80104-36-5

Upstream product

• 584-08-7 potassium carbonate 
• 214602-25-2 ethyl 1-benzyl-6,7,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylate 
• 865-47-4 potassium tert-butylate 

Downstream Products

• 228725-47-1 N-[(4-chlorophenyl)methyl]-6,7,8-trifluoro-4-hydroxy-3-quinolinecarboxamide 
• 115841-65-1 ethyl 9,10-difluoro-7-oxo-2-phenyl-7H pyrido[1,2,3 de][1,4]benzoxazine-6-carboxylate 
• 1428551-16-9 C₂₄H₂₁F₄NO₄S 
• 1352429-10-7 tert-butyl-(3R,5S,6E)-7-[6,7,8-trifluoro-4-(4-fluorophenylthio)quinoline-3-yl]-3,5-dihydroxyhept-6-enoate 
• 1442676-46-1 C₁₆H₁₁F₄NOS 
• 207231-24-1 ethyl 4-chloro-6,7,8-trifluoroquinoline-3-carboxylate 

Relevant academic research and scientific papers

Synthesis of new quinolone antibiotics utilizing azetidine derivatives obtained from 1-azabicyclo[1.1.0]butane

A series of 3-sulfenylazetidine derivatives 5a-f were synthesized via the ring-opening reactions of 1-azabicyclo[ 1.1.0]butane (ABB, 3) with thiols 4a-f in 50-92% yields. Treatment of ABB (3) with aromatic amines 9a-e and dibenzylamine (9f) in the presence of Mg(ClO4)2 afforded the corresponding 3-aminoazetidine derivatives 10a-f in 24-65% yields. N-Benzyl-3-bromoazetidine (13), which was obtained by the reaction of ABB (3) with benzyl bromide, gave 3-aliphatic amino-substituted azetidine derivatives 15a, b. Novel fluoroquinolones 7a-f, 11a-f, 16a, b and 25a-c were obtained by the introduction of these azetidine derivatives into the C7 position of a quinolone nucleus 6 and N1-heterocyclic quinolones 21a-c in 21-83% yields. Some of them exhibited a greater antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) in comparison with that of clinically used fluoroquinolone, levofloxacin (LVFX).

4-Hydroxy-quinoline-3-carboxylic

A process for the preparation of a compound of the formula STR1 in which Y is a nitrile group, an ester group COOR1 or an acid amide CONR2 R3, R1, R2 and R3 each independently is hydrogen or C1 -C4 -alkyl, and R3 may also be phenyl, and X2, X3, X4 and X5 each independently is hydrogen, halogen, nitro, cyano, alkyl having 1-3 carbon atoms, alkoxy having 1-3 carbon atoms, alkylmercapto having 1-3 carbon atoms, alkylsulphonyl having 1-3 carbon atoms, or a phenylsulphonyl group which is optionally substituted in the aryl radical, comprising reacting an aminoacrylate of the formula in which X1 is halogen, a nitro group, an alkoxy, alkoxy, alkylmercapto or alkylsulphonyl group having 1-3 carbon atoms in each case, or an arylsulphonyl group, W is hydrogen or a --CH2 CH2 Z radical, Z is is a nitrile group, an ester group COOR4 or an acid amide group CONR5 R6, and R4, R5 and R6 each independently is hydrogen or C1 -C4 -alkyl, and R5 may also be phenyl, with an acid acceptor in an aprotic solvent. Some of the reactants are new, as are the products which are intermediates for antibacterially active 1-alkyl-4-quinolone-3-carboxylic acids.