反应详情

A solution of 8-carbamoyl-7-chloro-6-phenyl-3,4-dihydro-1H-pyrrolo[1,2-a]pyrazine-2-carboxylic acid tert-butyl ester (2.75 g, Reference Example 2) in dichloromethane (60 mL) was treated with trifluoroacetic acid (5.64 mL). After stirring at room temperature for a further 3 hours the reaction mixture was further treated with trifluoroacetic acid (0.5 mL) and then further stirred for 1 hour. The reaction mixture was evaporated to afford an oil, which was azeotroped with toluene and then triturated with diethyl ether to give the title compound (2.61 g) as a white solid, m.p. 205–208° C. [Elemental Analysis: C, 49.32; H, 3.88; N, 10.78%. Calculated for C16H15ClF3N3O3: C, 49.30; H, 3.88; N, 10.78%].

1. stirringfurther stirred for 1 hour
2. customThe reaction mixture was evaporated
3. customto afford an oil, which
4. customwas azeotroped with toluene
5. customtriturated with diethyl ether