Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | Ethanesulfonyl chloride | HCID 11667 | — |
| Reactant | HCID 10248012 | HCID 10248012 | — |
| Solvent | Ethyl Acetate | HCID 8857 | — |
| Product | HCID 10072592 | HCID 10072592 | — |
Reaction Steps
A solution of the product from Example 63 (15 mg, 0.038 mmol), triethylamine (0.017 mL, 0.11 mmol) and ethanesulfonyl chloride (0.004 mL, 0.04 mmols) were combined in a sealed tube and heated to 65° C. overnight. The solvent was removed under a stream of N2 and replaced with DMF. After adding an additional 3 equivalents of ethanesulfonyl chloride and triethylamine, the reaction was heated to 65° C. for 8 hours and stirred at room temperature for 60 hours. The mixture was diluted with EtOAc and washed with 10% Na2CO3 and brine, dried over Na2SO4, filtered and concentrated in vac o. Purification by reversed-phase preparative HPLC gave the titled compound. ESI+ MS: 453 [M+H]+.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08008295B2 |
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| Source dataset | uspto-grants-2011_08 |
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| ORD ID | ord-9dddbb15f8e9441785da46e3de7943e5 |
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| Source note | uspto-grants-2011_08 |
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