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Dichloromethane → (7bR,11aS)-N-[2-Ethoxy-3-pyridinyl]-1,2,7b,8,9,10,11,11a-octahydro-4H-pyrido[4,3-b][1,4]thiazepino[6,5,4-hi]indole-6-amine, bis hydrochloride salt
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Dichloromethane | HCID 6344 | — |
| 反応物 | 3-Bromo-2-ethoxypyridine | HCID 10987308 | — |
| 反応物 | Sodium t-butoxide | HCID 23676156 | — |
| 反応物 | tert-butyl (7bR,11aS)-6-amino-1,2,7b,10,11,11a-hexahydro-4H-pyrido[4,3-b][1,4]thiazepino[6,5,4-hi]indole-9(8H) carboxylate | HCID 86586437 | — |
| 触媒 | Palladium | HCID 23938 | — |
| 触媒 | Bis(cyclopenta-1,4-dien-1-yl(diphenyl)phosphane);dichloropalladium;iron(2+) | HCID 178418228 | — |
| 生成物 | (7bR,11aS)-N-[2-Ethoxy-3-pyridinyl]-1,2,7b,8,9,10,11,11a-octahydro-4H-pyrido[4,3-b][1,4]thiazepino[6,5,4-hi]indole-6-amine, bis hydrochloride salt | HCID 131724731 | — |
反応手順
Following the procedures described in Example 175 and using 3-bromo-2-ethoxypyridine, sodium tert-butoxide as the base and [1,1′-bis(diphenylphosphino)ferrocene]dichloropalladium (II), complex with dichloromethane, as the palladium source, tert-butyl (7bR,11aS)-6-amino-1,2,7b,10,11,11a-hexahydro-4H-pyrido[4,3-b][1,4]thiazepino[6,5,4-hi]indole-9(8H)-carboxylate from Example 33, Part B was converted into the title compound of Example 186 as a solid. ESI MS m/z 383.2 [C21H26N4OS+H]+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06849619B2 |
| 出典データセット | uspto-grants-2005_02 |
| ORD ID | ord-6ab698a3457d407d84690cf4ec0f1a57 |
| 出典メモ | uspto-grants-2005_02 |