Synthesis
b) Synthesis of 2-morpholinoacetic acid
Ethyl 2-morpholinoacetate (1 g, 57.8 mmol, 1.0 eq.) was dissolved in 8N HCl and the reaction was stirred at 95°C for 16 hours. Upon completion of the reaction, the reaction mixture was concentrated, quenched, and extracted as in Intermediate Example 15(b). The solvent was removed by distillation to afford the target product 2-morpholinoacetic acid in 96.3% (0.8 g) yield. The product was analyzed by LC-MS (ESI): calculated mass: 145.16; measured mass: 146.3 [M + H]+ (retention time: 0.21 min).
References
[1] Patent: WO2013/53983, 2013, A1. Location in patent: Page/Page column 40
[2] Journal of Medicinal Chemistry, 2000, vol. 43, # 8, p. 1489 - 1494
[3] Liebigs Annalen der Chemie, 1983, # 6, p. 950 - 961
[4] Patent: US2015/11548, 2015, A1. Location in patent: Paragraph 0145
[5] Patent: WO2009/48559, 2009, A1. Location in patent: Page/Page column 70
