diazine Functionalization Using 2,2,6,6-Tetramethylpiperidino-Based Lithium-Metal Combinations: Application to the Synthesis of 5,9-Disubstituted Pyrido[3′,2′:4,5]pyrrolo[1,2- c ]pyrimidines

The synthesis of triaryl methanols was investigated by reacting different 4-metalated 2-substituted pyrimidines with diaryl ketones, the latter being generated by deprotocupration-aroylation of azine and diazine substrates. Cyclization of the triaryl meth

Synthesis of mono- and diaza-'pyridones' via stille coupling of alkoxystannanes

Various alkoxy-substituted heterocyclic stannanes provide access to the corresponding substituted 'pyridone' moieties via Stille cross-coupling. Both pyridyl and a series of diazinyl stannanes are prepared, and options for unmasking (via demethylation or debenzylation) of the pyridone unit are evaluated. Georg Thieme Verlag Stuttgart. New York.

Synthesis and antiproliferative activity of pyridinylcarbonylpyrimidines against melanoma cell line

The synthesis of the series of pyrimidinylamines 1a-d and pyrimidinylureas 1e-u bearing a novel pyridinylcarbonylpyrimidine scaffold and their antiproliferative activities against A375 human melanoma cell line were described. Among them, three compounds 1

Synthesis of cytimidine through a one-pot copper-mediated amidation cascade

A concise synthesis of cytimidine was developed utilizing tandem Cu-mediated N-aryl amidations followed by global deprotection. This sequence exploits a regioselective coupling of an iodobenzamide with a halopyrimidine that allows the union of three fragments in a single synthetic manipulation and will permit the efficient and rapid diversification of the cytimidine core.

2-Pyrimidinyl Pyrazolopyridine ErbB Kinase Inhibitors

The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.

MACROLIDES DERIVATIVES AS ANTIBACTERIAL AGENTS

The present invention provides macrolide derivatives, which can be used as antibacterial agents. Compounds described herein can be used for treating or preventing conditions caused by or contributed to by gram-positive, gram-negative or anaerobic bacteria