摘要 |
Production of aryllithium-electrophile reaction products comprises reacting an aryl halide with lithium, reacting the resulting aromatic lithium compound with an aromatic halide, and reacting the resulting aryllithium with an electrophile. Production of aryllithium-electrophile reaction products of formula (V) comprises reacting an aryl halide of formula (I) with lithium, reacting the resulting aromatic lithium compound of formula (II) with an aromatic halide of formula (III), and reacting the resulting aryllithium of formula (IV) with an electrophile: Ar-Hal (I).....Ar-Li (II) Ar'-Hal' (III) Ar'-Li (IV) Ar'-El (V) Ar = phenyl, pyridyl or naphthyl, all optionally substituted with alkyl, cycloalkyl, aryl, heteroaryl, alkoxy, dialkylamino, alkylthio, F or Br; Hal = F, Cl, Br or I; Hal' = Cl, Br or I; Ar' = a 6-membered aromatic ring in which the members are CR or N, or a 5-membered aromatic ring in which one member is O, S, NH or NR; R = H, 1-12C (cyclo)alkyl (optionally halogenated), substituted (cyclo)alkyl, alkoxy, (di)alkylamino, (di)arylamino, (un)substituted phenyl, (un)substituted heteroaryl, alkylthio, arylthio, diarylphosphino, dialkylphosphino, alkylarylphosphino, (di)alkyl- or (di)arylcarbamoyl, alkylarylcarbamoyl, carboxylate, alkoxycarbonyl, aryloxycarbonyl, hydroxyalkyl, alkoxyalkyl, F, Cl, NO2, CN, aryl- or alkylsulfone, alkyl- or arylsulfonyl, or adjacent R groups form an aromatic, heteroaromatic or alicyclic ring; El = electrophile.
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