MS (ESI) 372

MS (ESI) 372.3 [M + H]+. 6,7-Dimethoxy-N-(1-methylpiperidin-4-yl)-2-(piperidin-1-yl)-quinazolin-4-amine (12) The name compound (80% more than 2 techniques) was ready according to man made process of 4. The extreme potency lack of the ethoxy and isopropoxy analogues features the need for the interactions between your simple amino group and Leu1086 and Tyr1154. We found that also, as the fluoro group (47) totally abolished the actions against both GLP and G9a, the methyl group (48) was tolerated with no more than 2C3-fold potency reduction for GLP (IC50 = 29 12 nM) and G9a (IC50 = 1150 47 nM). Having set up preliminary SAR for the 6.92 (s, 1H), 6.79 (s, 1H), 5.21 (d, = 7.2 Hz, 1H), 4.17C4.12 (m, 1H), 3.96 (s, 3H), 3.95 (s, 3H), 3.83C3.79 (m, 8H), 2.90 (d, = 10.8 Hz, 2H), 2.33 (s, 3H), 2.21C2.15 (m, 4H), 1.71C1.61 (m, 2H). 13C NMR (151 MHz, CDCl3) 158.95, 158.32, 154.45, 149.05, 145.68, 106.11, 103.39, 100.69, 67.10, 56.32, 55.98, 54.80, Acetyllovastatin 47.75, 46.20, 44.67, 32.13. HRMS(ESI-TOF) 6.87 (s, 1H), 6.73 (s, 1H), 5.13 (d, = 7.6 Hz, 1H), 4.08C4.05 (m, 1H), 3.90 (s, 3H), 3.88 (s, 3H), 3.78C3.73 (m, 8H), 2.93 (d, = 12.0 Hz, 2H), 2.41 (q, = 6.8 Hz, 2H), 2.14C2.08 (m, 4H), 1.63C1.54 (m, 2H), 1.07 (q, = 7.2 Hz, 3H). MS (ESI) 402.3 [M + H]+. 6,7-Dimethoxy-2-morpholino-N-(1-propylpiperidin-4-yl)-quinazolin-4-amine (8) The name substance (76% over 2 techniques) was ready according to artificial process of 4. 1H NMR (400 MHz, CDCl3) 6.89 (s, 1H), 6.74 (s, 1H), 5.12 (d, = 7.2 Hz, 1H), 4.13C4.10 (m, 1H), 3.93 (s, 3H), 3.91 (s, 3H), 3.81C3.74 (m, 8H), 2.92 (d, = 11.6 Hz, 2H), 2.30 (q, = 6.8 Hz, 2H), 2.15C2.11 (m, 4H), 1.61C1.47 (m, 4H), 0.90 (q, = 7.2 Hz, 3H). MS (ESI) 416.1 [M + H]+. N-(1-Isopropylpiperidin-4-yl)-6,7-dimethoxy-2-morpholinoquinazolin-4-amine (9) The name substance (85% over 2 techniques) was ready according to artificial process of 4. 1H NMR (400 MHz, CDCl3) 6.88 (s, 1H), Acetyllovastatin 6.78 (s, 1H), 5.24 (d, = 7.2 Hz, 1H), 4.12C4.03 (m, 1H), 3.91 Acetyllovastatin (s, 3H), 3.89 (s, 3H), 3.81C3.74 (m, 8H), 2.91 (d, = 12.0 Hz, 2H), 2.81C2.75 (m, 1H), 2.33 (t, = 10.8 Hz, 2H), 2.16C2.14 (m, 2H), 1.67C1.58 (m, 2H), 1.06 (d, = 6.8 Hz, 6H). MS (ESI) 416.3 [M + H]+. N-(1-Cyclopropylpiperidin-4-yl)-6,7-dimethoxy-2-morpholinoquinazolin-4-amine (10) The name substance (77% over 2 techniques) was ready according to artificial process of 4. 1H NMR (400 MHz, CDCl3) 6.91 (s, 1H), 6.70 (s, 1H), 5.01 (d, = 6.8 Hz, 1H), 4.18C4.08 (m, 1H), 3.95 (s, 3H), 3.92 (s, 3H), 3.83C3.77 (m, 8H), 3.04 (d, = 12.4 Hz, 2H), 2.39 (td, = 11.6, 3.6 Hz, 2H), 2.15C2.11 (m, 2H), 1.66C1.60 Rabbit Polyclonal to CNTN4 (m, Acetyllovastatin 1H), 1.54 (qd, = 11.2, 4.0 Hz, 2H), 0.49C0.45 (m, 2H), 0.44C0.40 (m, 2H). MS (ESI) 414.3 [M + H]+. 6,7-Dimethoxy-N-(1-methylpiperidin-4-yl)-2-(pyrrolidin-1-yl)-quinazolin-4-amine (11) The name substance (80% over 2 techniques) was ready according to artificial process of 4. 1H NMR (400 MHz, CDCl3) 6.92 (s, 1H), 6.78 (s, 1H), 5.12 (d, = 6.8 Hz, 1H), 4.19C4.09 (m, 1H), 3.91 (s, 3H), 3.89 (s, 3H), 3.64C3.60 (m, 4H), 2.85 (d, = 12.0 Hz, 2H), 2.30 (s, 3H), 2.18C2.13 (m, 4H), 1.96C1.93 (m, 4H), 1.64C1.55 (m, 2H). MS (ESI) 372.3 [M + H]+. 6,7-Dimethoxy-N-(1-methylpiperidin-4-yl)-2-(piperidin-1-yl)-quinazolin-4-amine (12) The name substance (80% over 2 techniques) was ready according to artificial process of 4. 1H NMR (400 MHz, MeOH-7.64 (s, 1H), 7.11 (s, 1H), 4.58C4.46 (m, 1H), 3.94 (s, 3H), 3.90 (s, 3H), 3.87C3.81 (m, 4H), 3.63 (d, = 12.8 Hz, 2H), 3.26C3.19 (m, 1H), 2.89 (s, 3H), 2.34 (d, = 12.9 Hz, 2H), 2.10C1.96 (m, 2H), 1.82C1.66 (m, 7H). MS (ESI) 386.3 [M + H]+. 2-(4,4-Difluoropiperidin-1-yl)-6,7-dimethoxy-N-(1-methylpiperidin-4-yl)quinazolin-4-amine (13) Acetyllovastatin The name substance (84% over 2 techniques) was ready according to artificial process of 4. 1H NMR (400 MHz, CDCl3) 6.89 (s, 1H), 6.71 (s, 1H), 5.01 (d, = 7.2 Hz, 1H), 4.15C4.05 (m, 1H), 3.99 (t, = 6.0 Hz, 4H), 3.96 (s, 3H), 3.95 (s, 3H), 2.89C2.86 (m, 2H), 2.33 (s, 3H), 2.22C2.13 (m, 4H), 2.06C1.96 (m, 4H), 1.69C1.59 (m, 2H). MS (ESI) 422.3 [M + H]+. 2-(Azepan-1-yl)-6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-quinazolin-4-amine (14) The name substance (79% over 2 techniques) was ready according to artificial process of 4. 1H NMR (400 MHz, CDCl3) 6.88 (s, 1H), 6.72 (s, 1H), 4.97 (d, = 6.4 Hz, 1H), 4.12C4.05 (m, 1H), 3.93 (s, 3H), 3.91 (s, 3H), 3.78 (t, = 6.0 Hz, 4H), 2.88C2.85 (m, 2H), 2.33 (s, 3H), 2.17C2.13 (m, 4H), 1.82C1.74 (m, 4H), 1.64C1.53 (m, 6H). MS (ESI).

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