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1 tic fragment ion is formed via the loss of 2-fluoro-1,3,2-dioxaborale (MW of 88 Da) only in the case
3 S(N)V) reaction, which was directed toward 2-fluoro-1,4-benzoxazines and 2-fluoro-1,4-benzoxazepin-5-
4 ed very rapidly and selectively, affording 5-fluoro-1,4-pyrazoles with bimolecular rate constants up
5 have culminated in the discovery of 4-({5-[4-fluoro-1-(2H-indazol-6-yl)-1H-1,2,3-benzotriazol-6-yl]-1
6 vel estrogen receptor (ER) PET radiotracer 4-fluoro-11beta-methoxy-16alpha-(18)F-fluoroestradiol ((18
8 [(18)F]9) and (1S,3S,4R)-1-amino-3-fluoro-4-(fluoro-(18)F)cyclopentane-1-carboxylic acid ([(18)F]28)
9 c amino acids (1S,3R,4S)-1-amino-3-fluoro-4-(fluoro-(18)F)cyclopentane-1-carboxylic acid ([(18)F]9) a
10 o-1H-imidazol-2-yl)methyl)pyrrolidin-3-yl)-5-fluoro-1H-benzo [d]imidazole (42) with IC50 values of 44
11 assays, the most potent agonists being di(5-fluoro-1H-indole-3-yl)methane (38, PSB-15160, EC50 80.0
12 that dietary thymidine and serine enhance 5-fluoro 2'deoxyuridine (FUdR) toxicity in C. elegans thro
13 tors in Arabidopsis thaliana revealed that 2-fluoro 2-l-fucose (2F-Fuc) reduces root growth at microm
15 or 2'-O-methyl-substituted nucleosides, 2'-C-fluoro-2'-C-methyl-substituted nucleosides, 3'-O-methyl-
16 based on the suicide substrate arabinosyl-2'-fluoro-2'-deoxy NAD(+) (F-araNAD(+)), dimeric F-araNAD(+
21 of 0.4-4.7 muM), which contain one or two 2'-fluoro-2'-deoxyriboses and/or bis-phosphorothioate linka
22 otherapeutic drugs: 5-fluorouracil (5-FU), 5-fluoro-2'-deoxyuridine (FUDR), and camptothecin (CPT).
23 and sofosbuvir, which get metabolized to 2'-fluoro-2'C-methylcytidine-5'-triphosphate and 2'-fluoro-
24 ro-2'C-methylcytidine-5'-triphosphate and 2'-fluoro-2'C-methyluridine-5'-triphosphate, respectively.
28 etric transformations can be coupled using N-fluoro-2,4,6-trimethylpyridinium triflate as a terminal
29 ing materials by the F(+) transfer reagent N-fluoro-2,4,6-trimethylpyridinium triflate followed by tr
30 derivatization with a new chiral reagent, (5-fluoro-2,4-dinitrophenyl)-N(alpha)-l-tryptophanamide (FD
31 -d-fructose (6-[(18)F]FDF), 1-deoxy-1-[(18)F]fluoro-2,5-anhydro-mannitol (1-[(18)F]FDAM), 2-deoxy-2-[
32 which resulted in the identification of 5-[4-fluoro-2-(1-methyl-4-piperidyl)phenyl]-2-oxo-N-pentyl-ox
34 idin-5-yl)methanone (compound 29) and (S)-(3-fluoro-2-(trifluoromethyl)pyridin-4-yl)(1-(5-fluoropyrim
38 rocess by which tumor cells take up 2-[(18)F]fluoro-2-deoxy-D-glucose (FDG) is heterogeneous and infl
39 on tomography after an injection of [(18)F]2-fluoro-2-deoxy-d-glucose before the OGTT, and the rate o
40 to age- and sex-matched controls using 18F-2-fluoro-2-deoxy-d-glucose PET (n = 20 per group) and voxe
41 abolism in these subjects by means of [(18)F]fluoro-2-deoxy-d-glucose Positron Emission Tomography/Co
42 tissue (ATGU) glucose uptake with [(18) F]2-fluoro-2-deoxy-D-glucose/positron emission tomography, l
43 argeting TKIs are evaluated through 2-[(18)F]fluoro-2-deoxy-glucose ((18)FDG)-PET uptake, which is de
44 sociation between increased normalized (18)F fluoro-2-deoxyglucose PET SUVmax, outcome, and EMT in NS
45 data set that contained fluorine 18 ((18)F) fluoro-2-deoxyglucose positron emission tomography (PET)
46 m of the alkylation of indolphenol, 2, 4-[(4-fluoro-2-methyl-1 H-indol-5-yl)oxy]-6-methoxyquinazolin-
47 ic amount of iron(II) triflate (Fe(OTf)2), N-fluoro-2-methylbenzamides undergo chemoselective fluorin
48 up on the alpha-carbon, (S)-2-amino-7-[(18)F]fluoro-2-methylheptanoic acid ((S)-[(18)F]FAMHep, (S)-[(
49 881 [5-((7-benzyloxyquinazolin-4-yl)amino)-4-fluoro-2-methylphenol-hydrochloride] (20 mug/mL) was dri
50 S,2S)-2-({5-[(5-chloro-2,4-difluorophenyl)(2-fluoro-2-methylpropyl)amino]-3-methoxypyrazin-2-yl}carbo
54 be the use of a mechanism-based inhibitor, 2-fluoro-2-nitrovinylbenzene, to trap the putative cyclo-a
56 PA1163) has been studied by subjecting rac-2-fluoro-2-phenyl acetic acid to the defluorination proces
58 allows the straightforward synthesis of a 3'-fluoro-3'-deoxytetrose adenine phosphonate and can be ex
63 opa seems to improve the accuracy of 6-(18)F-fluoro-3,4-dihydroxy-l-phenylalanine ((18)F-FDOPA) PET f
64 nder factors, T(2) relaxometry and L-6-(18)F-fluoro-3,4-dihydroxyphenylalnine ((18)F-FDOPA) PET data
67 tivity in the nanomolar range and one, 2-((4-fluoro-3-(trifluoromethyl)phenyl)amino)-3-(methylthio)na
69 oses from d-glyceraldehyde and 2,3-dideoxy-2-fluoro-3-C-hydroxymethyl-2,3-endo-methylene-pentofuranos
70 es the pK(a) of the bound substrate analog 4-fluoro-3-hydroxybenzoate (4F3HB) by 1.6 pH units, consis
71 the production of the fluorinated diketide 2-fluoro-3-hydroxybutyrate at approximately 50 % yield.
72 -C center of spiro-epoxyoxindole furnishes 3-fluoro-3-hydroxymethyloxindoles, whereas TBAF-mediated f
74 LHP is synthesized from readily available 4-fluoro-3-methylphenol in six steps featuring a palladium
76 x was achieved via azide group activity of 4-fluoro-3-nitro-azidobenzene (FNAB), which act as cross-l
77 c organic crystal, 2,6-dichlorobenzylidine-4-fluoro-3-nitroaniline (DFNA), which also shows thermosal
78 lead structure, (3-chloro-4-fluorophenyl)(4-fluoro-4-(((2-(pyridin-2-yloxy)ethyl)amino)methyl)piperi
79 aniline ring, we generated Ethyl (2-amino-3-fluoro-4-((4-(trifluoromethyl)benzyl)amino)phenyl)carbam
80 ural cyclic amino acids (1S,3R,4S)-1-amino-3-fluoro-4-(fluoro-(18)F)cyclopentane-1-carboxylic acid ([
81 lic acid ([(18)F]9) and (1S,3S,4R)-1-amino-3-fluoro-4-(fluoro-(18)F)cyclopentane-1-carboxylic acid ([
83 PAH), revealing depression of the pK(a) of 3-fluoro-4-hydroxyphenylacetate by 2.5 pH units upon bindi
84 (trifluoromethyl)pyridin-2-yl)oxy)phenyl)(3- fluoro-4-hydroxypyrrolidin-1-yl)methanone 28, a potent i
85 r, we describe the discovery of 1-(6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinoli
86 ically 'rare' functional groups, such as the fluoro(5), chloro(6,7), bromo(7,8), phosphonate(9), ened
88 ered when analyzing the mode of action of 5'-fluoro-5'-deoxyadenosine synthase, the only known enzyme
89 the pharmacokinetics of (18)F-FPEB (3-(18)F-fluoro-5-(2-pyridinylethynyl)benzonitrile), a selective
90 of a clinically useful PET tracer, 3-[(18)F]fluoro-5-[(pyridin-3-yl)ethynyl] benzonitrile ([(18)F]FP
92 stribution volume of the radioligand (18)F-3-fluoro-5-[(pyridin-3-yl)ethynyl]benzonitrile ((18)F-FPEB
93 , to prepare the radiopharmaceutical (18)F-3-fluoro-5-[(pyridin-3-yl)ethynyl]benzonitrile ((18)F-FPEB
94 oazomycin arabinoside (or (18)F-1-alpha-D-[5-fluoro-5-deoxyarabinofuranosyl]-2-nitroimidazole [(18)F-
95 '-deoxy-3'-(18)F-fluorothymidine or 2'-(18)F-fluoro-5-methyl-1-beta-d-arabinofuranosyluracil may also
96 reomerically pure 6R- and 6S-3'-aza-2'-(18)F-fluoro-5-methyltetrahydrofolate (MTHF) (6R-(18)F-1 and 6
97 suggest that both 6R- and 6S-3'-aza-2'-(18)F-fluoro-5-MTHF are promising reduced radiofolates for ima
98 ully radiolabeled 6R- and 6S-3'-aza-2'-(18)F-fluoro-5-MTHF with (18)F using the integrated approach.
99 -axis in CRPC, using (18)F-FDG, (18)F-16beta-fluoro-5alpha-dihydrotestosterone ((18)F-FDHT), and a va
101 tential ERbeta-selective PET tracer: 2-(18)F-fluoro-6-(6-hydroxynaphthalen-2-yl)pyridin-3-ol ((18)F-F
102 We recently developed the tracer 2-(18)F-fluoro-6-(6-hydroxynaphthalen-2-yl)pyridin-3-ol ((18)F-F
105 yl]amin o}-3-quinolinecarboxamide (72) and 7-fluoro-6-[6-(methoxymethyl)pyridin-3-yl]-4-{[(1S)-1-(1-m
107 preclinical candidate compound containing 7-fluoro-6-oxybenzoxaborole (15, AN11251) was shown to hav
108 e palmitic acid surrogate tracer 14(R,S)-18F-fluoro-6-thia-heptadecanoic acid ([18F]-FTHA), consisten
110 (8S,9R)-47 (talazoparib; BMN 673; (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5
111 als injected with 2-chloro-2'-deoxy-2'-(18)F-fluoro-9-beta-d-arabinofuranosyl-adenine ((18)F-CFA), a
112 8)F]Clofarabine; 2-chloro-2'-deoxy-2'-[(18)F]fluoro-9-beta-d-arabinofuranosyl-adenine ([(18)F]CFA) an
113 -adenine ([(18)F]CFA) and 2'-deoxy-2'-[(18)F]fluoro-9-beta-d-arabinofuranosyl-guanine ([(18)F]F-AraG)
114 at a novel PET radiotracer, 2'-deoxy-2'-[18F]fluoro-9-beta-D-arabinofuranosylguanine ([18F]F-AraG), t
117 EcAldolase could catalyze the synthesis of 3-fluoro(a/e)-sialic acids and their C-9 analogues althoug
118 nctionalities, such as halides, alkyl ether, fluoro-alkyl ether, and thioether, and substituted amine
119 ction of aryl thiols to trisubstituted alpha-fluoro-alpha,beta-unsaturated esters both in racemic and
121 thylene phosphono analogues (7 and 8), and 6-fluoro-alphaG1P (9), were synthesized and assessed as po
123 eparation of a range of enantioenriched beta-fluoro amines (alpha,beta-disubstituted) is described in
126 to control, dietary supplementation with des-fluoro-anacetrapib reduced plasma CETP activity by 89 +/
129 er transfer protein (CETP) activity with des-fluoro-anacetrapib, an analog of the CETP inhibitor anac
131 vity of JWH-122, JWH-210, and PB-22, their 5-fluoro analogues (MAM-2201, EAM-2201, and 5F-PB-22, resp
132 t the synthesis of benzylated 3-fluoro and 4-fluoro analogues of phenyl 1-thioglucosazide and galacto
133 f the yet-unsynthesized bromo-, chloro-, and fluoro- analogues show a progressive lowering of the bar
134 therwise fully modified with the 2'-deoxy-2'-fluoro and 2'-O-methyl pentofuranose chemical modificati
135 ere, we report the synthesis of benzylated 3-fluoro and 4-fluoro analogues of phenyl 1-thioglucosazid
136 report the antimycobacterial activities of 4-fluoro and 6-methoxyindoles bearing a cationic amphiphil
137 benzene substituted as 2- or 4-methyl, or 4-fluoro, and defined the significance of thiophene substi
143 fy a novel agonist, the synthetic analogue 2-fluoro-ATP, and to confirm its agonist activity on rat P
145 d 2'-methoxyphenyl-(N-2'-pyridinyl)-p-[(18)F]fluoro-benzamidoethylpiperazine [(18)F]MPPF uptake in th
146 ields the corresponding syn-configured alpha-fluoro beta-hydroxy carboxylic acids which have >98 % ee
147 limination, the resulting transoid alpha-(1'-fluoro)-beta-(phenylsulfonyl)vinyl AA-esters undergo smo
149 n templates composed entirely of 2'-deoxy-2'-fluoro-beta-d-arabino nucleic acid (FANA) and alpha-l-th
154 e easily oxidized to the corresponding alpha-fluoro-beta-ketosulfones, which can be used for further
157 eadily available olefins to internal vicinal fluoro carbamates with high regioselectivity (N vs F), m
158 coupling reactions of aryl groups with alpha-fluoro carbonyl compounds catalyzed by palladium complex
159 g reactions of aryl electrophiles with alpha-fluoro carbonyl compounds have yet to be disclosed.
160 ws the compatibility of electron-withdrawing fluoro, chloro, ester, and nitro and electron-donating m
162 transferase inactivator (1R,3S,4S)-3-amino-4-fluoro cyclopentane-1-carboxylic acid (1), in this work,
165 -d-fructose (1-[(18)F]FDF), 6-deoxy-6-[(18)F]fluoro-d-fructose (6-[(18)F]FDF), 1-deoxy-1-[(18)F]fluor
169 o-mannitol (1-[(18)F]FDAM), 2-deoxy-2-[(18)F]fluoro-d-glucose (2-[(18)F]FDG), and 6-deoxy-6-[(18)F]fl
173 DG), a substrate for SGLTs; 4-deoxy-4-[F-18]-fluoro-d-glucose (4-FDG), a substrate for SGLTs and GLUT
174 glucose (2-[(18)F]FDG), and 6-deoxy-6-[(18)F]fluoro-d-glucose (6-[(18)F]FDG) was studied in EMT6 cell
179 mission tomography with (11)C-acetate, (18)F-fluoro-deoxyglucose ((18)FDG), and (18)F-fluoro-thiahept
180 ations in metabolism and volume using [(18)F]fluoro-deoxyglucose (FDG) and simultaneous time-of-fligh
181 um ions; however, in the cases of chloro and fluoro derivatives, open forms are more preferable.
182 sis of our results, we designed the di-ortho-fluoro di-ortho-chloro (dfdc) azobenzene and provided co
183 cal withC(C6H4)CH3)DPFN]NTf2 (DPFN = 2,7-bis(fluoro-di(2-pyridyl)methyl)-1,8-naphthyridine; NTf2(-) =
184 H5, 3,5-(CF3)2C6H3, and C6F5; DPFN = 2,7-bis(fluoro-di(2-pyridyl)methyl)-1,8-naphthyridine; X = BAr4(
185 ally simple reaction affords enantioenriched fluoro-diphenidine (up to 50 g scale) using 0.5 mol % of
187 ect the yield of RNA and incorporation of 2'-fluoro-dNMPs by Syn5 RNA polymerase have been identified
191 re included: brain tumor studies using (18)F-fluoro-ethyl-tyrosine ((18)F-FET) (n = 31) and (68)Ga-DO
192 evaluated if additional postoperative (18)F-fluoro-ethyl-tyrosine ((18)F-FET) PET in children and ad
193 a[5]helicenes are accessed from common ortho-fluoro-ethynylarene precursors, allowing the heteroatoms
195 4 weeks after injection of retrograde tracer Fluoro-Gold (FG), True Blue (TB) or Fluoro-Ruby (FR) in
198 mouse, this technique was achieved with only Fluoro-Gold, a neurotoxic fluorescent dye with membrane
199 ster) were infused with a retrograde tracer, Fluoro-Gold, and tested for affiliation and aggression t
201 ment and noncovalent interaction between the fluoro group and the aromatic proton on the thiophene si
203 t of the 5-iodo group with chloro, bromo, or fluoro groups led to losses in potency, as did the intro
205 However, electron-neutral and electron-rich fluoro(hetero)arenes are considerably underrepresented.
206 on of diverse alkyl, alkenyl, aryl, alkynyl, fluoro, hydroxyl and amino groups at the beta position o
208 orris Water Maze and a reduction in positive Fluoro-Jade B stained injured neurons and microglial act
209 thology characterized by positive silver and Fluoro-Jade B staining, and microglial proliferation and
211 ation in cortex and hippocampus indicated by Fluoro-Jade C in the different brain areas examined afte
213 ssessments, including neurological deficits, Fluoro-Jade C staining, brain edema, Evans blue extravas
215 ion utilizes branched vinyl or alkynyl alpha-fluoro ketones that can be coupled with a range of aryl,
220 amine synthesis capacity (Ki) using 6-[(18)F]fluoro-l-m-tyrosine ([(18)F]FMT; a substrate for aromati
222 00%, respectively, for 3,4-dihydroxy-6-(18)F-fluoro-l-phenylalanine ((18)F-FDOPA); and 100% and 70%-8
224 esis of each possible stereoisomer of a beta-fluoro lanicemine illustrates the potential ease with wh
225 n with hydroxy, cyano, nitro, acetamido, and fluoro led to high inhibitory activities toward ABCG2.
227 of novel imaging techniques (6-[fluoride-18]fluoro-levodopa [(18)F-DOPA] PET-CT and glucagon-like pe
229 nnoimidazole, or 2,4-dinitrophenol 2-deoxy-2-fluoro-mannoside reveal the residues essential for speci
233 e utility of N-(2,5-dimethoxybenzyl)-2-(18)F-fluoro-N-(2-phenoxyphenyl)acetamide ((18)F-PBR06) for de
234 dimethyl-4-oxo-2-thioxoimidazolidin -1-yl)-2-fluoro-N-(7-(hydroxyamino)-7-oxoheptyl)benzamide] and 10
235 etylglucosamine (4FGlcNAc) and UDP-4-deoxy-4-fluoro-N-acetylgalactosamine (4FGalNAc), were prepared u
236 iphosphate (UDP)-sugar donors, UDP-4-deoxy-4-fluoro-N-acetylglucosamine (4FGlcNAc) and UDP-4-deoxy-4-
237 ch analogue, (S)-2-(3,4-difluorophenyl)-5-(3-fluoro-N-pyrrolidylamido)benzothiazole (57) was chosen f
239 e catalyst that can deliver beta-amino-alpha-fluoro nitroalkanes with high enantio- and diastereosele
245 N, N-DABOs carrying 2,6-difluoro, 2-chloro-6-fluoro, or 2,6-dichloro substituted benzyl moieties.
246 roperties of fluorine and produced countless fluoro-organic compounds without which our everyday live
247 ormations resulted in the formation of novel fluoro-organics of the thiophene family, namely, product
249 bution demonstrated fast clearance of [(18)F]fluoro-PEG-folate from heart and blood vessels and no do
252 n study demonstrates the potential of [(18)F]fluoro-PEG-folate to image arthritis activity in RA with
254 CP) was synthesized using (19)F-labeled 2-(5-fluoro-pentyl)-2-methyl malonic acid ((19)F-FPMA) as the
255 tionally, the formation of 8-membered organo(fluoro)phosphate rings in lithium ion battery electrolyt
256 Since the high toxic potential of organo(fluoro)phosphates has emerged interest in safety assessm
257 (2,2-dimethyl-tetrahydro-pyran-4-ylmethyl)-4-fluoro-piperidin-4 -ylmethyl]-benzamide, a selective T-t
259 ion Findings with 2-(3-{1-carboxy-5-[(6-[18F]fluoro-pyridine 3-carbonyl)-amino]-pentyl}-ureido)-penta
260 ET agents such as 2-(3-{1-carboxy-5-[(6-[18F]fluoro-pyridine 3-carbonyl)-amino]-pentyl}-ureido)-penta
263 etic analysis of 2-(3-(1-carboxy-5-[(6-(18)F-fluoro-pyridine-3-carbonyl)-amino]-pentyl)-ureido)-penta
264 g (18)F-DCFPyL ([2-(3-(1-carboxy-5-[(6-(18)F-fluoro-pyridine-3-carbonyl)-amino]-pentyl)-ureido)-penta
265 re studied using 2-(3-(1-carboxy-5-[(6-(18)F-fluoro-pyridine-3-carbonyl)-amino]-pentyl)-ureido)-penta
266 , (18)F-DCFPyL (2-(3-(1-carboxy-5-[(6-[(18)F]fluoro-pyridine-3-carbonyl)-amino]-pentyl)-ureido)-penta
267 st (18)F-DCFPyL (2-(3-{1-carboxy-5-[(6-(18)F-fluoro-pyridine-3-carbonyl)-amino]-pentyl}-ureido)-p ent
268 le, MIP-1404, PSMA-11, 2-(3-{1-carboxy-5-[(6-fluoro-pyridine-3-carbonyl)-amino]-pentyl}-ureido)-penta
269 ed (18)F-DCFPyL (2-(3-{1-carboxy-5-[(6-(18)F-fluoro-pyridine-3-carbonyl)-amino]-pentyl}-ureido)-penta
270 g sessions using 2-(3-{1-carboxy-5-[(6-(18)F-fluoro-pyridine-3-carbonyl)-amino]-pentyl}-ureido)-penta
271 (18)F-DCFPyL (2-(3-{1-carboxy-5-[(6-(18)F-fluoro-pyridine-3-carbonyl)-amino]-pentyl}-ureido)-penta
272 e tracer Fluoro-Gold (FG), True Blue (TB) or Fluoro-Ruby (FR) in the tibial nerve in adult Spague-Daw
274 we have identified that carbamate-modified 3-fluoro sialic acid inhibitors are more efficiently metab
276 the synthesis of such glycans, especially 3-fluoro-sialic acid (3F-Neu5Ac) containing sialosides, ha
279 erved by NMR and crystallography with a para-fluoro substituent on the 4-phenylimidazole, but a para-
280 ity to COX-2 (6k = 70 nM, 8e = 60 nM) have a fluoro substituent, making them promising candidates for
281 ly genotoxic 3-nitro group by 3-chloro and 3-fluoro substituents, resulting in compounds with high To
282 or novel influenza inhibitors we evaluated 7-fluoro-substituted indoles as bioisosteric replacements
284 studying the regio- and chemoselectivity of fluoro-substituted thienothiophene and benzodithiophene
285 ign and synthesis it was discovered that cis-fluoro substitution on 4-hydroxy- and 4-methoxypiperidin
286 ine unit attached to a biphenyl carbamate, 5-fluoro substitution was responsible for M(3) subtype sel
287 d by introducing bulkier N-substituents, a 2-fluoro substitution, and additional hydroxyl groups at p
289 8)F-fluoro-deoxyglucose ((18)FDG), and (18)F-fluoro-thiaheptadecanoic acid ((18)FTHA), a fatty acid t
291 ethyl-tryptophan, 5-methyl-tryptophan, and 5-fluoro-tryptophan were efficient substrates of VioA.
292 ent derivatizations possessing two NO2, five fluoro, two fluoro, one fluoro, and no fluoro groups.
293 s; namely, a family of quaternary, alpha-(1'-fluoro)vinyl amino acids, bearing the side chains of the
294 beta-difluorovinyl phenyl sulfone, a new (1'-fluoro)vinyl cation equivalent, and an electrophile that
296 +/- 20 muM; t1/2 = 2.8 min) and D-alpha-(1'-fluoro)vinyllysine (Ki = 470 +/- 30 muM; t1/2 = 3.6 min)
297 arameters for the two antipodes, L-alpha-(1'-fluoro)vinyllysine (Ki = 630 +/- 20 muM; t1/2 = 2.8 min)
298 test of this new inhibitor class, alpha-(1'-fluoro)vinyllysine is seen to act as a time-dependent, i