608510-29-8

Upstream product

• 55289-35-5 2-bromo-6-nitrotoluene 
• 95-92-1 oxalic acid diethyl ester 

Downstream Products

• 861213-76-5 4-(2-ethylphenyl)-1H-indole-2-carboxylic acid 
• 103858-52-2 4-bromo-1H-Indole-2-carboxylic acid ethyl ester 
• 16732-64-2 4-bromo-1H-indole-2-carboxylic acid 
• 608510-30-1 3-(2-bromo-6-nitro-phenyl)-propane-1,2-diol 
• 608510-36-7 2-({2-[3-(tert-butyl-dimethyl-silanyloxy)-2-hydroxy-propyl]-3-decyl-phenyl}-methyl-amino)-3-methyl-butyric acid benzyl ester 
• 608510-35-6 (S)-2-{[3-Decyl-2-(2,3-dihydroxy-propyl)-phenyl]-methyl-amino}-3-methyl-butyric acid benzyl ester 
• 608510-33-4 acetic acid 1-acetoxymethyl-2-(2-decyl-6-formylamino-phenyl)-ethyl ester 
• 608510-32-3 acetic acid 1-acetoxymethyl-2-(2-dec-1-ynyl-6-nitro-phenyl)-ethyl ester 
• 608510-34-5 3-(2-decyl-6-methylamino-phenyl)-propane-1,2-diol 
• 608510-31-2 acetic acid 1-acetoxymethyl-2-(2-bromo-6-nitro-phenyl)-ethyl ester 
• 98592-11-1 6-bromo-2-nitrophenylpyruvic acid 

Relevant academic research and scientific papers

Improved synthetic route for the GluN2-specific NMDA receptor glycine site agonist AICP

(R)-2-Amino-3-(4-(2-ethylphenyl)-1H-indole-2-carboxamido)propanoic acid (AICP) is a N-methyl-D-aspartate (NMDA) receptor glycine site agonist with unprecedented high potency in the low nanomolar range, and a GluN2 subunit-dependent pharmacological profile in terms of potency and agonist efficacy (Jessen et al., 2017 [1]). Here, we report a scalable, practical and cost-efficient synthetic route for AICP, which is an improvement compared to the previously reported route. This improved synthetic route includes a versatile diphenylmethylester (DPM) protection for the amino acid moiety, which can be widely used in the synthesis of other amino acid ligands. Further functional evaluation of AICP at the different ionotropic glutamate receptor (iGluR) classes demonstrates that high affinity binding of AICP to the orthosteric binding site is selective for NMDA receptors over AMPA and kainate receptors. Furthermore, high affinity binding of AICP is not observed at GluN3A, GluN3B, and GluD2 subunits, which also bind glycine and D-serine. Thus, the new approach described here enables scalable synthesis of AICP for the use as a pharmacological tool compound to study the involvement of neuronal NMDA receptor subtypes in normal brain function and disease.

Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes

Benzolactone-V8 (4) is a lactone analogue of the artificial tumor promoter benzolactam-V8 (1). To investigate the effect of hydrophobic substituents at positions 7 and 15 of 4 on binding selectivity for protein kinase C (PKC) isozymes, 7- and 15-decylbenz

Indoline Analogues of Idazoxan: Potent α2-Antagonists and α1-Agonists

The synthesis and α-adrenergic activity of a series of substituted 2-imidazolinylindolines are described.Substitution in the indoline ring generated compounds with a spectrum of adrenoceptor antagonist/agonist profiles that proved sensitive to both the nature and position of the substituent.Many of the derivatives possess greater presynaptic antagonist potency that the corresponding benzodioxan 1, dihydrobenzofuran 2, and indan 3 analogues; however, this α2-antagonism is often accompanied by α1-agonist activity.It was not possible to separate α2-antagonist from α1-agonist properties in this series.Compounds of most interest proved to be the N-ethyl 6, 5-chloro-N-methyl 18 and 5-chloro-N-ethyl 23 derivatives, all being potent α2-antagonists and α1-agonists.Substitution at the 4- and 7-position of the indoline ring generally gave compounds with nonselective agonist properties.