Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | 1-Methylpiperazine | HCID 53167 | — |
| Reactant | Triphosgene | HCID 94429 | — |
| Reactant | HCID 18399114 | HCID 18399114 | — |
| Solvent | Chloroform | HCID 6212 | — |
| Product | HCID 18399312 | HCID 18399312 | 60.4% |
Reaction Steps
A solution of the compound obtained in Example 5 (100 mg) and triethylamine (50 mg) in chloroform (10 ml) is cooled to −10° C., and thereto is added dropwise a solution of triphosgene (49 mg) in chloroform. The mixture is warmed to room temperature, and the mixture is stirred for 30 minutes. To the mixture is added a solution of N-methylpiperazine (50 mg) and triethylamine (17 mg) in chloroform, and the mixture is further stirred for two hours. After the reaction is complete, the reaction mixture is washed, dried, and concentrated under reduced pressure. The residue is crystallized from diethyl ether to give 2[4-(tert-butoxycarbonylamino)phenyl]-6-methoxy-3-methoxycarbonyl-7-(4-methylpiperazinylcarbonyloxy)-4-(3,4,5-trimethoxyphenyl)-1(2H)-isoquinolinone (73 mg) as listed in Table 20.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US06486155B1 |
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| Source dataset | uspto-grants-2002_11 |
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| ORD ID | ord-8a5a6df550f24f12a0c97fbab162f9f6 |
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| Source note | uspto-grants-2002_11 |
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