ETHYL 5-FLUORO-1H-INDAZOLE-3-CARBOXYLATE synthesis
- Product Name:ETHYL 5-FLUORO-1H-INDAZOLE-3-CARBOXYLATE
- CAS Number:1016-36-0
- Molecular formula:C10H9FN2O2
- Molecular Weight:208.19
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Yield:1016-36-0 86%
Reaction Conditions:
with sulfuric acid at 20 - 80; for 24 h;Inert atmosphere;
Steps:
33.a 5-Fluoro-1-(4-(4-trifluoromethyl)phenoxy)phenyl)-1H-indazole-3-carboxamide (150)
(a) H2SO4 (1.5 mL) was added to a solution of compound 147 (5 g, Accela ChemBio) in EtOH (150 mL) at room temperature. The reaction mixture was heated at 80° C. under nitrogen for 24 hours. The mixture was concentrated to 40 mL, and diluted with EtOAc/water (200 mL/50 mL). The organic layer was washed with brine, and concentrated to give compound 148 as a white solid (5 g, 86%): 1H-NMR (400 MHz, CDCl3) δ: 7.78 (dd, 1H, 4.3 & 9.2 Hz), 7.73 (dd, 1H, 1.9 & 8.7 Hz), 7.15-7.21 (m, 1H), 4.5 (q, 2H, 7.2 Hz), 1.43 (t, 3H, 7.1 Hz).
References:
US2013/296281,2013,A1 Location in patent:Paragraph 0580
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