反应详情

温度

200 °C

DIPEA (2 eq.), K2CO3(4 eq.) and tert-butyl benzyl[(3-chloropropyl)sulfonyl]carbamate (was added to a solution of methyl (7S)-14-cyclohexyl-7-[2-(methylamino)ethoxy]-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylate (0.08 M) in MeCN. The mixture was heated in the microwave at 200° C. for 30 min. The resulting mixture was filtered, concentrated in vacuo, and the residue purified by RP-HPLC (WATERS XTERRA column, C18, 5 um, 19×150 mm. Mobile phase: MeCN/H2O buffered with 0.1% TFA). Fractions containing the pure compound were combined and freeze dried to afford the title compound (23%) as a white powder. (ES+) m/z 674 (M+H)+.

1. filtrationThe resulting mixture was filtered
2. concentrationconcentrated in vacuo
3. customthe residue purified by RP-HPLC (WATERS XTERRA column, C18, 5 um, 19×150 mm. Mobile phase: MeCN/H2O buffered with 0.1% TFA)
4. additionFractions containing the pure compound
5. customfreeze dried