反応 #155365

ord-9fdfc86de58e484c8c12a36262e7baec

反応方程式

CC(C)CC(NC(=O)CNC(=O)C(Cc1ccc(O)cc1)NC(=O)C(CO)NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)C(Cc1cnc[nH]1)NC(=O)C1CCC(=O)N1)C(=O)NC(CCCN=C(N)N)C(=O)N1CCCC1C(=O)NCC(N)=O
LHRH
OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO
PEG12
→
CC(C)CC(NC(=O)CNC(=O)C(Cc1ccc(O)cc1)NC(=O)C(CO)NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)C(Cc1cnc[nH]1)NC(=O)C1CCC(=O)N1)C(=O)NC(CCCN=C(N)N)C(=O)N1CCCC1C(=O)NCC(N)=O.OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO
LHRH PEG12
収率 60.0%

反応物

CC(C)CC(NC(=O)CNC(=O)C(Cc1ccc(O)cc1)NC(=O)C(CO)NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)C(Cc1cnc[nH]1)NC(=O)C1CCC(=O)N1)C(=O)NC(CCCN=C(N)N)C(=O)N1CCCC1C(=O)NCC(N)=O
LHRH
—
solution
OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO
PEG12

試薬

なし

溶媒

CC#N.O
acetonitrile water

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    その他The product was purified by RP-HPLC

実験手順

LHRH (10 mg) was dissolved in a mixture of acetonitrile:water (1:1, 500 μL) and to it was added PEG12-SATA stock solution (9.2 μL, 0.0025 mmol, 1.9 mg). The resulting mixture was stirred for 3 h at ambient temperature. The product was purified by RP-HPLC followed by lyophilization (60% yield).

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US08821850B2uspto-grants-2014_09