Sulfuric acid magnesium salt (1:1) → {(2R,4S)-2-Benzyl-4-[(quinolin-4-ylmethyl)-amino]-piperidin-1-yl}-(3,5-bis-trifluoromethyl-phenyl)-methanone

関与物質

反応手順

3.35 g (7.78 mmol) of (2R,4S)-2-benzyl-1-(3,5-bis-(trifluoromethyl)benzoyl)-4-piperidinamine are reacted in analogy to Example 2 g with 1.34 g (8.56 mmol) of quinoline-4-carboxaldehyde and 1.3 g of magnesium sulfate in 30 ml of toluene, and subsequently reduced with 324 mg (8.56 mmol) of sodium borohydride in 25 ml of methanol. The title compound ##STR64## is obtained (3.5 g, 79%) as white foam. TLC: methylene chloride/methanol/conc. ammonia (1000:50:1) Rf =0.21, FD-MS: M+ =571, [α]D =+0.7 (c=1, MeOH), IR: 1635 cm-1.

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