Azaindole derivatives as cftr modulators
A technology of -CONR and compounds, applied in the field of azaindole derivatives as CFTR regulators, can solve problems such as increasing the severity of diseases
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[0256] Table 2 below contains a listing of carboxylic acid synthesis materials that are commercially available or prepared by one of the methods described below.
[0257] Table 2: Carboxylic acid building blocks.
[0258]
[0259] 1. Preparation A-3 :1-Benzo[d][1,3]dioxol-5-yl-cyclopropanecarboxylic acid
[0260]
[0261] At 70 °C, heat benzo[1,3]dioxole-5-acetonitrile (5.10 g, 31.7 mmol), 1-bromo-2-chloro-ethane (9.00 mL, 109 mmol) and chloride A mixture of benzyltriethylammonium (0.181 g, 0.795 mmol), then 50% (wt / wt) aqueous sodium hydroxide (26 mL) was slowly added to the mixture. The reaction was stirred at 70°C for 18 hours, then heated at 130°C for 24 hours. The dark brown reaction mixture was diluted with water (400 mL), extracted once with an equal volume of ethyl acetate and once with an equal volume of dichloromethane. The basic aqueous solution was acidified to pH less than 1 with concentrated hydrochloric acid, and the precipitate was filtered and washe...
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