Dibutyltin oxide → HCID 178438341, compound

Participants

Reaction Conditions

Reaction Steps

5-[2-Isobutoxy-5-cyano-3-pyridinyl]-2-methyl-3-propyl-2,6-dihydro-7H-pyrazolo[4,3-a]pyrimidin-7-one (Example 36) (200 mg, 0.55 mmol), trimethylsilylazide (0.069 mL, 0.54 mmol) and dibutyltin oxide (54 mg, 0.22 mmol) were heated at 80° C. in toluene (10 mL) for 14 h. The reaction mixture was transferred to a PTFE lined sealed vessel, a further 0.069 mL trimethylsilylazide added and the reaction heated at 80° C. for a further 5 h. After cooling and filtering the filtrate was diluted with pentane. Further solid precipitated and this was combined with the original precipitate and purified by flash column chromatography (eluting with dichloromethane/methanol/ammonia in a ratio of 5:1:0.1) to give 144 mg product.

Provenance & Evidence