反応 #514364

ord-04c226e4c8a34e72ad24d61b137d785c

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    温度cooling until the solution
  2. 2
    温度with cooling for 1 h
  3. 3
    その他After this time the mother liquor was decanted off
  4. 4
    その他to remove residual solvent
  5. 5
    その他The resulting material was triturated with dry diethyl ether (×2)
  6. 6
    ろ過filtered off
  7. 7
    洗浄washed with more dry diethyl ether
  8. 8
    その他The yellow solid was recrystallised from ethanol/diethyl ether
  9. 9
    その他finally dried in a drying pistol

実験手順

1-Butoxycarbonylamino-4-(1-imino-2-fluoroethylamino) but-2-yne hydrobromide (500 mg) was deprotected by dissolving in glacial acetic acid (10 ml), cooling until the solution almost solidified and adding HBr in acetic acid (45% wv, 1.8 ml). The mixture was stirred with cooling for 1 h then at room temperature for 1 h. After this time the mother liquor was decanted off and the sticky residue subjected to an oil pump vacuum to remove residual solvent. The resulting material was triturated with dry diethyl ether (×2), filtered off and washed with more dry diethyl ether. The yellow solid was recrystallised from ethanol/diethyl ether and finally dried in a drying pistol to yield 1-amino-4-(1-imino-2-fluoroethylamino)but-2-yne dihydrobromide, Mpt 174°-176.5° C.(dec.), FAB M.S. M+1+144.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: USRE037438E1uspto-grants-2001_11