Реакция #41998

Уравнение реакции

N-{3-[5-fluoro-1-(3-iodo-propyl)-indan-1-yl]-1H-indol-7-yl}-methane sulfonamide

morpholine

→

title compound

Выход 83.0%

N-{3-[5-Fluoro-1-(3-morpholin-4-yl-propyl)-indan-1-yl]-1H-indol-7-yl}-methanesulfonamide

Выход 83.0%

Растворители

tetrahydrofuran

Условия реакции

Обработка

1. 1
   ДругоеRemove the volatiles under high vacuum
2. 2
   workup.DISSOLUTIONdissolve the residue in dichloromethane
3. 3
   workup.ADDITIONadd solid potassium carbonate
4. 4
   Фильтрацияfilter
5. 5
   Концентрированиеconcentrate in vacuo
6. 6
   ДругоеPurify the residue on silica eluting with 5 to 10% methanol in dichloromethane over 15 minutes

Методика

Combine N-{3-[5-fluoro-1-(3-iodo-propyl)-indan-1-yl]-1H-indol-7-yl}-methane sulfonamide (65 mg, 0.13 mmol) and morpholine (2 ml) in anhydrous tetrahydrofuran (2.5 ml) and stir at room temperature under nitrogen overnight. Remove the volatiles under high vacuum, dissolve the residue in dichloromethane, add solid potassium carbonate, stir for ten minutes, filter, and concentrate in vacuo. Purify the residue on silica eluting with 5 to 10% methanol in dichloromethane over 15 minutes to obtain the title compound as a white solid (50 mg, 83%). LC-MS m/z 472.2 (M++1).

Источник