反应详情

This compound was prepared by the method given for Example 82 using trans-2-carboxy-5,7-dichloro-4-(4-aminoethylphenyl)carbonylamino-1,2,3,4-tetrahydroquinoline hydrochloride Example 85, in the place of trans-2-carboxy-5,7-dichloro-4(3-aminomethylphenyl)carbonylamino-1,2,3,4-tetrahydroquinoline hydrochloride to give the title compound as a colourless crystalline solid, m.p. 218° C. (dec). δ (DMSO, 360 MHz) 1.78 (1H, ddd, J=13.2, 12.8 and 4.1 Hz, CHACHBHCCHD), 2.25 (1H, dm, J=13.2 Hz, CHACHBHCCHD), 2.92 (2H, t, J=7.0 Hz, CHE2CHF2), 3.04 (2H, t, J=7.0 Hz, CHE2CHF2), 3.71 (3H, s, CH3), 4.06 (1H, dd, J=12.5 and 2.4 Hz, CHACHBHCCHD), 5.26 (1H, m, CHACHBHCCHD), 6.69 (1H, d, J=2.0 Hz, 6-H or 8-H), 6.91 (1H, d, J=2.0 Hz, 6-H or 8-H), 6.94 (1H, s, Ar NHCH), 7.33 (2H, d, J=8.1 Hz, Ar-H), 7.86 (2H, d, J=8.1 Hz, Ar-H), 7.96 (2H, br, s, NH2), 8.70 (1H, d, J=7.1 Hz, NHCO); m/e (CI+, NH3) 422 (M+1); Found C, 48.59; H, 4.55; N, 8.48.C20H21Cl2N3O3.2HCl requires C, 48.51; H, 4.68; N, 8.48%.

1. customThis compound was prepared by the method