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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 2267869Generated: November 1, 2026

Tert-Butyl nitrite → 4-m-Tolyloxy-1H-indole-2-carboxylic acid ethyl ester

https://huagongshe.com/reaction/2267869

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTert-Butyl nitriteHCID 10906—
Reactant4-(2-Amino-5-methyl-phenoxy)-1H-indole-2-carboxylic acid ethyl esterHCID 66841523—
SolventDiethyl EtherHCID 3283—
SolventDimethylformamideHCID 6228—
Product4-m-Tolyloxy-1H-indole-2-carboxylic acid ethyl esterHCID 66841702—

Reaction Conditions

Temperature65 °C

Reaction Steps

Tert-butyl nitrite (0.428 ml, 3.609 mmol) is dissolved in 5 ml of dimethylformamide and heated to 65° C. A solution of 135 (1.1 g, 3.609 mmol) in 5 ml of dimethylformamide is added dropwise and the mixture is stirred of additional 10 minutes. The brown solution is cooled to room temperature, diluted with diethyl ether and washed with 2N HCl and brine. The organic layers are dried over sodium sulphate and evaporated. The crude product (930 mg of a brown oil) is further purified by flash-chromatography (hexane/ethyl acetate 7:3).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07858781B2
Source datasetuspto-grants-2010_12
ORD IDord-2720ce829c1d466aa244f8e6913d3b23
Source noteuspto-grants-2010_12