Methanamine, N-methoxy-, hydrochloride (1:1) → HCID 135423127, compound

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Reaction Steps

The title compound of Example 86 (710 mg, 1.8 mmol) was dissolved in dichloromethane (150 mL), 1-hydroxybenzotriazole hydrate (263 mg, 1.95 mmol), N,N-diisopropylethylamine (1.26 mL, 7 mmol) and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (374 mg, 1.95 mmol) were added followed by N,O-dimethylhydroxylamine hydrochloride (173 mg, 1.8 mmol), and the resultant mixture stirred at room temperature for 14 h. Saturated aq. sodium hydrogen carbonate (80 mL) and dichloromethane (50 mL) were added, the organic phase removed and the aqueous phase extracted with dichloromethane (2×50 mL). The combined organic phases were dried over MgSO4, concentrated and purified by column chromatography (dichloromethane to 10% methanol in dichloromethane as eluant) to afford the title compound as a yellow oil (590 mg, 1.3 mmol).

Provenance & Evidence