2-PYRROLIDIN-1-YL-PROPIONIC ACID synthesis

Yield:-

Reaction Conditions:

with water;sodium hydroxide at 20; for 3 h;Cooling with ice;

Steps:

65

[0332] In an ice bath, an aqueous 10 wt% NaOH (0.52 g/5.2 ml) solution was added to Compound 2 (1.5 g, 8.76mmol). A reaction solution was stirred for 3 hours at room temperature. The reaction solution was poured onto ice andpH was adjusted to approximately 2 using an aqueous 4 M HCl solution. EA was added thereto and an aqueous layerwas washed several times, and then a separated aqueous layer was vacuum evaporated. A concentrated solution wasdissolved in MC and MeOH again and undissolved solids were filtered out. The filtered solution was vacuum evaporatedand then intactly collected.Ivory solid (quantitative)1H NMR (300 MHz, DMSO) δ 10.99 (br, s, 1H), 4.18 (q, J= 6.6 Hz, 1H) 3.74-3.13 (m, 4H), 1.91 (s, 4H), 1.50 (d, J= 7.1 Hz, 3H)

References:

EP3091003,2016,A1 Location in patent:Paragraph 0330; 0332