PRODUCTION OF 7-(2-FLUOROPHENYL)-1-BENZOSUBERONE

摘要

PROBLEM TO BE SOLVED: To efficiently and inexpensively obtain 7-(2-fluorophenyl)-1- benzosuberone useful as an intermediate for production of immunosuppressant by reacting a diazonium compound produced by reaction of a specific benzosuberone compound with nitrites with a specific fluorobenzene derivative. SOLUTION: A diazonium compound produced by reaction of (A) 7-amino-1- benzosuberone of formula I or its salt with (B) a nitrite of the formula R-(ONO)n [R is a lower alkyl; (n) is 1-3] or a nitrous acid salt (e.g. isoamyl nitrite) or its salt is reacted with (C) a fluorobenzene derivative of formula II (X1 to X3 are each H, chlorine, bromine or the like (e.g. monofluorobenzene) to provide the objective compound of formula III [e.g. 7-(2-fluorophenyl)-1-benzosuberone]. The reaction is carried out without or in a solvent and the reaction is usually finished in 0.5 to 24 hr at 0 deg.C to a boiling point of the component C or the solvent.