HuagongsheHuagongshe Chemistry Print Report · For research reference only
1-Ethylpiperazine → HCID 67384989, compound
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 1-Ethylpiperazine | HCID 79196 | — |
| Reactant | 4-(4-{2-[Bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-yl)-benzoic acid | HCID 59244887 | — |
| Product | HCID 67384989 | HCID 67384989 | 67.2% |
Reaction Steps
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)-benzoic acid (48.0 mg, 0.0728 mmol) obtained in Step A in Example 1-D-19 and N-ethylpiperazine (37.0 μl, 0.291 mmol) instead of 3-(aminomethyl)pyridine, in the same manner as Step B in Example 1-D-19, amidation was carried out, 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]-phenyl}-(4-ethyl-piperazin-1-yl)-methanone as a brown solid (37 mg), and then the PMB groups were removed according to the above Deprotection method 2, to obtain the desired compound (D-83) as a yellow powder (25.0 mg, 67%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08022205B2 |
| Source dataset | uspto-grants-2011_09 |
| ORD ID | ord-c699d3c55adf4a258924210fc2f0458e |
| Source note | uspto-grants-2011_09 |