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Methanesulfonyl chloride → tert-butyl N-[4-[[[(6S)-3-(methanesulfonamido)-4-oxo-7,8-dihydro-6H-pyrrolo[1,2-a]pyrimidine-6-carbonyl]amino]methyl]benzenecarboximidoyl]carbamate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Methanesulfonyl chloride | HCID 31297 | — |
| 反応物 | tert-butyl N-[4-[[[(6S)-3-amino-4-oxo-7,8-dihydro-6H-pyrrolo[1,2-a]pyrimidine-6-carbonyl]amino]methyl]benzenecarboximidoyl]carbamate | HCID 145857226 | — |
| 溶媒 | Pyridine | HCID 1049 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | tert-butyl N-[4-[[[(6S)-3-(methanesulfonamido)-4-oxo-7,8-dihydro-6H-pyrrolo[1,2-a]pyrimidine-6-carbonyl]amino]methyl]benzenecarboximidoyl]carbamate | HCID 145857232 | 22% |
反応手順
To a solution of 1j (50 mg, 0.117 mmol) in 0.5 mL pyridine at 0° C. was added methanesulfonyl chloride (14.8 mg, 0.129 mmol). The solution was stirred at rt for 16 h. The mixture was diluted with 50 mL EtOAc, washed with H2O (2×) and brine, dried (Na2SO4) and concentrated to afford 13 mg (22%) of intermediate 16a. MS (ESI) 505.0 (M+H+).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07094783B2 |
| 出典データセット | uspto-grants-2006_08 |
| ORD ID | ord-57e4e8218a3f420ba2104755af395843 |
| 出典メモ | uspto-grants-2006_08 |