Ethylenediamine → HCID 58407578, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 187 mg (0.429 mmol) 5-(1,3-dioxan-2-yl)-N-(3-methoxypropyl)-N-methyl-1-{[2-(trimethylsilyl)ethoxy]methyl}-1H-indazol-3-amine (Example 49A) in anhydrous THF (12 ml) were added 6.2 ml (6.2 mmol) tetrabutylammonium fluoride solution (1 M in THF) and ethane-1,2-diamine (145 μl). The solution was stirred at 50° C. for 3 h. After addition of further 6.2 ml tetrabutylammonium fluoride solution (1 M in THF), stirring at 50° C. was continued for 24 h. After cooling, the mixture was concentrated under reduced pressure. The residue was dissolved in ethyl acetate and washed with saturated aqueous sodium hydrogencarbonate solution and with water. The organic layer was dried with sodium sulfate, filtered and evaporated to dryness. The remaining solid (131 mg, 99% of th.) was used in the next step without further purification.

Provenance & Evidence