反应 #88652

反应方程式

7-(2-Methoxy-pyridin-3-yl)-pyrrolo[2,1-f][1,2,4]triazin-2-ol

(±)-4-(4-amino-3-methoxy-phenyl)-3,3-difluoro-piperidine-1-carboxylic acid tert-butyl ester

→

title compound

(±)-[4-(3,3-Difluoro-piperidin-4-yl)-2-methoxy-phenyl]-[7-(2-methoxy-pyridin-3-yl)-pyrrolo[2,1-f][1,2,4]triazin-2-yl]-amine

反应条件

实验过程

7-(2-Methoxy-pyridin-3-yl)-pyrrolo[2,1-f][1,2,4]triazin-2-ol (prepared as described in U.S. Pat. No. 8,471,005/Appl. WO2010071885; 65 mg, 0.27 mmol) and (±)-4-(4-amino-3-methoxy-phenyl)-3,3-difluoro-piperidine-1-carboxylic acid tert-butyl ester (100 mg, 0.29 mmol) were converted to the title compound by a procedure similar to Example 4, to afford a yellow foam (86 mg, 69% yield). 1H NMR (CDCl3): 8.72 (s, 1H), 8.49 (d, J=7.4 Hz, 1H), 8.28 (d, J=8.2 Hz, 1H), 8.24 (m, 1H), 7.51 (s, 1H), 7.14 (d, J=4.0 Hz, 1H), 7.08 (m, 1H), 6.86 (m, 3H), 4.02 (s, 3H), 3.92 (s, 3H), 3.30 (m, 1H), 3.21 (m, 1H), 3.02 (m, 1H), 2.90 (dd, J=30.8 (F_H vic. coupling), 13.7 Hz, 1H), 2.75 (m, 1H), 2.10 (m, 1H), 1.95 (m, 2H); LC/MS (ESI+): 467.0 (M+H).

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