반응 #49493

ord-ce138090a4a54cb38cae9b163b2fc22c

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타followed by purification by preparative thin-layer chromatography (chloroform/methanol=5/1)

실험 절차

In a similar manner to Step 2 of Example 161, 4-trifluoromethanesulfonyloxy-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone (60.0 mg, 0.101 mmol) was dissolved in diethylamine (3.0 mL), and the solution was treated with bis(triphenylphosphine)dichloropalladium (8.6 mg, 0.012 mmol), copper iodide (6.9 mg, 0.036 mmol), propargyl alcohol (0.029 mL, 0.51 mmol), followed by purification by preparative thin-layer chromatography (chloroform/methanol=5/1) to obtain 4-(3-hydroxy-1-propinyl)-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone (18.8 mg, yield 37%).

출처

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