The novel synthesis of the protease inhibitor (S)??1??chloro??3??[(p??tolylsulfonyl) amino]??7??amino??2??[5, 5, 6, 6??3H] heptanone ([3H] TLCK) labeled to high specific …

AJ Villani, JR Heys

Index: Villani; Heys Journal of Labelled Compounds and Radiopharmaceuticals, 1997 , vol. 39, # 5 p. 379 - 386

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Citation Number: 2

Abstract

Abstract The protease inhibitor (S)-1-chloro-3-[(p-tolylsulfonyl) amino]-7-amino-2-[5, 5, 6, 6-3 H] heptanone ([3 H] TLCK) was prepared in an overall 41% radiochemical yield with a specific activity of 1.6 Ci/mmol in a 'one-pot'3 step sequence beginning with (S)-6-[[(1, 1- dimethylethyl) oxy] carbonyl]-2-(p-tolylsulfonyl) amino [4, 4, 5, 5-3 H] hexanoic acid. The latter was prepared with a specific activity of 123 Ci/mmol in a 3 step sequence beginning ...