Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Methylamine | HCID 6329 | — |
| Reactant | 4-(2-Fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxyquinoline-6-carboxylic acid hydrochloride | HCID 86650698 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Product | TAS-115 | HCID 44247727 | 96% |
Reaction Steps
Similar to the synthesis of Example 1, compound 1e (20 mg), 40% aqueous solution of methylamine (5 μL), and DMTMM•n-hydrate (22 mg) were dissolved in tetrahydrofuran (1 mL), followed by stirring at 30° C. for 1 hour, to thereby yield the titled compound 6 (18.4 mg, yield: 96%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patent number | US08304427B2 |
|---|
| Source dataset | uspto-grants-2012_11 |
|---|
| ORD ID | ord-809a1e33691c49f887541474d6bdfa5e |
|---|
| Source note | uspto-grants-2012_11 |
|---|
