Process for the resolution of enantiomers of 5-heteroaryl-1,3,4-

Details Process for the resolution of enantiomers of 5-heteroaryl-1,3,4- Process for the resolution of enantiomers of 5-heteroaryl-1,3,4-

1992-09-02

1993-04-27

Ford, John M.

Organic compounds -- part of the class 532-570 series

Organic compounds

Unsubstituted hydrocarbyl chain between the ring and the -c-...

544 8, C07D28516, C07D41702

Patent

active

052063631

ABSTRACT:
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, characterized 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 or alcohol, thereby achieving a complete resolution of one of the diastereoisomers and a very slight or partial 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.

REFERENCES:
Jonas et al., Chemical Abstracts, vol. 110, entry 192866w (1989).

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