tert-Butyl 3-(4-fluoro-1-piperidyl)azetidine-1-carboxylate → 1-(Azetidin-3-yl)-4-fluoropiperidine

関与物質

反応手順

A 25 mL round-bottomed flask was charged with a solution of 3-(4-fluoro-piperidin-1-yl)-azetidine-1-carboxylic acid tert-butyl ester (0.59 g, 2.26 mmol) in DCM/TFA (4 mL/4 mL). The reaction mixture was stirred for 6 h at room temperature. The reaction mixture was loaded onto an Isolute® SCX-2 cartridge. The cartridge was washed with MeOH and the desired product was eluted using 2 M NH3 in MeOH to give 1-Azetidin-3-yl-4-fluoropiperidine as a pale yellow oil (0.263 g, 74%). 1H NMR (CDCl3, 400 MHz) δ 4.60 (m, 1H); 3.64-3.52 (m, 4H); 3.26-3.18 (m, 1H); 2.45-2.38 (m, 2H); 2.28-2.17 (m, 2H); 1.96-1.81 (m, 4H)

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