70146-77-9

Upstream product

• 108-41-8 1-chloro-3-methylbenzene 
• 105-53-3 diethyl malonate 
• 587-04-2 m-Chlorobenzaldehyde 
• 766-80-3 1-bromomethyl-3-chlorobenzene 
• 620-20-2 1-Chloro-3-chloromethyl-benzene 
• 996-82-7 sodium diethylmalonate 

Downstream Products

• 683215-19-2 2-(3-chlorobenzyl)malonic acid 
• 21640-48-2 3-chlorohydrocinnamic acid 
• 1335027-61-6 6-[(3-chlorophenyl)methyl]-4H-[1,2,4]triazolo[1,5-a]pyrimidine-5,7-dione tri-n-butylamine salt 
• 1608506-16-6 C₁₇H₂₀ClNO₄ 
• 1608506-62-2 C₁₂H₁₄ClN₃O₂ 
• 1608506-52-0 C₁₂H₁₃ClN₄ 
• 1608506-32-6 C₁₂H₁₄ClNO 
• 1608506-24-6 C₁₄H₁₆ClNO₂ 
• 1608506-72-4 C₁₂H₁₃Cl₂N₃O 
• 1335026-71-5 5-butoxy-6-[(3-chlorophenyl)methyl]-4H-[1,2,4]triazolo[5,1-b]pyrimidin-7-one 
• 1335026-70-4 6-[(3-chlorophenyl)methyl]-5-methylsulfanyl-4H-[1,2,4]triazolo[5,1-b]pyrimidin-7-one 
• 1335026-63-5 5-chloro-6-[(3-chlorophenyl)methyl]-4H-[1,2,4]triazolo[5,1-b]pyrimidin-7-one 
• 1335026-62-4 6-[(3-chlorophenyl)methyl]-5-methoxy-4H-[1,2,4]triazolo[5,1-b]pyrimidin-7-one 
• 1335026-61-3 6-[(3-chlorophenyl)methyl]-5-pyrrolidin-1-yl-4H-[1,2,4]triazolo[5,1-b]pyrimidin-7-one 

Relevant academic research and scientific papers

Synthesis and insecticidal activity of mesoionic pyrido[1,2-α]pyrimidinone derivatives containing a neonicotinoid moiety

Mesoionic pyrido[1,2-α]pyrimidinone derivatives containing a neonicotinoid moiety were designed, synthesized, and evaluated for their insecticidal activity. Some of the title compounds showed remarkable insecticidal properties against Aphis craccivora. Compound I13 exhibited satisfactory insecticidal activity against A. craccivora. Meanwhile, label-free proteomics analysis of compound I13 treatment identified a total of 821 proteins. Of these, 35 proteins were up-regulated, whereas 108 proteins were down-regulated. Differential expressions of these proteins reflected a change in cellular structure and metabolism.

Unnatural α-amino ethyl esters from diethyl malonate or ethyl β-bromo-α-hydroxyiminocarboxylate

We have explored here the scope of the age-old diethyl malonate-based accesses to α-amino esters involving Knoevenagel condensations of diethyl malonate on aldehydes, reductions of the resulting alkylidenemalonates, the preparation of the corresponding α-hydroxyimino esters and their final reduction. This synthetic pathway turned out to be general although some unexpected limitations were encountered. The synthetic modifications of some of the intermediates - using Suzuki-Miyaura coupling or cycloadditions - before undertaking the oximation step - provided accesses to further α-amino esters. Moreover, other pathways to α-hydroxyimino esters were explored including an attempt to improve the cycloadditions between ethyl β-bromo-α-hydroxyiminocarboxylate and various alkylfuranes.

4H- [1, 2, 4] TRIAZOLO [5, 1 -B] PYRIMIDIN-7 -ONE DERIVATIVES AS CCR2B RECEPTOR ANTAGONISTS

The present invention relates to novel compounds for use in the compositions, to processes for their preparation, to intermediates useful in their preparation and to their use as therapeutic agents. The present invention also relates to pharmaceutical com

Modified pyrimidine glucocorticoid receptor modulators

The present invention provides a novel class of modified pyrimidine compounds and compositions and methods of using the compounds as glucocorticoid receptor modulators.

Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists

A series of 2,3-disubstituted indenes, which are analogues of the widely used histamine H1 receptor antagonist dimethindene, have been synthesized and studied as muscarinic and histamine receptor antagonists. The affinities of these compounds for the five human muscarinic receptor subtypes (M1-M5) and for human histamine H1 receptors were determined in radioligand binding studies using membranes from transfected Chinese hamster ovary (CHO) cells and [3H]N-methylscopolamine ([3H]NMS). The results demonstrate that the diisopropyl analogue 19 has a similar high affinity as (S)-dimethindene at M2 receptors ((S)-dimethindene: pKi = 7.52; (-)-19: pKi = 7.37) with an improved selectivity pattern ((S)-dimethindene: M2/M1 = 6-fold, M2/M3 = 5-fold, M2/M4 = 10-fold, M2/M5 = 25-fold; (-)-19: M2/M1 = 36-fold, M2/M3 = 96-fold, M2/M4 = 42-fold, M2/M5 = 275-fold). In addition, compound (-)-19 showed 35-fold lower affinity at histamine H1 receptors (pKi = 5.61) than (S)-dimethindene (pKi = 7.16). Another interesting compound is the fluoroethyl derivative 20 (pKi/M2 = 7.49), which also exhibits a higher M2 selectivity (M2/M1 = 19-fold; M2/M3 = 22-fold; M2/M4 13-fold; M2/M5 = 62-fold) than (S)-dimethindene. Unfortunately, compound 20 also shows a high affinity for histamine H1 receptors (pKi = 8.14). The compound with the highest affinity for M2 receptors (pKi = 7.91), the dimethylaminomethylene analogue 31, displayed only a small preference for M2 receptors. In conclusion, compound (-)-19 might be useful to test the hypothesis that blockade of muscarinic M2 receptors in the brain is a viable mechanism by which to produce improved cognition. This second-generation dimethindene analogue might also be the starting point for the development of M2-selective muscarinic antagonists useful for quantifying M2 receptors in the central nervous system with positron emission tomography imaging.