Process for the preparation of 1,2,4-substituted imidazoles and related aminoalkylimidazole derivatives
AssigneeSyntex Pharmaceuticals, Ltd.
InventorsGary McCort, Jean-Claude Pascal
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Abstract
The invention provides a new and efficient process for preparing 2,4(5)-substituted or 1,2,4-substituted imidazole derivatives. The invention also provides a process for preparing substituted aminoalkylimidazole derivatives, useful for the treatment of mammals having a variety of disease states, including stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism, and the like. The invention also relates to novel aminoalkylimidazole compounds.
Claims20
A process for the preparation of compounds represented by the formula:
- ##STR19## wherein:
- R.sup.1 is hydrogen, lower alkyl, or optionally substituted phenyl;
- R.sup.2 is hydrogen, lower alkyl, or optionally substituted lower alkyl phenyl;
- R.sup.3 is hydrogen, alkyl, optionally substituted phenyl, or optionally substituted biphenylmethyl;
- and
- R.sup.4 is hydrogen, lower alkyl, optionally substituted phenyl, or --SR.sup.5, in which R.sup.5 is lower alkyl, optionally substituted phenyl, or optionally substituted benzyl;
- which process comprises:
- cyclizing a compound represented by the formula:
- ##STR20## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined;
- in the presence of a palladium or gold catalyst.
The process of claim iii wherein R.sup.3 is hydrogen and R.sup.4 is 4-methylphenyl.
Dependencies are inferred from the claim text.