Synthesis of 4-methyl-5-arylpyrimidines and 4-arylpyrimidines: route specific markers for the Leuckardt preparation of amphetamine, 4-methoxyamphetamine, and 4-methylthioamphetamine

General synthetic routes to 4-methyl-5-arylpyrimidines and 5-arylpyrimidine s are described. 4-Benzylpyrimidine, 4-methyl-5-phenylpyrimidine, 4-(4-meth oxybenzyl)pyrimidine, and 4-methyl-5-(4-methoxyphenyl)pyrimidine have been positively identified as route-specific by-products in the Leuckardt prepar ations of amphetamine and 4-methoxyamphetamine. Using headspace solid phase microextraction (SPME) 4-(4-methoxybenzyl)pyrim idine and 4-methyl-5-(4-methoxyphenyl)pyrimidine have been identified in il licit tablets containing 4-methoxyamphetamine. This is an indication that i llicit laboratories use the Leuckardt method for the preparation of 4-metho xyamphetamine. Flatliner tablets containing 4-methylthioamphetamine have been screened for the presence of 4-(4-methylthiobenzyI)pyrimidine and 4-methyl-5-(4-methylt hiophenyl)pyrimidine using both headspace and aqueous phase SPME. As these pyrimidines were not detected it would appear likely that illicit laborator ies are not using the Leuckardt method for the preparation of 4-methylthioa mphetamine. (C) 2001 Elsevier Science Ireland Ltd. All rights reserved.