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

HRID 1371517Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1371517
[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

Komponenten

6

Edukt 4

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

Produkt 1

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

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6344DichloromethaneLösungsmittel

Versuchsvorschrift

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.

Aufarbeitung

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

Quellen und Nachweise

ORD-Eintrag
ord-b3442d9115a648a3bce533b88e405f98
Quelldatensatz
uspto-grants-2007_01
Patentnummer
US07157463B2

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