Phthalimide → HCID 58303300, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of trans-3-Hydroxy-4-methyl-piperidine-1-carboxylic acid tert-butyl ester (1.78 g, 8.28 mmol) (WO 01/87838), phthalimide (1.46 g, 9.94 mmol) and TPP-resin (4.14 g) in anhydrous THF (30 ml) at 23° C. was added DIAD (2.4 ml, 12.4 mmol). The reaction mixture was stirred at 23° C. for 48 h. then the resin was filtered off and the filtrate was concentrated under reduced pressure to give an oil. The crude oil was purified by flash chromatography using silica gel (0-50% EtOAc-Heptane) which gave the title compound VIIa (1.6 g, 47% yield).

Provenance & Evidence