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5-(But-2-ynyloxy)pyrazine-2-carboxylic acid → 5-But-2-ynyloxy-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
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 5-(But-2-ynyloxy)pyrazine-2-carboxylic acid | HCID 58448677 | — |
| 反応物 | (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 | — |
| 生成物 | 5-But-2-ynyloxy-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 72706009 | — |
反応手順
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-but-2-ynyloxy-pyrazine-2-carboxylic acid (CAS 1221447-98-814) following procedure Q yielded the title compound as an amorphous colorless material (34% yield). MS: m/z=474.2 [M+H]+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09181232B2 |
| 出典データセット | uspto-grants-2015_11 |
| ORD ID | ord-977f30d217fb42f19353fb3224212237 |
| 出典メモ | uspto-grants-2015_11 |