FIELD: chemistry.
SUBSTANCE: invention relates to a method of producing a compound of formula (4): (4) (2) (3) (1), wherein R1 is a hydrogen atom or a protective group, or salt thereof, by reacting a compound of formula (2), in which X1 is a leaving group, with a compound of formula (3), wherein R1 is defined above, or a salt thereof, wherein said method involves reacting a compound of formula (2), with a compound of formula (3), or a salt thereof in presence of (a) palladium compound and tertiary phosphine, or (b) palladium carbene complex, in an inert solvent or in absence of solvent; where tertiary phosphine is at least one compound selected from a group comprising tri-tert-butylphosphine, 2-(di-tert-butylphosphino)-1,1′-biphenyl, 2-(di-tert-butylphosphino)-2′-methyl-1,1′-biphenyl, 2-(di-tert-butylphosphino)-1,1′-binaphthyl, 2-dicyclohexylphosphino-2′,6′-dimethoxy-1,1′-biphenyl, 2-dicyclohexylphosphino-2′,6′-di-iso-propoxy-1,1′-biphenyl, N-phenyl-2-(di-tert-butylphosphino)pyrrole and 1-phenyl-2-(di-tert-butylphosphino)-1H-indene. Invention also relates to methods of producing a compound of formula (1).
EFFECT: obtaining compounds of formula 4 with high output.
14 cl, 1 tbl, 16 ex
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Authors
Dates
2016-11-10—Published
2012-07-27—Filed