Synthesis
General procedure for the synthesis of 3-(benzyloxy)azetidine-1-carboxylic acid tert-butyl ester from 3-(benzyloxy)azetidine-1-carboxylic acid: tert-butyl ester of 3-(benzyloxy)azetidine-1-carboxylic acid (1.0 g) was placed in a round-bottomed flask, methanol-HCl solution (15 ml, 20%) was added, and the reaction was stirred for 1 h at room temperature. The reaction progress was monitored by thin layer chromatography (TLC). After completion of the reaction, the solvent was evaporated under reduced pressure to give the crude product as a white solid. The crude product was washed several times with ethyl acetate and dried thoroughly to afford the target compound 3-(benzyloxy)azetidine hydrochloride as a white solid in 92% yield, which can be used for subsequent reactions without further purification.
References
[1] Patent: WO2012/83246, 2012, A1. Location in patent: Page/Page column 46
[2] Patent: US9388164, 2016, B2. Location in patent: Page/Page column 74; 75
[3] Organic Letters, 2017, vol. 19, # 9, p. 2270 - 2273
[4] Patent: WO2017/202704, 2017, A1. Location in patent: Page/Page column 44; 45
