3-Chloro-4-fluorobenzaldehyde → (7bR,11aS)-N-(3-chloro-4-fluorobenzyl)-1,2,7b,8,9,10,11,11a-octahydro-4H-pyrido[4,3-b][1,4]thiazepino[6,5,4-hi]indol-6-amine

関与物質

反応手順

Using 4-fluoro-3-chlorobenzaldehyde and following the procedures described in EXAMPLE 126, tert-butyl (7bR,11aS)-6-amino-1,2,7b,10,11,11a-hexahydro-4H-pyrido[4,3-b][1,4]thiazepino[6,5,4-hi]indole-9(8H)-carboxylate from EXAMPLE 33, Part B was converted into the title compound of EXAMPLE 155. 1H NMR(CDCl3): 7.42 (dd, 1H, J=7.0, 2.2 Hz), 7.27-7.20 (m, 1H), 7.12 (t, 1H, J=8.6 Hz), 6.32 (d, 1H, J=2.2 Hz), 6.21 (d, 1H, J=2.2 Hz), 4.23 (broad s, 2H), 3.67 (ABq, 2H, JAB=15.2 Hz), 3.57-3.48 (m, 1H), 3.38-3.30 (m, 2H), 3.19-3.08 (m, 1H), 3.05-2.90 (m, 4H), 2.65-2.55 (m, 2H), 2.02-1.88 (m, 2H). LRMS (ES)+: 404.4 (M+H)+.

情報源と証拠