2,1,3-Benzothiadiazol-5-amine → HCID 86627853, compound

Participants

Reaction Steps

62 mg of potassium tert-butoxide are added in 3 installments, at ambient temperature under argon, to 180 mg of compound of formula (II), described below, 8-[3-((tert-butyl)dimethylsilanyl)prop-2-ynyl]-6-(2,6-dichlorophenyl)-2-methylsulfonyl-8H-pyrido[2,3-d]pyrimidin-7-one, and 81 mg of the compound of formula (III), 2,1,3-benzothiadiazol-5-ylamine, in solution in 5 ml of DMSO. After a contact time of 75 min, the reaction medium is diluted with a mixture of water and ethyl acetate. The aqueous phase is brought back to neutral pH and extracted with dichloromethane. After drying the organic phase over sodium sulfate and filtering, the residue is chromatographed on silica (gradient: CH2Cl2 100 to CH2Cl2/MeOH 98:2) to give 52 mg of the expected product.

Provenance & Evidence