HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
2-Aminothiazole → 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-N-thiazol-2-yl-benzamide
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | 2-Aminothiazole | HCID 2155 | — |
| 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-N-thiazol-2-yl-benzamide | HCID 86640140 | 147,2% |
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 (80.0 mg, 0.118 mmol) obtained in Step A in Example 1-D-21 and 2-aminothiazole (23.6 mg, 0.236 mmol) instead of 1-pyridine-3-yl-piperazine, amidation was carried out in the same manner as Step B in Example 1-D-21, to obtain 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-N-thiazol-2-yl-benzamide as a yellow solid (132 mg), and then the PMB groups were removed according to the above Deprotection method 3, to obtain the desired compound (D-270) as a yellow powder (37.8 mg, 62%).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08022205B2 |
| Quelldatensatz | uspto-grants-2011_09 |
| ORD ID | ord-b3d0a3593cff455eb1abefb03237858d |
| Quellennotiz | uspto-grants-2011_09 |