C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 417/04 (2006.01) C07D 417/14 (2006.01)
Patent
CA 2077031
Abstract of the Disclosure The invention relates to a process for the resolution of enantiomers of 5-heteroaryl-1,3,4- thiadiazinones of formula I by the kinetic resolution of racemates, characterised in that racemic I is dissolved in an inert solvent or solvent mixture and acylated with a chiral acid chloride, the resulting mixture of diastereoisomers is reacted with an amine, thereby achieving a complete resolution of one of the diastereoisomers and a very slight resolution of the other diastereoisomer into the enantiomers on which they are based, the resolution products are then separated off and the remaining pure diastereoisomer is converted to the corresponding pure enantiomer by reaction with an amine or an alcohol.
Ersing Peter
Jonas Rochus
Fetherstonhaugh & Co.
Merck Patent Gesellschaft Mit Beschraenkter Haftung
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