4-Methylmorpholine → HCID 58465654, compound

Participants

Reaction Steps

To a solution of 5-[(2-nitrophenyl)sulfonyl]-5,6,7,8-tetrahydro-4H-pyrazolo[1,5-a][1,4]diazepine-2-carboxylic acid (0.116 g, 0.316 mmol) and O-(tetrahydropyran-2-yl)hydroxylamine (0.0407 g, 0.347 mmol) in methylene chloride (2.5 mL) was added N,N,N′,N′-tetramethyl-O-(7-azabenzotriazol-1-yl)uronium hexafluorophosphate (0.144 g, 0.379 mmol) and N-methylmorpholine (0.1 mL, 0.9 mmol). The resulting reaction mixture was stirred at room temperature overnight. The solvent was evaporated and the residue obtained purified via silica chromatography (80-100% EtOAc/hexane) to afford Intermediate 21 as a clear colorless oil (0.152 g, 100%). LC-MS: (FA) ES+466.

Provenance & Evidence