Indole → 1H-Indole, 7-(1-piperazinyl)-

HRID 1371517ノート

反応式

HRID 1371517 の反応式
[NH:1]1[C:9]2[C:4](=[CH:5][CH:6]=[CH:7][CH:8]=2)[CH:3]=[CH:2]1.BrC1C=CC=C2C=1NC=C2.C([N:27]1[CH2:32][CH2:31][NH:30][CH2:29][CH2:28]1)(OC(C)(C)C)=O.C(O)(C(F)(F)F)=O>C(Cl)Cl>[N:27]1([C:8]2[CH:7]=[CH:6][CH:5]=[C:4]3[C:9]=2[NH:1][CH:2]=[CH:3]3)[CH2:32][CH2:31][NH:30][CH2:29][CH2:28]1

参加物

6

反応物 4

HCID 798IndoleHCID 6422Trifluoroacetic acidHCID 143452tert-Butyl piperazine-1-carboxylateHCID 27570207-Bromoindole

生成物 1

HCID 30695021H-Indole, 7-(1-piperazinyl)-収率 54%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

The Boc protected indole (200 mg, 1.5 mmol) prepared from 7-bromoindole and N-Boc piperazine as described in Step 1 of Preparation 54A is dissolved in DCM (1 mL). TFA (1 mL) is added and the mixture is stirred at r.t. for about an hour. The mixture is then concentrated to oil, which is taken up in methanol and freebased via SCX purification to afford about 164 mg (54%) of the final compound.

後処理

  1. concentrationThe mixture is then concentrated to oil, which
  2. customis taken up in methanol and freebased via SCX purification

出典と根拠

ORDレコード
ord-b3442d9115a648a3bce533b88e405f98
出典データセット
uspto-grants-2007_01
特許番号
US07157463B2

反応ノート

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