HuagongsheHuagongshe Chemistry Print Report · For research reference only
5-(Fluoromethyl)pyrazine-2-carboxylic acid → 5-Fluoromethyl-pyrazine-2-carboxylic acid [3-((4S,4aR,7aR)-2-amino-5,5-difluoro-4-methyl-4,4a,5,6,7,7a-hexahydro-cyclopenta[e][1,3]oxazin-4-yl)-4-fluoro-phenyl]-amide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 5-(Fluoromethyl)pyrazine-2-carboxylic acid | HCID 66869584 | — |
| Reactant | (4S,4aR,7aR)-4-(5-amino-2-fluoro-phenyl)-5,5-difluoro-4-methyl-4,4a,5,6,7,7a-hexahydro-cyclopenta[e][1,3]oxazin-2-ylamine | HCID 90021263 | — |
| Product | 5-Fluoromethyl-pyrazine-2-carboxylic acid [3-((4S,4aR,7aR)-2-amino-5,5-difluoro-4-methyl-4,4a,5,6,7,7a-hexahydro-cyclopenta[e][1,3]oxazin-4-yl)-4-fluoro-phenyl]-amide | HCID 72943699 | 75% |
Reaction Steps
The coupling of (4S,4aR,7aR)-4-(5-amino-2-fluoro-phenyl)-5,5-difluoro-4-methyl-4,4a,5,6,7,7a-hexahydro-cyclopenta[e][1,3]oxazin-2-ylamine (intermediate XIIIa-1) and 5-fluoromethyl-pyrazine-2-carboxylic acid (CAS 1262803-66-6) following procedure Q yielded the title compound as a white solid (75% yield). MS: m/z=438.2 [M+H]+.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09181232B2 |
| Source dataset | uspto-grants-2015_11 |
| ORD ID | ord-53df7868b10d466ba2213af93ff418b0 |
| Source note | uspto-grants-2015_11 |