474645-96-0

Upstream product

• 343798-02-7 (1-benzotriazol-1-yl-propyl)-(4-trifluoromethyl-phenyl)-amine 
• 84713-20-2 benzyl N-vinylcarbamate 
• 474645-97-1 (R)-3-aminopentanenitrile methanesulfonic acid salt 
• 474645-91-5 (R)-3-((4-(trifluoromethyl)phenyl)amino)pentanenitrile 
• 667937-05-5 (3R)-3-(4-trifluoromethylphenylamino)pentanoic acid amide 
• 455-14-1 4-trifluoromethylphenylamine 
• 123-38-6 propionaldehyde 
• 400090-60-0 (R)-3-aminopentanenitrile 
• 98-56-6 4-chlorobenzotrifluoride 

Downstream Products

• 880145-77-7 (2R,4S)-[4-(4-benzyloxycarbonylamino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carbonyl)-cyclohexyl]-acetic acid ethyl ester 
• 1140966-17-1 (2R,4S)-4-benzyloxycarbonylamino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester 
• 874501-92-5 C₂₆H₂₄F₉N₃O₂ 
• 874502-03-1 C₃₀H₃₁F₉N₆O₂ 
• 874501-96-9 C₂₈H₂₆F₉N₇O₂ 
• 874502-50-8 C₂₉H₂₈F₉N₇O₂ 
• 874502-29-1 C₂₈H₂₈ClF₉N₆O₂ 
• 874502-23-5 C₂₈H₂₉F₉N₆O₃ 
• 874502-05-3 C₂₉H₂₉F₉N₆O₄ 
• 874502-32-6 C₂₈H₂₈F₉N₇O₃ 
• 874502-11-1 C₂₉H₃₁F₉N₆O₂ 
• 874502-20-2 C₃₀H₃₃F₉N₆O₂ 
• 874502-14-4 C₃₀H₃₃F₉N₆O₂ 
• 474645-99-3 C₂₄H₂₇F₃N₂O₄ 

Relevant academic research and scientific papers

Fragment-based discovery of novel pentacyclic triterpenoid derivatives as cholesteryl ester transfer protein inhibitors

Cholesteryl Ester Transfer Protein (CETP) is an important therapeutic target for the treatment of atherosclerotic cardiovascular disease. Our molecular modeling study revealed that pentacyclic triterpenoid compounds could mimic the protein-ligand interactions of the endogenous ligand cholesteryl ester (CE) by occupying its binding site. Alignment of the docking conformations of oleanolic acid (OA), ursolic acid (UA) and the crystal conformations of known CETP inhibitor Torcetrapib in the active site proposed the applicability of fragment-based drug design (FBDD) approaches in this study. Accordingly, a series of pentacyclic triterpenoid derivatives have been designed and synthesized as novel CETP inhibitors. The most potent compound 12e (IC50:0.28?μM) validated our strategy for molecular design. Molecular dynamics simulations illustrated that the more stable hydrogen bond interaction of the UA derivative 12e with Ser191 and stronger hydrophobic interactions with Val198, Phe463 than those of OA derivative 12b mainly led to their significantly different CETP inhibitory activity. These novel potent CETP inhibitors based on ursane-type scaffold should deserve further investigation.

Highly enantioselective three-component Povarov reaction catalyzed by SPINOL-phosphoric acids

Chiral SPINOL-phosphoric acids exhibited high activities and excellent diastereo- and enantioselectivities in the catalysis of the three-component Povarov reaction of benzyl N-vinylcarbamate, anilines and aldehydes with a catalyst loading of 5 mol%. The synthetic utility of this protocol was demonstrated by the asymmetric synthesis of enantioenriched benzo[e]indolizidine with excellent yield and excellent level of sterecontrol.

Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors

This letter describes the discovery and SAR optimization of tetrazoyl tetrahydroquinoline derivatives as potent CETP inhibitors. Compound 6m exhibited robust HDL-c increase in hCETP/hApoA1 double transgenic model and favorable pharmacokinetic properties.

A PROCESS FOR PREPARING TETRAHYDROQUINOLINE DERIVATIVES

The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof. Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.

Asymmetric synthesis of the cholesteryl ester transfer protein inhibitor torcetrapib

Previously our group reported synthetic efforts used to synthesize kilogram quantities of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, 1, via a mid-stage resolution. This account describes research conducted to develop an asymmetri

Therapeutic combination

Pharmaceutical combinations of a CETP inhibitor and atorvastatin or hydroxy metabolites thereof or a pharmaceutically acceptable salt thereof, methods of using such combinations and kits containing such combinations for the treatment of atherosclerosis, a