Tert-butyl 3-(methanesulfonyloxy)azetidine-1-carboxylate → tert-Butyl 3-(3-fluoro-4-(pyrrolidin-1-ylmethyl)phenoxy)azetidine-1-carboxylate

Participants

Reaction Steps

Using a similar protocol as described in Example 29C employing 31A (6.6 g, 33.8 mmol) and tert-butyl 3-(methylsulfonyloxy)azetidine-1-carboxylate (10.2 g, 40.6 mmol) as starting materials afforded 9.4 g (80%) of 31B as a solid. 1H NMR (500 MHz, CDCl3): δ 1.45 (s, 9H), 1.77 (m, 4H), 2.52 (m, 4H), 3.61 (s, 2H), 3.99 (m, 2H), 4.27 (m, 2H), 4.84 (m, 1H), 6.43 (dd, 1H), 6.49 (dd, 1H), 7.27 (t, 1H), MS (APCI+) m/z 351 [M+H]+.

Provenance & Evidence