Water → HCID 69264825, compound

Participants

Reaction Steps

A mixture of 2-methoxycarbonyl-3-(3-chloro-4-methoxybenzylamino)-5-chloropyrazine (prepared in 297-(3)) 150 mg, 2-hydroxymethylpyrrolidine 88.6 mg and triethylamine 0.12 ml in tetrahydrofuran 5 ml is stirred for 4 hours at room temperature and heated at 50° C. for 2 hours. Then 2-hydroxymethylpyrrolidine 44.3 mg is added thereto and the mixture is heated at 50° C. for 1 hour. After cooling, water is added thereto and the solution is extracted with ethyl acetate. The extract is washed with water and brine, dried over anhydrous sodium sulfate and concentrated in vacuo. The resulting yellowish oil is purified with silica gel frash column chromatography (solvent; chloroform:hexane=1:1) to give (S)-2-methoxycarbonyl-3-(3-chloro-4-methoxybenzylamino)-5-(2-hydroxymethyl-1-pyrrolidinyl)pyrazine as a pale yellowish powder, 123 mg. MS(m/z): 407(M+H)+

Provenance & Evidence