Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Water | HCID 962 | — |
| Reactant | Acetyl chloride | HCID 6367 | — |
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | HCID 53949705 | HCID 53949705 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Product | HCID 54282592 | HCID 54282592 | — |
Reaction Steps
52 mg of ethyl 2-[(R)-2-[[(S)-2-[2-(6-amidino-1-ethylindol-2-yl)ethyl]pyrrolidinyl]carbonyl]pyrrolidinyl]acetate obtained in Example 60 was dissolved in dry dichloromethane. To the resulting solution was added 31 μl of triethylamine, and the mixture was cooled to −78° C. After 16 μl of acetyl chloride was added, the reaction solution was stirred for 3 hours and warmed to room temperature. Water was added and the mixture was extracted with dichloromethane. The extract was dried over MgSO4 and evaporated under reduced pressure to remove the solvent. The residue was purified with silica gel column chromatography [eluent: ethyl acetate/methanol(50:1)] to obtain 7 mg of the title compound as a pale yellow solid.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US06201006B1 |
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| Source dataset | uspto-grants-2001_03 |
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| ORD ID | ord-baf95a1ba62f4868b0e54e3483385d9c |
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| Source note | uspto-grants-2001_03 |
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