HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
1-Ethylpiperazine → {4-[4-{2-[Bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl]-3-fluoro-phenyl}-(4-ethyl-piperazin-1-yl)-methanone
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | 1-Ethylpiperazine | HCID 79196 | — |
| Edukt | 4-(4-{2-[Bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl)-3-fluoro-benzoic acid | HCID 59244395 | — |
| Produkt | {4-[4-{2-[Bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl]-3-fluoro-phenyl}-(4-ethyl-piperazin-1-yl)-methanone | HCID 67386285 | — |
Reaktionsschritte
Using 4-(4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl)-3-fluoro-benzoic acid (65.6 mg, 0.0968 mmol) obtained in Step A in Example 1-D-21 and N-ethylpiperazine (24.6 μl, 0.194 mmol) instead of 1-pyridin-3-yl-piperazine, amidation was carried out in the same manner as Step B in Example 1-D-21, and a crude product of {4-[4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl]-3-fluoro-phenyl}-(4-ethyl-piperazin-1-yl)-methanone was obtained as a yellow solid (64.2 mg). Then the PMB groups were removed according to the above Deprotection method 3, to obtain the desired compound (D-138) as a yellow powder (39.2 mg, 76%).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08022205B2 |
| Quelldatensatz | uspto-grants-2011_09 |
| ORD ID | ord-9367fd566c914752a698b57c56ddca96 |
| Quellennotiz | uspto-grants-2011_09 |