DETAILED DESCRIPTION "Lower alkyl of from one to four" or "ten carbons" in the present invention means methyl, ethyl, propyl, butyl or further pentyl, hexyl, heptyl or the like and isomers thereof respectively.
"Halogen is chloro, fluoro or bromo.
"Lower alkenyl of from two to ten carbons" means ethenyl, 1- or 2-propenyl, 1-, 2- or 3-butenyl and the like and isomers thereof.
"Lower alkynyl of from two to ten carbons" means ethynyl, 1- or 1-propynyl, 1-, 2- or 3-butynyl and the like and isomers thereof.
"Alkylenyl of from one to three" or "to four" is a bridging alkyl chain, i.
e.
having two open bonds, such as methylenyl, ethylenyl, propylenyl or further butylenyl and isomers thereof.
The compounds of the present invention may contain asymmetric carbon atoms, and, therefore, the instant invention may also include the individual diastereomers and enantiomers, which may be prepared or isolated by methods known to those skilled in the art.
In other words, any resulting racemate can be resolved into the optical antipodes by known methods, for example, by separation of the diastereomeric salts thereof, with an optically active acid, and liberating the optically active amine compound by treatment with a base.
Racemic compounds of the present invention can thus be resolved into their optical antipodes e.
g.
, by fractional crystallization of d- or 1-(tartrates, mandelates, or camphorsulfonate) salts.
Additional methods for resolving optical isomers, known to those skilled in the art may be used, for example, those discussed by J.
Jaques, A.
Collet, and S.
Wilen in Enantiomers, Racemates, and Resolutions, John Wiley and Sons, New York (1981).
The compounds I of the invention may preferably be pharmaceutically acceptable salts.
Such salts may be basic or acid salts, for example, sodium, potassium, ammonium, calcium, magnesium, acetate, adipate, alginate, citrate, aspartate, benzoate, benzenesulfonate, bisulfate, butyrate, camphorate, camphorate, camphorsulphonate, digluconate, cyclopentanepropionate, dodecylsulfate, ethanesulfonate, glucoheptanoate, glycerophosphate, hemisulfate, heptanoate, hexanoate, fumarate, hydrochloride, hydrobromide, hydroiodide, 2-hydroxyethanesulfonate, lactate, maleate, methanesulfonate, nicotinate, 2-naphthalenesulfonate, oxalate, palmoate, pectinate, persulfate, 3-phenylpropionate, picrate, pivalate, propionate, succinate, tartrate, thiocyanate, tosylate, mesylate, and undecanoate, or phosphate, sulfate, chloride, carbonate and the like
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