PROCESS FOR THE PREPARATION OF SUBSTITUTED KETO-ENAMINES

The present invention discloses a process for the preparation of a substantially pure compound having formula (4). The process comprises the step of reacting an enolate having formula (A) with a Grignard reagent. The enolate salt is formed in situ from the reaction of a protected ester wherein M is...

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Bibliographic Details
Main Authors MENZIA, JEROME A, STUK, TIMOTHY L, HAIGHT, ANTHONY R
Format Patent
LanguageEnglish
French
Published 03.12.1998
Edition7
Subjects
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Summary:The present invention discloses a process for the preparation of a substantially pure compound having formula (4). The process comprises the step of reacting an enolate having formula (A) 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 (i) 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 (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents 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 (B) or (C), wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, lower alkyl, alkoxy, halogen and trifluoromethyl.
Bibliography:Application Number: CA19982292399