Synthesis
GENERAL METHOD: An appropriate amount of diketone (9a or 9b) (0.3 mol) was mixed with ethanol (500 mL), heated to 80 °C and refluxed for 5 hours. Upon completion of the reaction, the mixture was cooled to room temperature and the solvent was removed by distillation under reduced pressure to give the target product ester (10a or 10b) in the form of a red oil.
7.10.1 Preparation of ethyl 3-(2-fluorophenyl)-3-oxopropanoate (10a): the product obtained was a red oily material in 85% yield; mass spectrum (ESI) m/z: 233.1 [M + Na] , 443.1 [2M + Na]
References
[1] Bioorganic and Medicinal Chemistry, 2013, vol. 21, # 11, p. 2843 - 2855
[2] Archiv der Pharmazie, 2013, vol. 346, # 7, p. 521 - 533
[3] Patent: EP2799437, 2014, A1. Location in patent: Paragraph 0057
[4] Patent: US2014/364431, 2014, A1. Location in patent: Paragraph 0188
[5] Patent: WO2017/37672, 2017, A1. Location in patent: Page/Page column 48
