1: (2R)-3-Bromo-2-hydroxy-2-methylpropanoic Acid With thionyl chloride in isobutyramide T=-10°C; Inert atmosphere; 2: 4-amino-2-(trifluoromethyl)benzonitrile in isobutyramide T=20°C;
参考文献
CONSIGLIO NAZIONALE DELLE RICERCHE; ISTITUTO SCIENTIFICO ROMAGNOLO PER LO STUDIO E LA CURA DEI TUMORI (I.R.S.T.) S.R.L.; VARCHI, Greta; TESEI, Anna; GUERRINI, Andrea; BRIGLIADORI, Giovanni
Patent: WO2010/116342 A2, 2010 ;
Location in patent: Page/Page column 42-43 ;
1: 3-bromomethyl-3-methyl-tetrahydro-pyrrolo[2,1-c][1,4]oxazine-1,4-dione With hydrogenchloride Hydrolysis; Heating; 2: With thionyl chloride; dimethylammonium 2,4-dichlorophenoxyacetate T=-10 - -5°C; Chlorination; 3: 4-amino-2-(trifluoromethyl)benzonitrile With dimethylammonium 2,4-dichlorophenoxyacetate Acylation; Further stages. Title compound not separated from byproducts.;
参考文献
Kirkovsky, Leonid; Mukherjee, Arnab; Yin, Donghua; Dalton, James T.; Miller, Duane D.
Journal of Medicinal Chemistry, 2000 , vol. 43, # 4 p. 581 - 590
1: N1-[4-cyano-3-(trifluoromethyl)phenyl]-(2R)-3-bromo-2-hydroxy-2-methylpropanamide With potassium carbonate in acetone 2 h; Reflux; 2: α-naphthol in isopropyl alcohol 18 h; Reflux;
参考文献
Duke III, Charles B.; Jones, Amanda; Bohl, Casey E.; Dalton, James T.; Miller, Duane D.
Journal of Medicinal Chemistry, 2011 , vol. 54, # 11 p. 3973 - 3976