Yield: 100%

Reaction Conditions:

with ammonia in ethanol at 100; for 5 h;Sealed tube;

Steps:

30 Preparation 30Ethyl (3-a m i nooxeta n -3-yl )acetate
Preparation 30Ethyl (3-a m i nooxeta n -3-yl )acetateEthyl oxetan-3-ylideneacetate (Preparation 38, 781 g, 5.49 mol) was dissolved in 2M ammonia in ethanol (8.24 L) and heated to 100°C in a bomb for 5 hours. The reaction was concentrated in vacuo to afford the title compound as a mobile oil (750 g, 100% yield).¹HNMR (CDCIs): ? 1 .25 (t, 3H), 2.0 (br s, 2H), 2.85 (s, 2H), 4.2 (q, 2H), 4.5 (d, 2H), 4.55 (d, 2H).

References:

PFIZER LIMITED;BAGAL, Sharanjeet Kaur;KEMP, Mark Ian;MILLER, Duncan Charles;MURATA, Yoshihisa WO2013/61205, 2013, A2 Location in patent:Page/Page column 63