33245-78-2

Upstream product

• 1575-61-7 5-Chlorovaleroyl chloride 
• 151-10-0 1,3-Dimethoxybenzene 

Downstream Products

• 187396-92-5 5-chloro-1-(2,4-dimethoxy-5-nitrophenyl)-1-pentanone 
• 185376-97-0 N-{5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)pentanoyl]-2,4-dimethoxyphenyl}-4-trifluoromethylbenzenesulfonamide 
• 187397-00-8 N-[5-(5-chloropentanoyl)-2,4-dimethoxyphenyl]-4-trifluoromethylbenzenesulfonamide 

Relevant academic research and scientific papers

Synthesis and pharmacological evaluation of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as sigma-2 receptor ligands

Increasing evidences have implicated that sigma-2 receptor is a biomarker and significantly over-expressed in many proliferative cancer cells with no or low expression in normal cells. Sigma-2 receptor selective ligands have been successfully used as valuable tools to study its pharmacological functions, tumor imaging, and cancer therapeutics or adjuvants. 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinolinylalkyl benzamides are among a few categories of structures that have demonstrated high affinities and selectivities for sigma-2 receptor and been used extensively as study tools in various tumor imaging and therapy. As a continuous effort, we have synthesized a new series of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives and evaluated their affinities for both sigma-1 and sigma-2 receptors. Most of these newly developed analogs showed good to excellent binding affinities for sigma-2 receptor with no or low affinities for sigma-1 receptor. In particular, compounds 3b, 3e, 4b, and 4e demonstrated Ki values of 5–6 nM affinities and excellent selectivities for sigma-2 receptor. In addition, these analogs also demonstrated moderate anticancer activities against human liver Huh-7 tumor cells and human esophagus KYSE-140 cancer cells. But their cytotoxicities seem not to be correlated with their sigma-2 receptor affinities.

Tetrahydroisoquinoline derivatives preparation and application of (by machine translation)

The invention mainly relates to a series of containing tetrahydroisoquinoline structure the synthesis of the compounds and in the medical field of application. Specifically, the invention relates to a series of tetrahydroisoquinoline structure compound, it can inhibit the polymerization of A β, antagonizing A β O in combination and in nerve cells caused by the cytotoxic, therapeutic or improve AD has application prospect. (by machine translation)

Some benzenesulfonamido-substituted valerophenones that are selective antagonists for the 5-HT(2C) receptor

Substituted benzenesulfonyl derivatives of m-aminovalerophenones bearing a 1,3,8-triazaspiro[4.5]decane-2,4-dione at the alkyl terminus are the first known, selective ligands for the 5-HT(2C) receptor. A brief structure-activity relationship of this series is outlined.