1,2-Dichloroethane → (1-(4-fluorobenzyl)-1H-indol-2-yl)(4-(piperidin-1-ylmethyl)piperidin-1-yl)methanone

The following was added to anhydrous DMF (2 mL) sequentially: 1-(4-fluorobenzyl)-1H-indole-2-carboxylic acid (66.8 mg, 0.248 mmol), Hunig's Base (0.217 ml, 1.240 mmol), EDC (52.3 mg, 0.273 mmol), HOBT (41.8 mg, 0.273 mmol), and 1-(piperidin-4-ylmethyl)piperidine (45.2 mg, 0.248 mmol) (from SJB-2-083.) This was stirred at room temperature for 24 h with 3 Å MS. At this time, a 1:1 solution of EtOAc:Et2O was added and the solution was washed with 10% aq. Na2CO3. The organic phase was dried with MgSO4 and concentrated in vacuo. The residue was then purified by silica gel chromatography (20 g silica, 80% EtOAc/Hexanes) to give 58 mg of the title compound as an oil.

1. washthe solution was washed with 10% aq. Na2CO3
2. dry with materialThe organic phase was dried with MgSO4
3. concentrationconcentrated in vacuo
4. customThe residue was then purified by silica gel chromatography (20 g silica, 80% EtOAc/Hexanes)

ORD 기록

ord-44aac94db3cf41a589a1708213bec840

출처 데이터셋

uspto-grants-2014_09

DOI

10.6084/m9.figshare.5104873.v1

특허 번호

US08846684B2