Water → HCID 58280123, compound

Participants

Reaction Conditions

Reaction Steps

Dissolve 631.7 mg (1.87 mmol) of 4-chloro-5-(4-methoxyphenyl)-6-phenylfuro[2,3-d]pyrimidine and 490 mg (1.71 mmol) of tert-butyl(2R,4R)-4-hydroxy-2-(3-methoxy-3-oxopropyl)piperidine-1-carboxylate in 1 ml of DMF, cool to −10° C. and add 1.02 ml (2.05 mmol) of phosphazene base P2-t-Bu (approx. 2 M solution in THF). Stir the reaction mixture at 0° C. for 1 h and then add to water. Extract three times with dichloromethane, combine the organic phases, wash with satd. sodium chloride solution and dry over magnesium sulphate. After concentrating under reduced pressure, purify the product by chromatography on silica gel (eluent: cyclohexane/ethyl acetate 20:1→3:1). 420 mg (38.1% of theory) of the target compound are obtained.

Provenance & Evidence