反応 #73939

ord-778d7f5e63f94085bc1bae2701c3a430

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    洗浄washed with NaHCO3 (50 mL)
  2. 2
    抽出The aqueous layer was extracted with DCM (2×50 mL)
  3. 3
    洗浄the combined organic fractions washed with water (200 mL), brine (200 mL)
  4. 4
    乾燥dried over Na2SO4
  5. 5
    その他Removing the solvent

実験手順

To a solution of 3-(6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl)benzene-1-sulfonyl chloride (intermediate 1.6) (600 mg, 1.41 mmol) in chloroform (2.82 mL) was added DIEA (545.7 mg, 4.24 mmol) and 2-(2-(2-(2-azidoethoxy)ethoxy)ethoxy)ethanamine (616.3 mg, 2.82 mmol). The reaction was stirred overnight at which point the mixture was diluted with 50 mL DCM and washed with NaHCO3 (50 mL). The aqueous layer was extracted with DCM (2×50 mL) and the combined organic fractions washed with water (200 mL), brine (200 mL), and dried over Na2SO4. Removing the solvent gave the title compound as an oil which was used without further purification.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US08541448B2uspto-grants-2013_09