153968-97-9

Upstream product

• 160375-37-1 2-Cyclopropyl-4-(4-fluoro-phenyl)-quinoline-3-carboxylic acid 
• 62-53-3 aniline 
• 1246224-43-0 1-fluoro-4-(iodoethynyl)benzene 
• 369-57-3 benzenediazonium tetrafluoroborate 
• 5500-21-0 cyclopropropanecarbonitrile 
• 24922-02-9 Ethyl 3-cyclopropyl-3-oxopropionate 
• 6311-23-5 2-(toluene-4-sulfonylamino)-benzoic acid 
• 765-43-5 Cyclopropyl methyl ketone 
• 148516-11-4 2-cyclopropyl-4-(4-fluoro-phenyl)-3-quinoline carboxylic acid ethyl ester 
• 118-92-3 anthranilic acid 
• 3800-06-4 2-amino-4'-fluorobenzophenone 
• 934560-46-0 N-[2-(4-fluorobenzoyl)phenyl]-4-methylbenzenesulfonamide 
• 42840-02-8 2-(Toluene-4-sulfonylamino)-benzoyl chloride 

Downstream Products

• 147489-06-3 (4R,6S)-(E)-{6-[2-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-vinyl]-2,2-dimethyl-1,3-dioxan-4-yl}acetic acid tert-butyl ester 

Relevant academic research and scientific papers

Cascade annulations of aryldiazonium salts, nitriles and halo-alkynes leading to 3-haloquinolines

A regiospecific access to 3-haloquinolines has been developed via a three-component annulation of aryldiazonium salts, nitriles and haloalkynes. This reaction proceeds through an initial formation of reactive nitrilium ion and further cascade annulation with haloalkynes. This method provides a straightforward access to a diverse array of functionalized quinolones (28 examples) under mild conditions and exhibits broad functional group tolerance. Applications of this method in a gram scale reaction and a formal synthesis of Pitavastatin are illustrated.

A NOVEL SYNTHETIC METHOD OF HMG-CoA REDUCTASE INHIBITOR NK-104 VIA HYDROBORATION-CROSS COUPLING SEQUENCE

The regioselective hydroboration of ethyl (3R,5S)-3,5-isopropylidenedioxy-6-heptynoate, followed by the cross-coupling reaction with an aryl halide, provides ethyl (3R,5S,6E)-7-aryl-3,5-isopropylidenedioxy-6-heptenoate, a precursor of a highly potent HMG-