| 摘要 |
PROBLEM TO BE SOLVED: To efficiently obtain the subject compound useful as an intermediate for synthesizing physiologically active fluoro (iso) quinoline derivatives by reacting a specific difluorostyrene derivative with a specific nucleophile or base. SOLUTION: This fluoroheterocyclic compound of formula II [Y is CR2=N, N=CH or (R3SOn)N-CH2] is obtained by reaction between aβ,β-difluorostyrene derivative of formula I [R1 is a 1-8C alkyl; X is isocyano or R3SOnNHCH2 group (R3 is phenyl optionally substituted with 1-3C alkyl (s), a 1-3C alkyl or the like; (n) is 1 or 2)] and a nucleophile of the formula (R2) (R2 is a 1-8C alkyl) or base of the formula MH (M is an alkali metal). For example, one of the objective compounds, 4-butyl-3-fluoro-2-tosyldihydroisoquinoline, is obtained by reacting sodium hydride with 2-o-(N-tosylaminomethyl)phenyl-1,1-difluoro-1- hexene.
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