VERFAHREN ZUR HERSTELLUNG VON SUBSTITUIERTEN KETO-ENAMINEN

• Main Authors: MENZIA, JEROME, A, HAIGHT, ANTHONY, R, STUK, TIMOTHY, L
• Format: Patent
• Language: German
• Published: 15.10.2002
• Edition: 7
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY

The present invention discloses a process for the preparation of a compound having formula 4: The process comprises the step of reacting an enolate having the formula: with a Grignard reagent. The enolate salt is formed in situ from the reaction of a protected ester wherein M is an alkali metal. R6 and R7 are each hydrogen or are independently selected from wherein Ra and Rb are independently selected from hydrogen, lower alkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, lower alkyl, trifluoromethyl, alkoxy, halo and phenyl; and wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from lower alkyl, trifluoromethyl, alkoxy and halo. Alternatively, R6 is as defined above and R7 is R12OC(O)- wherein R12 is benzyl; or R6 and R7 taken together with the nitrogen atom to which they are bonded form wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, lower alkyl, alkoxy, halogen and trifluoromethyl.