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Isopropylamine → 10-bromo-N3-isopropyl-6,7-dihydro-5H-5,7-methanobenzo[c]imidazo[1,2-a]azepine-2,3-dicarboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Isopropylamine | HCID 6363 | — |
| 反応物 | 10-bromo-2-carbamoyl-6,7-dihydro-5H-5,7-methanobenzo[c]imidazo[1,2-a]azepine-3-carboxylic acid | HCID 86693348 | — |
| 生成物 | 10-bromo-N3-isopropyl-6,7-dihydro-5H-5,7-methanobenzo[c]imidazo[1,2-a]azepine-2,3-dicarboxamide | HCID 86693420 | 99% |
反応手順
10-bromo-2-carbamoyl-6,7-dihydro-5H-5,7-methanobenzo[c]imidazo[1,2-a]azepine-3-carboxylic acid was reacted with isopropylamine similarly to as described in example 2 with non-critical modifications to afford 166 mg (99%) 10-bromo-N3-isopropyl-6,7-dihydro-5H-5,7-methanobenzo[c]imidazo[1,2-a]azepine-2,3-dicarboxamide. 10-bromo-N3-isopropyl-6,7-dihydro-5H-5,7-methanobenzo[c]imidazo[1,2-a]azepine-2,3-dicarboxamide was reacted with (3R)-3-ethynyl-3-hydroxy-1-methyl-pyrrolidin-2-one similarly to as described in General Procedure F with non-critical modifications to afford 43 mg (23%) of 10-[2-[(3R)-3-hydroxy-1-methyl-2-oxo-pyrrolidin-3-yl]ethynyl]-N3-isopropyl-5,6,7,12-tetrahydro-5,7-methanobenzo [c]imidazo[1,2-a]azepine-2,3-dicarboxamide.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09034866B2 |
| 出典データセット | uspto-grants-2015_05 |
| ORD ID | ord-d00e9aa207ac4a19acab1dc5b24f3fb1 |
| 出典メモ | uspto-grants-2015_05 |