Pyrrolidine → HCID 58043119, compound

Participants

Reaction Conditions

Reaction Steps

Pyrrolidine (0.60 g, 8.4 mmol) was added to a solution of 59B (2.0 g, 6.5 mmol) and DCM (25 mL). The mixture was cooled to 0° C. and then DIPEA and TBTU were added in the given order. The mixture was stirred at 0° C. for 20 min and then at RT for 1.5 h. The solution was washed with aqueous Na2CO3 (1M) and then the organic solution was evaporated. The product was purified by silica-gel chromatography using 1-5% methanol in DCM. There was obtained 2.3 g (98%) of 59C as an oil. 1H NMR (500 MHz, CDCl3): δ 1.42 (s, 9H), 1.89 (m, 4H), 3.41 (m, 2H), 3.62 (m, 2H), 3.86 (m, 2H), 4.04 (m, 1H), 4.34 (m, 2H), 7.19 (d, 2H), 7.45 (d, 2H), MS (APCI+) m/z 363 [M+H]+.

Provenance & Evidence