Phosphorus oxychloride → HCID 59730557, compound

Participants

Reaction Steps

4-Hydroxy-4-(1-H-indol-4-yl)-piperidine-1-carboxylic acid tert-butyl ester 4-5 (1.0 g, 3.17 mmol) was combined with pyridine (20 mL) and phosphorus oxychloride (0.7 mL, 7.4 mmol) at room temperature under nitrogen, and was stirred overnight. The reaction was partitioned between ethyl acetate (55 mL) and water (55 mL). The ethyl acetate layer was washed with water (2×30 mL) and brine (55 mL), then dried (MgSO4), filtered and concentrated to afford (670 mg, 71%) of 4-(1H-Indol-4-yl)-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester 4-6.

Provenance & Evidence