5-DifluoroMethoxyindazole-3-carboxylic acid synthesis
- Product Name:5-DifluoroMethoxyindazole-3-carboxylic acid
- CAS Number:858661-78-6
- Molecular formula:C9H6F2N2O3
- Molecular Weight:228.15
858671-83-7
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Yield:858661-78-6 27%
Reaction Conditions:
Stage #1: C13H12F2N2O4with sodium hydroxide;water at 60; for 24 h;
Stage #2: with hydrogenchloride pH=1;
Steps:
9
The ester (63.8 mmol), sodium hydroxide (193 mmol), and water (65 mL) were combined and the reaction was maintained for 24 h at 60 °C. After cooling to rt, the aqueous layer was washed with dichloromethane (3x50mL). The aqueous layer was adjusted to pH 1 with concentrated hydrochloric acid. The precipitated solids were collected by filtration, washed with water and dichloromethane, and dried to provide the acid in 27% yield. The following acids were prepared according to this method: 5- (Difluoromethoxy)-1H-indazole-3-carboxylic acid.
References:
WO2005/63767,2005,A2 Location in patent:Page/Page column 47
1352396-52-1
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858661-78-6
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