반응 #49420

ord-184acb04f5cf477ea9e532ae5e34a17c

반응 방정식

CC(C)(C)OC(=O)n1c(-c2ccc(O)c3c2C(=O)NC3)cc2cc(CN3CCCCC3)ccc21
4-hydroxy-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone
CCN(CC)CC
triethylamine
O=S(=O)(Cl)c1ccc(C(F)(F)F)cc1
4-trifluoromethylbenzenesulfonyl chloride
CC(C)(C)OC(=O)n1c(-c2ccc(OS(=O)(=O)c3ccc(C(F)(F)F)cc3)c3c2C(=O)NC3)cc2cc(CN3CCCCC3)ccc21
4-(4-trifluoromethylbenzenesulfonyloxy)-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone
수율 27.1%

반응 조건

상세 조건
See reaction.notes.procedure_details.

실험 절차

In a similar manner to Step 1 of Example 233, 4-hydroxy-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone (0.0310 g, 0.0672 mmol) was dissolved in acetonitrile (0.650 mL), and the solution was treated with triethylamine (0.0540 mL, 0.390 mmol) and 4-trifluoromethylbenzenesulfonyl chloride (0.0477 mL, 0.195 mmol) to obtain 4-(4-trifluoromethylbenzenesulfonyloxy)-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone (0.0122 g, yield 27%).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07745641B2uspto-grants-2010_06