METHOD FOR THE RESOLUTION OF 2-AMINO-6-PROPYLAMINO-4,5,6,7-TETRAHYDROBENZOTHIAZOL AND INTERMEDIATE COMPOUNDS

摘要

Method for resolving racemic 2-amino-6-propylamino-4,5,6,7-tetrahydrobenzothiazole (I) or for enriching a mixture with an excess of one enantiomer. Method for resolving racemic 2-amino-6-propylamino-4,5,6,7-tetrahydrobenzothiazole (I) or for enriching a mixture with an excess of one enantiomer comprises; (a) reacting the racemate (or enriched mixture) with a chiral acid of formula (IV) as an organic solution, optionally mixed with water; and (b) (fractional) crystallization of a mono-salt, diastereomerically pure or enriched, of formula (V). R : phenyl or alkylphenyl; and X : anion of (IV). An independent claim is included for diastereoisomeric salts, optically pure or enriched, of formula (V). [Image] ACTIVITY : Antiparkinsonian; Neuroleptic; Hypotensive. No details of tests for these activities are given. MECHANISM OF ACTION : Dopamine D2 agonist.