ライフサイエンスコーパス: fluorination

1 ol purple) were synthesized by electrophilic fluorination.

2 nger intra- and intermolecular contacts upon fluorination.

3 and electrophiles with different degrees of fluorination.

4 idual reaction components in decarboxylative fluorination.

5 achieved on the basis of differing levels of fluorination.

6 efficient set of reaction conditions for the fluorination.

7 -light irradiation results in very efficient fluorination.

8 tructural complexity and current methods for fluorination.

9 electfluor effects mild, catalytic sp(3) C-H fluorination.

10 L-rhamnose scaffold with varying degrees of fluorination.

11 t precursor for nucleophilic aromatic [(18)F]fluorination.

12 the well-recognized challenges of late-stage fluorination.

13 matic (18)F-labeled molecules via late-stage fluorination.

14 of the intricate challenges associated with fluorination.

15 ared by metalation followed by electrophilic fluorination.

16 tin nucleophiles exhibit no activity towards fluorination.

17 use of these activation manifolds for (18)F-fluorination.

18 unced rate enhancement is achieved by distal fluorination.

19 iously developed UV-mediated decarboxylative fluorinations.

20 within 1 hour with exclusive selectivity for fluorination adjacent to nitrogen.

21 [(18)F]13 was synthesized by nucleophilic fluorination, affording a product with >99% radiochemica

22 ates a cyclization, an aryl migration, and a fluorination all in one step.

23 harges on the carbon atoms at high levels of fluorination, all anions under study prefer hydrogen bon

24 Fluorination also results in an enhanced tendency to agg

25 We offer a mild, metal-free sp(3) C-H fluorination alternative using Selectfluor and a substoi

26 i((2)) increasing 7.5x upon chromophore core fluorination and 15x with hydrogen-bonding donor substit

27 ems provide an alternative route to chemical fluorination and could enable the production of organofl

28 tes computation indicate that molecular-core fluorination and hydrogen-bond donor incorporation can i

29 lization is accomplished by a combination of fluorination and nucleophilic aromatic substitution of t

30 predicted to be selective, leading to 97% of fluorination and only 3% of elimination.

31 ymer-fullerene blends with differing polymer fluorination and photovoltaic performance.

32 ation and borylation reactions, although C-H fluorination and radical C-H arylation processes were no

33 The combination of both fluorination and receptor binding is sufficient to block

34 that may topotactically be both oxidized by fluorination and reduced by deintercalation of oxygen fr

35 trategies, LUMO lowering through propargylic fluorination and strain enhancement through fused aryl r

36 and glycosylase-catalyzed depurination by 2'-fluorination and toward base-catalyzed degradation using

37 e Au(I)-catalyzed halide exchange (including fluorination) and Csp2-O bond formation reactions utiliz

38 n, elimination, stereoselective epoxidation, fluorination, and oxidation-reduction sequence of the Vi

39 tramolecular hydrogen atom transfer, radical fluorination, and ultimate restoration of the enone.

40 to recently published findings) and (ii) the fluorinations appear to take place at the gas bubble-sol

41 Fluorination appears to be a promising strategy for chem

42 that gamma-, beta-, homoallylic, and allylic fluorination are all possible and predictable through th

43 es are observed as the compounds increase in fluorination as well as upon exchange of the ancillary c

44 -substituted pyridines undergo high-yielding fluorination at room temperature using this reagent.

45 tigated for their abilities to promote rapid fluorination at silicon.

46 ort to compare the electronic effects of the fluorination at the methyl group.

47 ine-doped SiCDC at three different levels of fluorination, based on a hybrid reverse Monte Carlo cons

48 uggests that not only could strategic hapten fluorination be useful for improving upon the current co

49 ntribution to the timely problem of benzylic fluorination but also as a functional equivalent to a co

50 manganese porphyrin complex catalyzes alkyl fluorination by fluoride ion under mild conditions in co

51 reaction scope, which demonstrates that the fluorination can be performed in the presence of a wide

52 ules are inaccessible for imaging because no fluorination chemistry is available to make them.

53 spite tremendous progress within the area of fluorination chemistry, methods for the direct introduct

54 f areas ranging from sensing to nucleophilic fluorination chemistry.

55 anic chemistry, are currently on the rise in fluorination chemistry.

56 Organocatalytic fluorination, chlorination, and amination of the homo-Ro

57 t-mediated procedures can be used for remote fluorination, chlorination, and azidation, and were appl

58 d temperatures (i.e., more traditional halex fluorination conditions).

59 2-propenyl PT-sulfone required heterogeneous fluorination conditions.

60 chanistic study of copper-promoted aliphatic fluorination, constructively turning O2 from an enemy to

61 onolactone) after consecutive silylation and fluorination cycles.

62 We show that increasing fluorination dramatically increases binding to mammalian

63 We report that alkyl group fluorination (e.g., CB[7].1-AdNH2Et versus CB[7].1-AdNH2

64 ied PFAS classes derive from electrochemical fluorination (ECF) processes, most of which have the sam

65 ted sulfonamide synthesis by electrochemical fluorination (ECF).

66 mography (PET), with high and reliable radio-fluorination efficiency of [(18)F]FTAG (88 +/- 7%, n = 1

67 Late-stage fluorination enables the synthesis of conventionally una

68 kyl group (polarizability) and the degree of fluorination (field effect).

69 development affects the efficiency of (18)F-fluorination for a representative aryl boron reagent, an

70 A one-step oxidative fluorination for carbon-fluorine bond formation from wel

71 promote palladium-catalyzed beta-C(sp(3))-H fluorination for the first time.

72 Due to the fluorination, Franck-Condon states S1(FC) and S2(FC) are

73 )-H arylation and subsequent stereoselective fluorination from readily available L-alanine.

74 tion, gave a cyclohexane triflate, which, on fluorination, gave the all-cis 1,2,3-trifluoro-2-phenylc

75 l effect of fluorination, showing that while fluorination generates more hydrophilic carbon surfaces,

76 The first organomediated asymmetric (18)F fluorination has been accomplished using a chiral imidaz

77 A new approach to alkyl fluorination has been developed that utilizes the reagen

78 nthons prepared by the stereospecific double fluorination has enabled a significant decrease in the s

79 Fluorination has the effect of increasing the antiferrom

80 The use of these reagents in alkyl radical fluorination has the potential to enable powerful new tr

81 developments in gold-catalyzed nucleophilic fluorinations have been covered.

82 ized by no-carrier-added nucleophilic [(18)F]fluorination in 52-66% decay-corrected yields with radio

83 ic coupling, if any, between common sites of fluorination in both the azaindole and pyrazole classes

84 vation energy barriers are both decreased on fluorination, indicating weakened solid-fluid binding en

85 arable accuracy and precision as the current fluorination-IRMS techniques in delta(18)O, delta(17)O,

86 Fluorination is a reaction that is useful in improving t

87 Fluorination is achieved by spin coating a poly(vinylide

88 he oxygen atom, site-selective photochemical fluorination is achieved on steroids and bioactive polyc

89 An enantioselective fluorination is employed, taking advantage of the method

90 n increase in apparent hydrophobicity due to fluorination is mediated by larger free energy barriers

91 Property tuning by fluorination is very effective for a number of purposes,

92 non-fluorinated polymers shows that backbone fluorination leads to an increase in the polymer ionizat

93 Fluorination lowers the polymer HOMO level, resulting in

94 These results suggest that fluorination may be an effective strategy to increase th

95 fluorination reactivity, and the high-yield fluorination mechanism it undergoes have been clarified.

96 an unprecedented outer-sphere electrophilic fluorination mechanism.

97 The scope and efficiency of this new C-H fluorination method are significantly better than those

98 oro-beta-ketosulfides using an electrophilic fluorination method has been reported for the first time

99 This operationally simple, redox-neutral fluorination method is amenable to a wide variety of car

100 A rapid allylic fluorination method utilizing trichloroacetimidates in c

101 ication of a two-step enolization/NFSI alpha-fluorination method.

102 natural products using newly developed alpha-fluorination methodology is disclosed.

103 Despite all current limitations, modern fluorination methods have made fluorinated molecules mor

104 be overcome to increase the impact of modern fluorination methods on the synthesis of complex organof

105 previous KSP inhibitors, we found that beta-fluorination modulated the p K a of the piperidine nitro

106 nriched alkylcarbastannatranes are employed, fluorination occurs predominately via a stereoinvertive

107 Herein we report that excess oxidative fluorination of 2,2'-dipyridyl disulfide with a KF/Cl2 /

108 ones proceeded under homogeneous conditions, fluorination of 2-methyl-2-propenyl PT-sulfone required

109 synthetic strategy involves stereoselective fluorination of 3,4-trans-4,5-cis-3-aroyl-5-arylparaconi

110 TP was synthesized by no-carrier-added (18)F fluorination of 5-hydroxy-l-tryptophan.

111 idine amination can be adapted for selective fluorination of a broad range of nitrogen heterocycles.

112 of (18)F-DOPA, which relies on nucleophilic fluorination of a diaryliodonium salt precursor, lie in

113 ctivity are controlled through electrophilic fluorination of a ketene enolate intermediate.

114 This synthesis featured fluorination of a novel prosthetic group, followed by a

115 e data are consistent with a stereoretentive fluorination of a P(2)Pt-alkyl cation intermediate.

116 th the microwave-assisted nucleophilic (18)F-fluorination of a precursor containing a terminal p-tolu

117 Electrophilic fluorination of a protected 2-deoxy-2-trimethylsilylarab

118 This procedure is applied to the SNAr fluorination of a range of electron-deficient aryl and h

119 cable and safe method for the site-selective fluorination of a single carbon-hydrogen bond in pyridin

120 Fluorination of a triazolium bicyclic catalyst had been

121 cular orbital (LUMO) energy level due to the fluorination of A units.

122 allows for the room-temperature Pd-catalyzed fluorination of a variety of activated (hetero)aryl trif

123 e used to investigate the mechanism by which fluorination of acetylnitrene reduces the stabilization

124 ighly enantioselective (up to >99% ee) alpha-fluorination of acid chlorides to produce a variety of o

125 r studies on the catalytic, asymmetric alpha-fluorination of acid chlorides, a practical method that

126 pment, there are no direct protocols for the fluorination of aliphatic C-H bonds using conveniently h

127 The silver-catalyzed fluorination of aliphatic carboxylic acids by Selectfluo

128 t a catalytic enantioselective electrophilic fluorination of alkenes to form tertiary and quaternary

129 es more efficient than 18C6 for nucleophilic fluorination of alkyl halides.

130 A chemoselective catalytic fluorination of alkyl triflates is described using potas

131 The analogous Cu-F reagent was suitable for fluorination of allyl chlorides.

132 An enantioselective fluorination of allylic alcohols under chiral anion phas

133 ontext of a chiral phosphoric acid catalyzed fluorination of allylic alcohols using aryl boronic acid

134 nomical approach to the stereoselective beta-fluorination of alpha,beta-unsaturated systems.

135 of this approach with the direct asymmetric fluorination of alpha-substituted cyclohexanones to gene

136 The reaction proceeds via an electrophilic fluorination of alpha-sulfenyl-beta-diketones followed b

137 y diastereoselective (>98% de) electrophilic fluorination of amide enolates.

138 The new process has enabled the fluorination of an array of aryl and heteroaryl amines.

139 m reactions have also been developed for the fluorination of arenes and aryl bromides through arylbor

140 Fluorination of aromatic side chains has been suggested

141 radioligands using the copper-mediated (18)F-fluorination of aryl boron reagents with (18)F-fluoride

142 reaction design, a Pd-catalyzed nucleophilic fluorination of aryl bromides and iodides has been devel

143 paper describes the room-temperature S(N)Ar fluorination of aryl halides and nitroarenes using anhyd

144 mmunication describes a mild copper-mediated fluorination of aryl stannanes and aryl trifluoroborates

145 We report a regiospecific silver-mediated fluorination of aryl stannanes.

146 halogen exchange (halex) nucleophilic (18)F-fluorination of aryl-OCHFCl, -OCF2Br and -SCF2Br precurs

147 ommunication describes the Cu(OTf)2-mediated fluorination of aryltrifluoroborates with KF.

148 An efficient protocol for the selective fluorination of benzylic C-H bonds is described.

149 ntinuous-flow protocol for the light-induced fluorination of benzylic compounds is presented.

150 mmunication describes a mild, amide-directed fluorination of benzylic, allylic, and unactivated C-H b

151 direct, copper-catalyzed, auxiliary-assisted fluorination of beta-sp(2) C-H bonds of benzoic acid der

152 An alternative approach to selective fluorination of biaryls is to couple an arene that alrea

153 A strategy for last-step (18)F fluorination of bioconjugated peptides is reported that

154 ily and to perform site- and stereoselective fluorination of complex organic molecules.

155 raightforward and practical (18)F late-stage fluorination of complex small molecules with potential f

156 de a leap forward in the design of selective fluorination of complex substrates that should be releva

157 The origin of selectivity in the alpha-fluorination of cyclic ketones catalyzed by cinchona alk

158 A method for the palladium-catalyzed fluorination of cyclic vinyl triflates has been develope

159 Aromatic [(18)F]fluorination of drug-like small molecules is particularl

160 n of the desired product in the Pd-catalyzed fluorination of electron-rich, non-ortho-substituted ary

161 nonpolar solvent allows the enantioselective fluorination of enamides using Selectfluor as the fluori

162 eta-fluoroalcohols by catalytic nucleophilic fluorination of epoxides is described.

163 ar dynamic calculations reveal that backbone fluorination of F-P3EHT leads to an extended rod-like si

164 Fluorination of fluorophores can substantially enhance t

165 These CENCs proved efficacious in the fluorination of hindered silicon substrates, with fluori

166 f colitis-associated dysplasia after in situ fluorination of inflammatory macrophages in a mouse mode

167 to be superhydrophobic despite only partial fluorination of its organic backbone.

168 Direct fluorination of L(Cl)Si with Me(3)SnF resulted in oxidat

169 The present study shows that controlled fluorination of LMNMe2 (L = PhC(N(t)Bu)2, M = Ge, Sn) us

170 Fluorination of molecules often imparts desirable proper

171 A direct alpha-fluorination of N-acyloxazolidinones based on the unique

172 y-efficient alternative for asymmetric alpha-fluorination of N-acyloxazolidinones.

173 Although metalation-fluorination of n-propyl, 5-hexenyl, and (cyclopropyl)me

174 des were synthesized in high yield by double fluorination of N-protected (2S,4R)-4-hydroxyproline wit

175 This paper describes the fluorination of nitrogen heterocycles using anhydrous NB

176 s allows efficient and regioselective [(18)F]fluorination of non-activated aromatic moieties.

177 new synthetic technologies for the selective fluorination of organic compounds has increased with the

178 The fluorination of organic molecules is a rapidly evolving

179 xes were shown to be active in the catalytic fluorination of p-toluoyl chloride.

180 Judicious fluorination of peptides often results in increased ther

181 tent with a cation-pi interaction, increased fluorination of Phe401, which reduces the negative elect

182 An operationally simple ipso fluorination of phenols with a new deoxyfluorination rea

183 diastereoselective cation-olefin cyclization/fluorination of polyene substrates.

184 Side-chain fluorination of polymers is demonstrated as a highly eff

185 A catalytic method for the nucleophilic fluorination of propargylic electrophiles is described.

186 and arabino analogues have been prepared by fluorination of protected precursors.

187 The Ir-catalyzed enantioselective fluorination of racemic, branched allylic trichloroaceti

188 We herein describe the asymmetric fluorination of racemic, secondary allylic electrophiles

189 nium compounds play a pivotal role in (18) F-fluorination of radiopharmaceuticals containing non-acti

190 as redox photocatalysts for decarboxylative fluorination of several carboxylic acids showcases the p

191 ionic compounds was granted by electrophilic fluorination of sigma-sydnone Pd(II) precursors in the p

192 ility and crystallinity arising from partial fluorination of soluble anthradithiophene derivatives.

193 xplore in detail the iron-catalyzed benzylic fluorination of substrates containing aromatic rings and

194 Fluorination of the aminoisoquinoline reduced the basici

195 Catalytic fluorination of the aromatic ring has also been investig

196 .51, show consistent trends upon progressive fluorination of the aromatic side chain.

197 Electrophilic fluorination of the beta-ketosulfonamides using Selectfl

198 Methods:(18)F-FHNP was synthesized by fluorination of the corresponding nitro precursor, follo

199 ble, highly energetic material formed by the fluorination of the dinitramide anion using NF4(+) salts

200 ly, a 400-fold rate enhancement is seen upon fluorination of the distal arene ring, arising from favo

201 charge generation, and charge transport, as fluorination of the donor polymer optimizes the band ali

202 Our results suggest that half-fluorination of the GaBi honeycomb under tensile strain

203 3 and 5 positions, controlled electrophilic fluorination of the Li-ribonolactone enolate by N-fluoro

204 The most successful modifications involved fluorination of the nucleoside that provided substantial

205 ogues were subsequently obtained through the fluorination of the piperidinemethanols using DAST.

206 de photosensitizer has been increased by the fluorination of the porous Vycor glass tip.

207 y valuable compounds via diastereocontrolled fluorination of the readily available precursor 2-deoxy-

208 tions indicate that increasing the degree of fluorination of the tripodal transmembrane transporters

209 agenesis close to the flavin C2 carbonyl and fluorination of the tyrosine, respectively.

210 In the ideal case, the (18)F fluorination of these substrates would be performed thro

211 Further electrophilic fluorination of this species yields the difluorovinylide

212 Metalation-electrophilic fluorination of TMS- and TIPS-protected 1,3-benzothiazol

213 Pd(OTf)(2) x 2 H(2)O-catalyzed ortho-fluorination of triflamide-protected benzylamines is rep

214 The fluorination of unactivated C(sp(3) )-H bonds remains a

215 his study presents a technique for selective fluorination of various carboxylic acids by exposure to

216 t and highly regioselective protocol for the fluorination of vinyl triflates.

217 In addition to fluorinations of alcohols, aldehydes, and enolizable ket

218 chievements made in the iodine(iii) mediated fluorinations of aliphatic Csp(2)-carbon atoms with spec

219 n atom abstraction catalyst that can mediate fluorinations of certain alkanes upon activation with vi

220 synthesized in order to study the effect of fluorination on bulk thermal stability.

221 ations, to elucidate the impacts of backbone fluorination on morphology and excitonic coupling on the

222 tion of the effects of side-chain volume and fluorination on solvation dynamics.

223 are used to gain insight into the effect of fluorination on the field dependence of free charge-carr

224 With this method, the influence of fluorination on the lipophilicity of fluorinated aliphat

225 Here we examine the effect of surface fluorination on water-protein interactions.

226 so efficiently catalyzes bromination but not fluorination or iodination; (v) SgcC3 can utilize both (

227 favoring ArF-ArH interactions, and (ii) the fluorination pattern of the ArF ring, with 2,3,4,5,6-pen

228 For these orthogonal processes, the fluorination pattern of the substrate enabled the ligand

229 derstood) to HCA are, despite differences in fluorination pattern, indistinguishable; they nonetheles

230 an in-depth study of the effects of various fluorination patterns on their properties, such as lipop

231 The (18) F-fluorination precursors are readily prepared from aryl c

232 nary mechanistic investigations suggest that fluorination proceeds via copper acetylides and that cat

233 Therefore, this facile surface fluorination process brings huge benefit to both the exi

234 We show that LiFSI allows avoiding the fluorination process of the silicon particles surface up

235 Here we developed a surface fluorination process to form a homogeneous and dense LiF

236 ntentional byproducts in the electrochemical fluorination process used for polyfluorinated sulfonamid

237 mands the development of efficient catalytic fluorination processes.

238 etically useful functional groups makes this fluorination protocol broadly applicable in medicinal ch

239 thway is operable in this broadly applicable fluorination protocol.

240 ed with established asymmetric electrophilic fluorination protocols.

241 Fluorination provides better stability for biological ap

242 y efficient diastereoselective electrophilic fluorination reaction (94% yield; >50:1 dr).

243 In addition, a regioselective fluorination reaction allows access to the desired 3'-fl

244 describe the first catalytic decarboxylative fluorination reaction based on the nucleophilic fluoride

245 mild and selective photocatalytic C-H (18)F-fluorination reaction has been developed that provides d

246 Mechanistic studies suggest that this fluorination reaction occurs through facile oxidation of

247 ere have not been demonstrated for any other fluorination reaction to date.

248 l translation of a modern palladium-mediated fluorination reaction to non-human primate (NHP) baboon

249 The first catalytic allylic C-H fluorination reaction using a nucleophilic fluoride sour

250 The fluorination reaction was performed in a mixture of thex

251 When the fluorination reaction was performed with Cs2CO3 as base,

252 In studying the fluorination reaction, we have shown that the catalyst c

253 gioselectivities in this palladium-catalyzed fluorination reaction.

254 ssay examines the recent surge in late-stage fluorination reactions and outlines challenges that need

255 The appearance of late-stage fluorination reactions catalyzed by transition metal or

256 All reported transition-metal-catalyzed fluorination reactions for the synthesis of functionaliz

257 The use of metal complexes to promote fluorination reactions is of great current interest, but

258 in, we report selective C-H chlorination and fluorination reactions promoted by an electron-deficient

259 before, but selective, general and practical fluorination reactions remain sought after.

260 Most fluorination reactions still lack generality, predictabi

261 As with several previous palladium-catalyzed fluorination reactions using fluoride salts, controlling

262 chelating leaving groups were used in (18)F-fluorination reactions using no-carrier-added [18F]fluor

263 Review gives a brief summary of conventional fluorination reactions, including those reactions that i

264 e chemistry has been limited to nucleophilic fluorination reactions.

265 rbastannatrane nucleophiles in site-specific fluorination reactions.

266 s on 1k in thermal and hydrolytic stability, fluorination reactivity, and the high-yield fluorination

267 velopment of a palladium-based electrophilic fluorination reagent derived from fluoride and its appli

268 The DMPU/HF complex is a new nucleophilic fluorination reagent that has high acidity and is compat

269 sforms [(18)F]fluoride into an electrophilic fluorination reagent, provides access to aryl-(18)F bond

270 Fluorination represents an important strategy in develop

271 and microwave-assisted, palladium-catalyzed fluorination sequence.

272 plicity and the broad substrate scope of the fluorination should render this reaction a useful tool f

273 We demonstrate an apparent dual effect of fluorination, showing that while fluorination generates

274 ces, the molecule with the highest degree of fluorination shows a hole mobility of 0.15 cm(2)/V.s and

275 ene as a significant co-product of the final fluorination step.

276 nd other protic acids inhibit each of the 12 fluorination steps (in contradiction to recently publish

277 steps of the synthesis were an electrophilic fluorination/stereospecific hydrogenation sequence of a

278 steps via a one-pot lithiation-electrophilic fluorination strategy.

279 ulated or probed indirectly in photochemical fluorination systems) and, consequently, have provided k

280 ried hydrophobic surface area that accompany fluorination than by specific fluorous interactions betw

281 lfonamide ligands with different patterns of fluorination--that we use to define enthalpy/entropy (H/

282 In the realm of aliphatic fluorination, the problem of reactivity has been very su

283 of the difficulty associated with selective fluorination, this class of molecules represent a formid

284 oup, a range of acyclic substrates underwent fluorination to afford highly enantioenriched alpha-fluo

285 ns of the nucleoside was performed by direct fluorination to enhance activity and improve drug dispos

286 d problem of selectivity, that is, directing fluorination to specific sites in complex molecules, rem

287 are two competing forces: one directing the fluorination to take place ortho to the boronic acid and

288 also propose that the previously determined fluorination trend at W6.48 is likely due to a sulfur-pi

289 h yield from a second round of electrophilic fluorination (two steps, 51% from protected ribonolacton

290 nmentally friendly alternative for selective fluorination under mild conditions.

291 NBu4F compare favorably to traditional halex fluorinations using alkali metal fluorides, which genera

292 The desired selectivity of fluorination was achieved using an unorthodox protecting

293 he range of (hetero)arenes amenable to (18)F-fluorination was limited by the lack of chemically diver

294 ificant, conceptual advances in the field of fluorination were enabled most prominently by organo- an

295 investigated by DFT calculations to compare fluorination with chlorination, proving a larger thermod

296 NMe4F is generally more cost-effective than fluorination with CsF.

297 yst system, simple olefin substrates undergo fluorination with Et3N.3HF in good yields with high bran

298 imidazole derivatives through electrophilic fluorination with N-fluorobenzenesulfonimide enabled via

299 cost analysis is presented, which shows that fluorination with NMe4F is generally more cost-effective

300 ination of hindered silicon substrates, with fluorination yields dependent on the length of linker co