1: glycine ethyl ester hydrochloric acid With sodium hydrogencarbonate in 2-methyl tetrahydrofuran; water 0.5 h; Cooling; 2: 2-fluoro-benzoyl chloride in 2-methyl tetrahydrofuran; water T=10°C; Schotten-Baumann reaction; 3 h; Cooling;
参考文献
Chavez, Flavio; Kennedy, Nicole; Rawalpally, Thimma; Williamson, R. Thomas; Cleary, Thomas
Organic Process Research and Development, 2010 , vol. 14, # 3 p. 579 - 584
1: 3-cyano-benzoic acid With hydroxylamine in water; tert-butyl alcohol T=38 - 41°C; 21 h; 2: 2-fluoro-benzoyl chloride With triethylamine in water; tert-butyl alcohol T=27 - 40°C; 7 h; 3: With hydrogenchloride; water Product distribution / selectivity; more than 3 stages;
参考文献
PTC THERAPEUTICS, INC.
Patent: WO2008/30570 A1, 2008 ;
Location in patent: Page/Page column 23-24 ;