1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → tert-butyl 4-(1H-indole-6-carbonyl)piperazine-1-carboxylate

HRID 20977

反応式

HRID 20977 の反応式
[NH:1]1[C:9]2[C:4](=[CH:5][CH:6]=[C:7]([C:10]([OH:12])=O)[CH:8]=2)[CH:3]=[CH:2]1.CCN=C=NCCCN(C)C.C1C=C2N=NN(O)C2=CC=1.O.[C:35]([O:39][C:40]([N:42]1[CH2:47][CH2:46][NH:45][CH2:44][CH2:43]1)=[O:41])([CH3:38])([CH3:37])[CH3:36]>CN(C=O)C>[C:35]([O:39][C:40]([N:42]1[CH2:47][CH2:46][N:45]([C:10]([C:7]2[CH:8]=[C:9]3[C:4]([CH:3]=[CH:2][NH:1]3)=[CH:5][CH:6]=2)=[O:12])[CH2:44][CH2:43]1)=[O:41])([CH3:38])([CH3:36])[CH3:37]

参加物

6

反応物 4

HCID 159081-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 143452tert-Butyl piperazine-1-carboxylateHCID 5952301H-indole-6-carboxylic acidHCID 27960291-Hydroxybenzotriazole hydrate

生成物 1

HCID 17591552tert-butyl 4-(1H-indole-6-carbonyl)piperazine-1-carboxylate収率 129.5%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

In a similar manner to Step 1 of Reference Example 2, indole-6-carboxylic acid (200 mg, 1.24 mmol) was dissolved in DMF (2 mL), and the solution was treated with EDCI (475 mg, 2.48 mmol), HOBT monohydrate (168 mg, 1.24 mmol) and 1-(tert-butoxycarbonyl)piperazine (461 mg, 2.48 mmol) to obtain 6-[4-(tert-butoxycarbonyl)piperazin-1-ylcarbonyl]indole (529 mg).

出典と根拠

ORDレコード
ord-748ecd693fb347e59cfe97c9f4049039
出典データセット
uspto-grants-2010_06
特許番号
US07745641B2

関連ノート

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