反応 #1885023

ord-a8f0ea010b0f497ab6664d25ef542706

反応方程式

CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)O.COc1ccc2c3c1O[C@H]1C(=O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314
Boc-Leu Hydrocodone
Cl
HCl
→
CC(C)C[C@H](N)C(=O)O.COc1ccc2c3c1O[C@H]1C(=O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314
solid
収率 97.0%
CC(C)C[C@H](N)C(=O)O.COc1ccc2c3c1O[C@H]1C(=O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314
Leu Hydrocodone
収率 97.0%

反応物

CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)O.COc1ccc2c3c1O[C@H]1C(=O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314
Boc-Leu Hydrocodone
Cl
HCl

試薬

なし

溶媒

C1COCCO1
dioxane

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    その他Solvent was removed
  2. 2
    乾燥final product dried under vacuum

実験手順

To the Boc-Leu-Hydrocodone was added 25 ml of 4N HCl in dioxane. The resulting mixture was stirred at ambient temperatures for 18 hours. Solvent was removed and final product dried under vacuum. Solid was collected as a slightly yellow solid (1.96 g, 97% yield): 1H NMR (DMSO-d6) δ 0.94 (d, 6H), 1.52 (m, 1H), 1.75-1.90 (m, 4H), 2.22 (dt, 1H), 2.34 (dt, 1H), 2.64 (q, 1H), 2.75 (s, 3H), 2.95-3.23 (m, 4H), 3.74 (s, 3H), 3.91 (d, 1H), 4.07 (s, 1H), 5.10 (s, 1H), 5.72 (d, 1H), 6.76 (d, 1H), 6.86 (d, 1H), 8.73 br s, 3H).

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US08343927B2uspto-grants-2013_01