N-(4-氟苯基)-1,2-乙二胺

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: The title compound was prepared from 2-chlorobenzoxazole, L-cyclohexylalanine and N1-(4-fluoro-phenyl)-ethane-1,2-diamine.2HCl using the procedure analogous to that described in example 2. 1H NMR (DMSO-d6, 400 MHz) δ 8.16(m, 2H), 7.30(m, 1H) 7.16(m, 1H), 7.04(m, 1H), 6.92(m, 1H), 6.84(m, 2H), 6.50(m, 2H), 4.24 (m, 1H), 3.15(m, 2H), 2.97(m, 2H), 1.55(m, 7H), 1.30(m, 1H), 1.05(m, 3H), 0.83(m, 2H). HPLC-MS calcd. for C24H29FN4O2 (M+H+)424.23. found 425.5.

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: The title compound was prepared from 2-Chloro-benzooxazole-6-carboxylic acid methyl ester, L-cyclohexylalanine and N1-(4-fluoro-phenyl)-ethane-1,2-diamine.2HCl using the procedure analogous to that described in example 2. HPLC-MS calcd. for C26H31FN4O4 (M+H+)483.23. found 483.5.

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: The title compound was prepared from 2-chloro-5-fluorobenzoxazole, L-cyclohexylalanine and N1-(4-fluoro-phenyl)-ethane-1,2-diamine.2HCl using the procedure analogous to that described in example 2. 1H NMR (DMSO-d6, 400 MHz) δ 8.29 (d, 1H, J=8.0 Hz), 8.16 (t, 1H, J=5.6 Hz), 7.27 (dd, 1H, J=4.4 Hz, J=8.4 Hz), 6.97 (dd, 1H, J=2.6 Hz, J=9.4 Hz), 6.80 (m, 2H), 6.72(m, 1H), 6.46(m, 2H), 5.42(m, 1H), 4.20 (m, 1H), 3.15(m, 2H), 2.95(m, 2H), 1.55(m, 7H), 1.30(m, 1H), 1.05(m, 3H), 0.83(m, 2H). HPLC-MS calcd. for C24H28F2N4O2(M+H+) 443.22. found 443.5.

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: The title compound was prepared from 2-chloro-6-fluorobenzoxazole, L-cyclohexylalanine and N1-(4-fluoro-phenyl)-ethane-1,2-diamine.2HCl using the procedure analogous to that described in example 2. 1H NMR (DMSO-d6, 400 MHz) δ 8.18(m, 2H), 7.30(dd, 1H, J=2.4 Hz, J=8.6 Hz), 7.11(dd, 1H, J=4.8 Hz, J=8.4 Hz), 6.89(m, 1H), 6.84(m, 2H), 6.51(m, 2H), 4.28 (m, 1H), 3.15(m, 2H), 2.95(m, 2H), 1.55(m, 7H), 1.30(m, 1H), 1.05(m, 3H), 0.83(m, 2H). HPLC-MS calcd. for C24H28F2N4O2 (M+H+)443.22. found 443.4.

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: The title compound was prepared from 2,6-dichlorobenzothiazole, L-cyclohexylalanine and N1-(4-fluoro-phenyl)-ethane-1,2-diamine.2HCl using the procedure analogous to that described in example 2. 1H NMR (DMSO-d6, 400 MHz) δ 8.30 (d, 1H, J=8.0 Hz), 8.17 (t, 1H, J=5.6 Hz), 7.72 (d, 1H, J=2.4 Hz), 7.23 (d, 1H, J=8.4 Hz), 7.15 (dd, 1H, J=8.4 Hz, J=2.4 Hz), 6.84(m, 2H), 6.50(m, 2H), 4.40(m, 1H), 3.16(m, 2H), 2.97(m, 2H), 1.55(m, 7H), 1.30(m, 1H), 1.05(m, 3H), 0.83(m, 2H). HPLC-MS calcd. for C24H28ClFN4OS (M+H+)475.17. found 475.3.

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: The title compound was prepared from 2,6-dichlorobenzooxazole, L-cyclohexylalanine and N1-(4-Fluoro-phenyl)-ethane-1,2-diamine.2HCl using the procedure analogous to that described in example 2. 1H NMR (DMSO-d6, 400 MHz) δ 8.30 (d, 1H, J=8.4 Hz), 8.17 (t, 1H, J=5.2 Hz), 7.46 (d, 1H, J=2.0 Hz), 7.13 (d, 1H, J=8.4 Hz), 7.08 (dd, 1H, J=8.4 Hz, J=2.0 Hz), 6.84(m, 2H), 6.51(m, 2H), 4.19(m, 1H), 3.15(m, 2H), 2.98(m, 2H), 1.55(m, 7H), 1.30(m, 1H), 1.05(m, 3H), 0.83(m, 2H). HPLC-MS calcd. for C24H28ClFN4O2(M+H+) 459.19. found 459.4.

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: The title compound was prepared from 2-chlorobenzoxazole, L-cyclohexylalanine and N1-(4-fluoro-phenyl)-ethane-1,2-diamine.2HCl using the procedure analogous to that described in example 2. 1H NMR (DMSO-d6, 400 MHz) δ 8.16(m, 2H), 7.30(m, 1H) 7.16(m, 1H), 7.04(m,1H), 6.92(m, 1H), 6.84(m, 2H), 6.50(m, 2H), 4.24 (m, 1H), 3.15(m, 2H), 2.97(m, 2H), 1.55(m, 7H), 1.30(m, 1H), 1.05(m, 3H), 0.83(m, 2H). HPLC-MS calcd. for C24H29FN4O2 (M+H+)424.23, found 425.5.

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: The title compound was prepared from 2-chlorobenzoxazole, L-cyclohexylalanine and N1-(4-fluoro-phenyl)-ethane-1,2-diamine.2HCl using the procedure analogous to that described in example 2. 1H NMR (DMSO-d6, 400 MHz) δ 8.16(m, 2H), 7.30(m, 1H) 7.16(m, 1H), 7.04(m,1H), 6.92(m, 1H), 6.84(m, 2H), 6.50(m, 2H), 4.24 (m, 1H), 3.15(m, 2H), 2.97(m, 2H), 1.55(m, 7H), 1.30(m, 1H), 1.05(m, 3H), 0.83(m, 2H). HPLC-MS calcd. for C24H29FN4O2 (M+H+)424.23, found 425.5.

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: The title compound was prepared from 2-chloro-5-fluorobenzoxazole, L-cyclohexylalanine and N1-(4-fluoro-phenyl)-ethane-1,2-diamine.2HCl using the procedure analogous to that described in example 2. 1H NMR (DMSO-d6, 400 MHz) δ 8.29 (d, 1H, J=8.0 Hz), 8.16 (t, 1H, J=5.6 Hz), 7.27 (dd, 1H, J=4.4 Hz, J=8.4 Hz), 6.97 (dd, 1H, J=2.6 Hz, J=9.4 Hz), 6.80 (m, 2H), 6.72(m, 1H), 6.46(m, 2H), 5.42(m, 1H), 4.20 (m, 1H), 3.15(m, 2H), 2.95(m, 2H), 1.55(m, 7H), 1.30(m, 1H), 1.05(m, 3H), 0.83(m, 2H). HPLC-MS calcd. for C24H28F2N4O2(M+H+) 443.22, found 443.5.

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: The title compound was prepared from 2-chloro-6-fluorobenzoxazole, L-cyclohexylalanine and N1-(4-fluoro-phenyl)-ethane-1,2-diamine.2HCl using the procedure analogous to that described in example 2. 1H NMR (DMSO-d6, 400 MHz) δ 8.18(m, 2H), 7.30(dd, 1H, J=2.4 Hz, J=8.6 Hz), 7.1 1(dd, 1H, J=4.8 Hz, J=8.4 Hz), 6.89(m, 1H), 6.84(m, 2H), 6.51(m, 2H), 4.28 (m, 1H), 3.15(m, 2H), 2.95(m, 2H), 1.55(m, 7H), 1.30(m, 1H), 1.05(m, 3H), 0.83(m, 2H). HPLC-MS calcd. for C24H28F2N4O2 (M+H+)443.22, found 443.4.

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: The title compound was prepared from 2-chloro-6-fluorobenzoxazole, L-cyclohexylalanine and N1-(4-fluoro-phenyl)-ethane-1,2-diamine.2HCl using the procedure analogous to that described in example 2. 1H NMR (DMSO-d6, 400 MHz) δ 8.18(m, 2H), 7.30(dd, 1H, J=2.4 Hz, J=8.6 Hz), 7.1 1(dd, 1H, J=4.8 Hz, J=8.4 Hz), 6.89(m, 1H), 6.84(m, 2H), 6.51(m, 2H), 4.28 (m, 1H), 3.15(m, 2H), 2.95(m, 2H), 1.55(m, 7H), 1.30(m, 1H), 1.05(m, 3H), 0.83(m, 2H). HPLC-MS calcd. for C24H28F2N4O2 (M+H+)443.22, found 443.4.

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: The title compound was prepared from 2,6-dichlorobenzooxazole, L-cyclohexylalanine and N1-(4-Fluoro-phenyl)-ethane-1,2-diamine.2HCl using the procedure analogous to that described in example 2. 1H NMR (DMSO-d6, 400 MHz) δ 8.30 (d, 1H, J=8.4 Hz), 8.17 (t, 1H, J=5.2 Hz), 7.46 (d, 1H, J=2.0 Hz), 7.13 (d, 1H, J=8.4 Hz), 7.08 (dd, 1H, J=8.4 Hz, J=2.0 Hz), 6.84(m, 2H), 6.51(m, 2H), 4.19(m, 1H), 3.15(m, 2H), 2.98(m, 2H), 1.55(m, 7H), 1.30(m, 1H), 1.05(m, 3H), 0.83(m, 2H). HPLC-MS calcd. for C24H28ClFN4O2(M+H+) 459.19, found 459.4.