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HRID 85627作成日:2026年10月24日
Divinyl sulfone → methyl 4-((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)-3a-((3-(1,1-dioxido-4-thiomorpholinyl)propyl)amino)-1-isopropenyl-5a,5b,8,8,11a-pentamethyl-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1H-cyclopenta[a]chrysen-9-yl)benzoic acid
https://huagongshe.com/ja/reaction/85627
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
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| 反応物 | Divinyl sulfone | HCID 6496 | — |
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | methyl 4-((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)-3a-(3-aminopropylamino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1H-cyclopenta[a]chrysen-9-yl)benzoate | HCID 86676591 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 生成物 | methyl 4-((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)-3a-((3-(1,1-dioxido-4-thiomorpholinyl)propyl)amino)-1-isopropenyl-5a,5b,8,8,11a-pentamethyl-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1H-cyclopenta[a]chrysen-9-yl)benzoic acid | HCID 86676592 | 83.4% |
反応手順
Vinylsulfonylethene (5.90 mg, 0.050 mmol) and triethylamine (6.96 μl, 0.050 mmol) were added to a mixture of methyl 4-((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)-3a-(3-aminopropylamino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1H-cyclopenta[a]chrysen-9-yl)benzoate (15 mg, 0.025 mmol) in EtOH (1 mL). The reaction mixture was heated to 100° C. for 3 hours. The reaction mixture was concentrated under reduced pressure to provide the desired product as a brown solid (15 mg, 76%). LCMS: m/e 719.46 (M+H)+, 3.68 min (method 10).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08846647B2 |
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| 出典データセット | uspto-grants-2014_09 |
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| ORD ID | ord-9651d5b1da8f433cb811e2faa8c72009 |
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| 出典メモ | uspto-grants-2014_09 |
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