反応 #1885024

ord-64dbd5b485ae49abbf21a14f04f8fc21

反応方程式

COc1ccc2c3c1O[C@H]1C(=O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314.C[C@H](NC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1C(=O)O
Boc-Ala-Pro Hydrocodone
Cl
HCl
→
COc1ccc2c3c1O[C@H]1C(=O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314.C[C@H](N)C(=O)N1CCC[C@H]1C(=O)O
solid
COc1ccc2c3c1O[C@H]1C(=O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314.C[C@H](N)C(=O)N1CCC[C@H]1C(=O)O
Ala-Pro Hydrocodone

反応物

COc1ccc2c3c1O[C@H]1C(=O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314.C[C@H](NC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1C(=O)O
Boc-Ala-Pro 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-Ala-Pro-Hydrocodone (0.100 g) was added 10 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 (0.56 g, 71% yield): 1H NMR (DMSO-d6) δ 1.38 (s, 3H), 1.48 (t, 1H), 1.80-2.29 (m, 8H), 2.65 (m, 1H), 2.80 (s, 3H), 2.96 (m, 3H), 3.23 (m, 2H), 3.76 (s, 3H), 3.92 (s, 1H), 4.22 (s, 1H), 4.53 (s, 1H), 5.00 (s, 1H), 5.84 (d, 1H), 6.77 (d, 1H), 6.86 (d, 1H), 8.25 (br s, 3H).

出典

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