HuagongsheHuagongshe Chemistry Print Report · For research reference only
4-Aminotetrahydropyran → 2-{(E)-2-[3-(5-Fluoro-pyridin-2-yl)-5-methyl-isoxazol-4-yl]-vinyl}-4-methyl-thiazole-5-carboxylic acid (tetrahydro-pyran-4-yl)-amide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 4-Aminotetrahydropyran | HCID 419223 | — |
| Reactant | 2-{(E)-2-[3-(5-Fluoro-pyridin-2-yl)-5-methyl-isoxazol-4-yl]-vinyl}-4-methyl-thiazole-5-carboxylic acid | HCID 66643630 | — |
| Solvent | Methanol--water (1/1) | HCID 22242641 | — |
| Product | 2-{(E)-2-[3-(5-Fluoro-pyridin-2-yl)-5-methyl-isoxazol-4-yl]-vinyl}-4-methyl-thiazole-5-carboxylic acid (tetrahydro-pyran-4-yl)-amide | HCID 59568529 | 70% |
Reaction Steps
As described for example 71d, 2-{(E)-2-[3-(5-fluoro-pyridin-2-yl)-5-methyl-isoxazol-4-yl]-vinyl}-4-methyl-thiazole-5-carboxylic acid (69 mg, 0.2 mmol) was converted, using 4-aminotetrahydropyran instead of isopropylamine, to the title compound (60 mg, 70%) which was obtained as a white solid after trituration from methanol/water. MS: m/e=429.2 [M+H]+.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08178522B2 |
| Source dataset | uspto-grants-2012_05 |
| ORD ID | ord-9a827859aae24093918be0d3cbf57914 |
| Source note | uspto-grants-2012_05 |