反応 #2006470

ord-a1a89b9a8c674d9a8cfb73c4b8a74568

反応方程式

CCN(C(C)C)C(C)C
Hunig's Base
O=C([O-])C(=O)c1c[nH]c2ncccc12.[K+]
Potassium 7-azaindole 3-glyoxylate
O=C([O-])C(=O)c1c[nH]c2ncccc12.[K+]
Potassium (7-azaindol-3-yl)-oxoacetate
C[C@@H]1CN(C(=O)c2ccccc2)CCN1
(R)-3-methyl-N-benzoylpiperazine
CCOP(=O)(OCC)On1nnc2ccccc2c1=O
3-(diethoxyphosphoryloxy)-1,2,3-benzotriazin-4(3H)-one
→
C[C@@H]1CN(C(=O)c2ccccc2)CCN1C(=O)C(=O)c1c[nH]c2ncccc12
(R)—N-(benzoyl)-3-methyl-N′-[(7-azaindol-3-yl)-oxoacetyl]-piperazine

反応物

CCN(C(C)C)C(C)C
Hunig's Base
O=C([O-])C(=O)c1c[nH]c2ncccc12.[K+]
Potassium 7-azaindole 3-glyoxylate
O=C([O-])C(=O)c1c[nH]c2ncccc12.[K+]
Potassium (7-azaindol-3-yl)-oxoacetate
C[C@@H]1CN(C(=O)c2ccccc2)CCN1
(R)-3-methyl-N-benzoylpiperazine
CCOP(=O)(OCC)On1nnc2ccccc2c1=O
3-(diethoxyphosphoryloxy)-1,2,3-benzotriazin-4(3H)-one

試薬

なし

溶媒

CN(C)C=O
DMF

反応条件

詳細条件
See reaction.notes.procedure_details.

実験手順

Potassium 7-azaindole 3-glyoxylate 3a (25.4 g, 0.111 mol), (R)-3-methyl-N-benzoylpiperazine 4a (22.7 g, 0.111 mol), 3-(diethoxyphosphoryloxy)-1,2,3-benzotriazin-4(3H)-one (DEPBT) (33.3 g, 0.111 mol) and Hunig's Base (28.6 g, 0.222 mol) were combined in 500 ml of DMF. The mixture was stirred at room temperature for 8 hours.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US08168615B2uspto-grants-2012_05