反应详情

Five grams of 2-pivaloylamino-4-hydroxy-6-(4-carboxyphenylethynyl)pyrido[2,3-d]pyrimidine described in European Pat. Application No. 87308921.3) and 1.60 g. of platinum oxide in 200mL. of trifluoroacetic acid were hydrogenated in a Parr apparatus at ambient temperature and 60 psi for 24 hours. Removal of the catalyst by filtration and concentration of the filtrate yielded 2-pivaloylamino-4-hydroxy-6-[2-(4-carboxycyclohex-1-yl)ethyl]-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine as a white solid which was further purified by column chromatography (Waters 200) eluting with 1:9 methanol:dichloromethane. m.p. 218°-234° C. Anal. Calc. for C21H32N4O4 : C, 63.35; H, 7.97; N, 13.85. Found: C, 63.30; H, 7.48; N, 13.57.

1. customwere hydrogenated in a Parr apparatus at ambient temperature
2. customRemoval of the catalyst
3. filtrationby filtration and concentration of the filtrate