Citation:
ZHUO Lin-Sheng, DONG Huan, HUANG Wei, ZHAO Xing-E, SHE Neng-Fang. Synthesis, Crystal Structure and Biological Activity of 8-((4-((2,3-diaminopyridin-4-yl)oxy)-3-fluorophenyl)-amino)-2-(4-fluorophenyl)-3-methyl-2,7-naphthyridin-1(2H)-one[J]. Chinese Journal of Structural Chemistry,
2014, 33(6): 859-864.
Synthesis, Crystal Structure and Biological Activity of 8-((4-((2,3-diaminopyridin-4-yl)oxy)-3-fluorophenyl)-amino)-2-(4-fluorophenyl)-3-methyl-2,7-naphthyridin-1(2H)-one
摘要:
The new title compound 8-((4-((2,3-diaminopyridin-4-yl)-oxy)-3-fluorophenyl)-amino)-2-(4-fluorophenyl)-3-methyl-2,7-naphthyridin-1(2H)-one (C26H20F2N6O2, Mr=486.48) has been prepared and determined by single-crystal X-ray diffraction. The crystal is of monoclinic, space group P21/c with a=15.365(3), b=13.144(2), c=11.863(2)Å, β=108.882(3)°, Z=4, V=2267.0(7)Å3, Dc=1.425 g/cm3, F(000)=1008, μ=0.105 mm-1, MoKa radiation (λ=0.71073Å), R=0.0480 and wR=0.1294 for 3197 observed reflections with I>2σ(I). X-ray diffraction analysis reveals that the region C (substituents of 8-amino group and 3-methyl group on the 2,7-naphthyridin-1(2H)-one ring) of compound 6 are effectively planar. Intramolecular and intermolecular hydrogen bonds together with π…π interations are found in the structure. In addition, compound 6 shows potent c-Met and c-Kit kinase inhibition activities.
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关键词:
- naphthyridine
- / crystal structure
- / synthesis
- / c-Met inhibitor
English
Synthesis, Crystal Structure and Biological Activity of 8-((4-((2,3-diaminopyridin-4-yl)oxy)-3-fluorophenyl)-amino)-2-(4-fluorophenyl)-3-methyl-2,7-naphthyridin-1(2H)-one
Abstract:
The new title compound 8-((4-((2,3-diaminopyridin-4-yl)-oxy)-3-fluorophenyl)-amino)-2-(4-fluorophenyl)-3-methyl-2,7-naphthyridin-1(2H)-one (C26H20F2N6O2, Mr=486.48) has been prepared and determined by single-crystal X-ray diffraction. The crystal is of monoclinic, space group P21/c with a=15.365(3), b=13.144(2), c=11.863(2)Å, β=108.882(3)°, Z=4, V=2267.0(7)Å3, Dc=1.425 g/cm3, F(000)=1008, μ=0.105 mm-1, MoKa radiation (λ=0.71073Å), R=0.0480 and wR=0.1294 for 3197 observed reflections with I>2σ(I). X-ray diffraction analysis reveals that the region C (substituents of 8-amino group and 3-methyl group on the 2,7-naphthyridin-1(2H)-one ring) of compound 6 are effectively planar. Intramolecular and intermolecular hydrogen bonds together with π…π interations are found in the structure. In addition, compound 6 shows potent c-Met and c-Kit kinase inhibition activities.
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Key words:
- naphthyridine
- / crystal structure
- / synthesis
- / c-Met inhibitor
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