221121-46-6

Upstream product

• 116622-90-3 2-(2,6-difluorophenyl)acetyl chloride 
• 85068-28-6 2,6-difluorophenylacetic acid 
• 6148-64-7 ethyl potassium malonate 
• 221121-33-1 2-(2,6-difluoro-phenyl)-1-imidazol-1-yl-ethanone 

Downstream Products

• 850075-94-4 2-amino-6-(2,6-difluorophenylmethyl)pyrimidin-4(3H)-one 
• 1281819-06-4 4-(4-(2,6-difluorobenzyl)-6-oxo-1,6-dihydropyrimidin-2-ylamino)benzonitrile 
• 1281819-15-5 4-(4-chloro-6-(2,6-difluorobenzyl)pyrimidin-2-ylamino)benzonitrile 
• 1281819-28-0 4-(4-amino-6-(2,6-difluorobenzyl)pyrimidin-2-ylamino)benzonitrile 
• 1281819-22-4 4-(4-(2,6-difluorobenzyl)pyrimidin-2-ylamino)benzonitrile 
• 221121-65-9 6-(2,6-difluorophenylmethyl)-3,4-dihydro-2-thioxopyrimidin-4(3H)-one 
• 221122-07-2 2-cyclohexylsulfanyl-6-(2,6-difluoro-benzyl)-3H-pyrimidin-4-one 
• 221122-06-1 2-cyclopentylthio-6-(2,6-difluorophenylmethyl)-3,4-dihydrogyrimidin-4-(3H)-one 
• 221122-04-9 6-(2,6-difluoro-benzyl)-2-isobutylsulfanyl-3H-pyrimidin-4-one 
• 221122-05-0 2-sec-butylsulfanyl-6-(2,6-difluoro-benzyl)-3H-pyrimidin-4-one 
• 221122-02-7 6-(2,6-difluoro-benzyl)-2-isopropylsulfanyl-3H-pyrimidin-4-one 
• 221122-01-6 6-(2,6-difluorophenylmethyl)-3,4-dihydro-2-methylthiopyrimidin-4(3H)-one 

Relevant academic research and scientific papers

Structural insight into the optimization of ethyl 5-hydroxybenzo[g]indol-3-carboxylates and their bioisosteric analogues as 5-LO/m-PGES-1 dual inhibitors able to suppress inflammation

The release of pro-inflammatory mediators, such as prostaglandines (PGs) and leukotrienes (LTs), arising from the arachidonic acid (AA) cascade, play a crucial role in initiating, maintaining, and regulating inflammatory processes. New dual inhibitors of 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase-1 (mPGES-1), that block, at the same time, the formation of PGE2 and LTs, are currently emerged as a highly interesting drug candidates for better pharmacotherapie of inflammation-related disorders. Following our previous studies, we here performed a detailed structure-based design of benzo[g]indol-3-carboxylate derivatives, disclosing several new key factors that affect both enzyme activity. Ethyl 2-(3,4-dichlorobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate (4b, RAF-01) and ethyl 2-(3,4-dichlorophenyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate (7h, RAF-02) emerged as the most active compounds of the series. Additionally, together with selected structure based analogues, both derivatives displayed significant in vivo anti-inflammatory properties. In conclusion, modeling and experimental studies lead to the discovery of new candidate compounds prone to further developments as multi-target inhibitors of the inflammatory pathway.

Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains

Following the disclosure of dihydro-alkoxy-, dihydro-alkylthio-, and dihydro-alkylamino-benzyl-oxopyrimidines (DABOs, S-DABOs, and NH-DABOs) as potent and selective anti-HIV-1 agents belonging to the non-nucleoside reverse transcriptase inhibitor (NNRTI)

Substituted 6-benzyl-4-oxopyrimidines, process for their preparation and pharmaceutical compositions containing them

The invention concerns novel substituted 6-benzyl-4-oxopyrimidines and pharmaceutically acceptable salts thereof. These compounds inhibit reverse transcriptase encoded by human immunodeficiency virus (HIV), and are useful to prevent and treat HIV infectio

Does the 2-methylthiomethyl substituent really confer high anti-HIV-1 activity to S-DABOs?

S-DABO derivatives containing the methylthiomethyl (MTM) group have been synthesized and tested for anti-HIV-1 activity in cell-based assay (MTT and p24 assays) and for their capability to target the HIV-1 reverse transcriptase in enzyme assays. Data of experiments lead to the conclusion that the introduction of a 2-MTM-thio side chain is not sufficient per se to significantly increase S-DABO's potency. Nevertheless, potent MTM-S-DABOs can be obtained by introducing a 2,6-difluorophenylmethyl moiety as a C-6 substituent.

5-alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3,4-dihydropyrimidin- 4(3H)-ones: Novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives

Molecular modeling analysis of compounds belonging to the recently published series of dihydro-alkoxy-benzyl-oxopyrimidines (DABOs), such as S- DABOs and DATNOs, gave support to the design of new 2,6-disubstituted benzyl- DABO derivatives as highly potent