Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|
| Edukt | Diisopropylethylamine | HCID 81531 | — |
| Edukt | PyBOP | HCID 2724699 | — |
| Edukt | (4-Methylpiperazin-1-yl)acetic acid | HCID 2762732 | — |
| Edukt | tert-butyl 5-(2-(3-aminophenyl)quinazolin-4-ylamino)-1H-indazole-1-carboxylate | HCID 66825994 | — |
| Lösungsmittel | Dichloromethane | HCID 6344 | — |
| Produkt | HCID 59361937 | HCID 59361937 | — |
Reaktionsschritte
A suspension of 2-(4-methylpiperazin-1-yl)acetic acid (34 mg, 0.22 mmol), PyBOP® (11 mg, 0.22 mmol), DIEA (300 μL, 1.72 mmol) in CH2Cl2 (0.5 mL) was stirred at RT for 10-15 minutes. This solution of activated acid was added to a suspension of tert-butyl 5-(2-(3-aminophenyl)quinazolin-4-ylamino)-1H-indazole-1-carboxylate (100 mg, 0.22 mmol) and CH2Cl2 (1 mL). The reaction mixture was stirred at RT for 1.5 h. Activated another 1 equivalent of the acid as described above and it was once again added to the reaction mixture. Stirred for 16 h, diluted with more CH2Cl2 and extracted with H2O (3×). Organic layer was dried under Na2SO4 and concentrated in vacuo to give the desired product tert-butyl 5-(2-(3-(2-(4-methylpiperazin-1-yl)acetamido)phenyl)quinazolin-4-ylamino)-1H-indazole-1-carboxylate.
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patentnummer | US09440961B2 |
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| Quelldatensatz | uspto-grants-2016_09 |
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| ORD ID | ord-099752b8629947b6b90a7cd5ee89b2f0 |
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| Quellennotiz | uspto-grants-2016_09 |
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