HuagongsheHuagongshe Chemistry Print Report · For research reference only
Isopropanol → (R)-4-(7-oxo-6,7-dihydrothiazolo[4,5-d]pyridazin-2-yl)-1-(4-trifluoromethoxy-benzenesulfonyl)-piperazine-2-carboxylic acid 4-trifluoromethoxy-benzylamide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Isopropanol | HCID 3776 | — |
| Reactant | 2-chloro-6H-thiazolo[4,5-d]pyridazin-7-one | HCID 59703713 | — |
| Reactant | (R)-1-(4-trifluoromethoxy-benzenesulfonyl)-piperazine-2-carboxylic acid 4-trifluoromethoxy-benzylamide | HCID 59703800 | — |
| Solvent | Triethylamine | HCID 8471 | — |
| Product | (R)-4-(7-oxo-6,7-dihydrothiazolo[4,5-d]pyridazin-2-yl)-1-(4-trifluoromethoxy-benzenesulfonyl)-piperazine-2-carboxylic acid 4-trifluoromethoxy-benzylamide | HCID 59703755 | 92.7% |
Reaction Steps
To a mixed solution of the compound (26 mg) obtained in Example 783, the compound (10 mg) obtained in Step 6 and isopropanol (1.0 ml) was added triethylamine (14 μl) at room temperature, and the mixture was heated under reflux overnight. The reaction mixture was concentrated under reduced pressure, and the residue was purified by thin layer silica gel chromatography (methanol:chloroform=1:20, developed twice) to give the title compound (31 mg).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08017612B2 |
| Source dataset | uspto-grants-2011_09 |
| ORD ID | ord-59236c2e876944b590d91a9b414dcfc8 |
| Source note | uspto-grants-2011_09 |