tert-Butyl 2,7-diazaspiro[3.5]nonane-2-carboxylate → 6-[2-(tert-Butoxycarbonyl)-2,7-diazaspiro[3.5]nonan-7-yl]-4-(5-methyl-1H-pyrazol-3-ylamino)-2-[2-{3-(pyrid-2-yl)isoxazol-5-yl}pyrrolidin-1-yl]pyrimidine

Participants

Reaction Conditions

Reaction Steps

A mixture of 6-chloro-N-(3-methyl-1H-pyrazol-5-yl)-2-[2-(3-pyridin-2-ylisoxazol-5-yl)pyrrolidin-1-yl]pyrimidin-4-amine (Example 17) (300 mg, 0.7 mmol) and 2-(tert-butoxycarbonyl)-2,7-diazaspiro[3.5]nonane (949 mg, 4.2 mmol) in 1,4-dioxane (8 ml) was heated at 160° C. in a sealed vessel under microwave irradiation for 120 minutes. The mixture was allowed to cool and the volatiles removed by evaporation. The residue was purified by column chromatography on silica gel eluting with DCM/methanol/aqueous ammonia (100:0:0 increasing in polarity to 90:10:1) to give the product (235 mg, 55%) as a mauve solid.

Provenance & Evidence