反应详情

In analogy to the procedure described in Example 15, 4-[(R)-4-(3-chloro-4-trifluoromethyl-phenyl)-3-methyl-7-oxo-2,3,4,7-tetrahydro-[1,4]diazepin-1-yl]-butyric acid (22% ee) (intermediate 34) and 1.1 eq. of (S)-6-aza-spiro[2.5]octan-4-ol; hydrochloride (intermediate 2) gave after purification by flash chromatography (50 g amine-silica, ethyl acetate/n-heptane 1:1, 4:1, 9:1, 100%, ethyl acetate/ethanol 99:1 to 95:5) 69% of the title compound as off-white foam. MS: 500.19 (MH+, Cl).