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US 3,946,009 AGranted
2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazines
AssigneeMerck Sharp & Dohme (I.A.) Corp.
InventorsBurton Kendall Wasson, Leonard M. Weinstock
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Abstract
2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazine compounds optionally having substituents in the 5 and/or 6 positions, possessing .beta.-adrenergic blocking properties are described. The products are prepared by reaction of a 2-chloro(or hydroxy)pyrazine with a 5-hydroxy-methyl(or sulfonyloxymethyl)oxazolidine followed by acid hydrolysis.
Claims7
A pyrazine compound having the structure ##SPC12##
- or a pharmacologically acceptable salt thereof wherein
- R represents phenyl, substituted phenyl wherein the substituent is C.sub.1-3 alkyl, C.sub.1-3 alkoxy, amino, nitro or halo, phenyl-C.sub.1-3 -alkyl, hydroxyphenyl-C.sub.1-3 -alkyl, phenoxy or substituted phenoxy wherein the substituent is C.sub.1-3 alkyl, C.sub.1-3 alkoxy, amino, nitro or halo;
- R.sup.1 represents a straight or branched chain C.sub.3.notident. alkyl, a straight or branched chain hydroxy substituted C.sub.3.notident. alkyl, a straight or branched chain C.sub.3.notident. alkinyl, phenyl-C.sub.1.notident. -alkyl or indolyl-C.sub.1.notident. -alkyl;
- R.sup.2 represents hydrogen, C.sub.1' alkyl, C.sub.5-7 cycloalkyl or an N- containing heterocycle selected from the group consisting of 1-pyrrolidinyl, piperidino, hexahydroazepinyl, morpholino, thiomorpholino, imidazolyl, pyrazolyl and thiazolyl;
- and
- R.sup.3 is N-containing heterocycle selected from the group consisting of 1-pyrrolidinyl, piperidino, hexahydroazepinyl, morpholino, thiomorpholino, imidazolyl, pyrazolyl and thiazolyl.
3 more elements
Dependencies are inferred from the claim text.