反应详情

温度

95 °C

Add water (1.3 L) and 36.5% hydrochloric acid (9.07 Kg, 90.81 moles) to a mixture of dimethyl (3R)-5-bromo-3,4-dihydro-1H-isoquinoline-2,3-dicarboxylate and (3R)-5-bromo-2-methoxycarbonyl-3,4-dihydro-1H-isoquinoline-3-carboxylic acid (Preparation 3a) (520 g, 1.27 moles) in an appropriate vessel and stir the mixture at 95° C. After 12 hours cool the mixture to 10° C. and stir for 15 minutes. Filter the mixture and dry the solid under vacuum at 40° C. give the title compound (332 g, 1.13 moles). MS (m/z): 256.1 (M-Cl (79Br)), 258 (M-Cl (81Br)).

1. temperatureAfter 12 hours cool the mixture to 10° C.
2. stirringstir for 15 minutes
3. filtrationFilter the mixture
4. customdry the solid under vacuum at 40° C.