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HRID 1265925作成日:2026年10月26日
Ethylthiourea → 8-Chloro-7-dimethylamino-4-[3-(2-ethylamino-thiazol-4-yl)-phenyl]-1,3-dihydro-benzo[b][1,4]diazepin-2-one
https://huagongshe.com/reaction/1265925
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Ethylthiourea | HCID 3032338 | — |
| 反応物 | 4-(3-Bromoacetyl-phenyl)-8-chloro-7-dimethylamino-1,3-dihydro-benzo[b][1,4]diazepin-2-one | HCID 18613234 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | 8-Chloro-7-dimethylamino-4-[3-(2-ethylamino-thiazol-4-yl)-phenyl]-1,3-dihydro-benzo[b][1,4]diazepin-2-one | HCID 18613266 | 18.3% |
反応手順
A mixture of 4-(3-bromoacetyl-phenyl)-8-chloro-7-dimethylamino-1,3-dihydro-benzo[b][1,4]diazepin-2-one (130 mg) (Example 193a) and N-ethyl-thiourea (31 mg) in THF (3 mL) was heated at 60° C. for 15 min. The mixture was diluted with AcOEt and washed with sat. NaHCO3 solution and with brine. The organic layer was dried and evaporated and the residue was purified by chromatography on silica gel using AcOEt/hexane (1:1) as eluent. The purified product was triturated with Et2O to give the title compound (24 mg) as yellow solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US06544985B2 |
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| 出典データセット | uspto-grants-2003_04 |
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| ORD ID | ord-89dc9320dc1e44cf92bb308e978ae586 |
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| 出典メモ | uspto-grants-2003_04 |
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