摘要 |
PURPOSE: Provided a method for manufacturing (S)-N-tert-butyl-1,2,3,4- tetrahydroisoquinoline-3 carboxamide, which is useful as an intermediate for manufacturing a compound having an improved pharmaceutical activity for the treatment or prevention of infectious diseases caused by human immunodeficiency virus (HIV), in a higher purity and yield. CONSTITUTION: The method for manufacturing (S)-N-tert-butyl-1,2,3,4- tetrahydroisoquinoline-3-carboxamide, is characterized by reacting tert-butylamine with an N-carboxylic anhydride of the formula(7) at a lower temperature than -30 deg.C, preferably -75 to -65 deg.C, in an inactive organic solvent. Where, the solvent is selected from the group consisting of toluene, THF, dioxan and CHCl.
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