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Syntheses of radiolabelled forms of a novel histamine H1 antagonist (SK&F 93944)

✍ Scribed by M M Cashyap; M B Mitchell; D C Osborne; D Saunders

Publisher
John Wiley and Sons
Year
1985
Tongue
French
Weight
378 KB
Volume
22
Category
Article
ISSN
0022-2135

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✦ Synopsis

A novel hlstamlne H1 antagonist SKbF 93944 , 2-[4-(5-bromo-3methylpyrid-2-yl ) butylamino]-5-( 6-methylpyrid-3-yl-methyl)-4( 3H)pyrlmldone. has been labelled with carbon-14 in two dlfferent positions for use in metabolism and pharmacokinetic studies. four stage synthesis o f [p~rimldone-2-~~C] SKLF 93944 (1) from barium [ Clcyanamide is described. The overall radiochemlcal yield was 38%. synthesised in four steps from [ Clmethyl Iodide. The key steps in this synthesis were alkylation of 2-lithio-3-methyl pyrldine wlth [14C]nethyl Iodide and the brominatlon of 4-(3- methyl-2-pyridyl)[4-14C]butylamine in a liquid sulphur trloxide/freon mlxture. The overall radiochemlcal yield was 1.6% from [14C]methyl lodlde. The 14 [but~lamino-4-~~C] SKLF 93944 (14) was 14

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