1-cyclopropyl-6-fluoro-8-methoxy-7-

Dimethyl-[l-methoxy-2,2,3,3-tetra-methyl-cyclopropyl]- -fluoro-sulfonate 1666... 

CN 1 -Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4a5,7a5)-octahydro-6//-pyrrolo[3,4-fc]pyridin-6-yl]-... 

The products obtained in the reaction of A -cyclopropyl-4,5-difluoroanthranilic acid hydrazides 429 with triphosgene were dependent on the steric hindrance imposed by substituent R at position 3, and not the electronic effect of this group. While the unsubstituted compound 429 (R = H) gave exclusively the 4-hydrazono-3,l-benzoxazin-2-one-type product 430, the similar reactions of the chloro-, methyl-, and methoxy-substituted analogs 429 (R = Cl, Me, OMe) resulted in formation of the corresponding quinazoline-2,4-diones 431 as the sole products. For the fluoro-substituted compound 429 (R = F), a 20 80 mixture of the products 430 and 431 was obtained (Equation 46) <2005JHC669>. 

The treatment of 6-chloro-4-cyclopropyl-7-fluoro-5-methoxy-lH,3H-pyr-ido[l, 2-c]pyrimidine-1,3-dione with 0-(2,4-dinitrophenyl)hydroxylamine in the presence of K2C03 in a mixture of THF and DMF at 80 °C for 2 h gave 2-amino derivative in 88% yield (09TL785). 

It was claimed that cyclization of ethyl 2-chloro-5-cyclopropyl-6- [(7V-(4,5-dimethoxy-2-nitrophenyl)methoxy)carbonyl]-A-(2-fluoro-3-hydroxy-l-oxo-2-propen-l-yl)amino nicotinate (321) in boiling aqueous dioxane in the presence of K2C03 overnight yielded l- [(4,5-dimethoxy-2-nitrophe-nyl)methoxy]carbonyl -9-cyclopropyl-3-fluoro-2-oxo-2,6-dihydropyrido[l, 2-u]pyrimidine-7-carboxylate (160) (95MIP1, 96MIP4, 96USP5580872). 

Chemical Name 3-Quinolinecarboxylic acid, l-cyclopropyl-6-fluoro-l,4-dihydro-8-methoxy-7-(3-(methylamino)-l-piperidinyl)-4-oxo-... 

Syntesis of l-cyclopropyl-7-(2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-l,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid hydrochloride (moxifloxacin hydrochloride) ... 

Ethyl l-cyclopropyl-6-fluoro-7- (1-methoxy vinyl)-4-oxo-1,4-dihydro-1, 8-naphthyridine-3-carboxylate 151-152, IR, MS, NMR 1158... 

Cyclopropyl methyl sulfides 44, substituted at the 1-position with a wide variety of heteroatombearing substituents, e.g. methylsulfanyl, phenylsulfanyl, methoxy, ethoxy, phenoxy and fluoro, are readily methylated at sulfur with methyl fluorosulfonate to form sulfonium salts 45 in quantitative yield. 

Moxifloxacin, l-cyclopropyl-7-[(lS,65)-2,8-diazabicyclo[4.3.0]nonan-8-yl]-6-fluoro-8-methoxy-4-oxoquinoline-3-carboxylic acid, is a fourth-generation synthetic fluoroquinolone antibacterial agent. Photostability of moxifloxacin studies after UVA irradiation in solutions and solid phase, with and without participation of Cu(II), Zn(II), Al(III), and Fe(in), were carried out by TLC-densitometric method and LC-MS/MS method [10] (Figure 14.6). 

Guo H, Liu J, Wang Y (2004) Preparation of 5-amino-l-cyclopropyl-6-fluoro-8-methoxy-l,4-dihydroquinolin-4-one-3-carboxylic acid derivatives as antibacterial agents. CN Patent 1491944, 28 Apr 2004... 

Deshpande P, Bhavsar S, Chugh Y, Yeole R, De Souza N, Patel M (2005) Novel polymorphs of racemic dextrorotatory and levorotatory enantiomers of l-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidinl-yl)-l,4-dihydro-4-oxoquinoline-3-carboxylic acid and hydrochloride and mesylate salts. WO Patent 66154, 21 July 2005 Takahashi Lt, Hagiwara T, Hayakawa 1 (2002) Preparation of fluoroquinoUne drug with reduced effect on the heart. WO Patent 76458,3 Oct 2002... 

Senthilkumar P, Dinakaran M, Baneijee D, Devakaram R, Yogeeswari P, China A, Nagaraja V, Sriram D (2008) Synthesis and antimycobacterial evaluation of newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(substituted)-4-oxoquinoline-3-carboxylic acids. Bioorg Med Chem 16 2558-2569... 

In the recent year Thomas et al. [15] designed, synthesized and evaluated antimicrobial activity of some new 1,2,3-triazole containing quinoline derivatives. The in-vitro preliminary antimicrobial screening revealed that, the presence of active groups like cyclopropyl, substituted piperazines, methoxy and fluoro has contributed significantly in enhancing the activity. 

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