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Triethylamine → 1-(4'-Fluorobiphenyl-4-sulfonylamino)cyclopentanecarboxylic acid benzyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Benzyl 1-aminocyclopentanecarboxylate 4-methylbenzenesulfonate | HCID 254983 | — |
| 反応物 | 4'-Fluorobiphenyl-4-sulfonyl chloride | HCID 2794749 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 1-(4'-Fluorobiphenyl-4-sulfonylamino)cyclopentanecarboxylic acid benzyl ester | HCID 15480008 | — |
反応手順
To a solution of 1-aminocyclopentanecarboxylic acid benzyl ester p-toluenesulfonic acid salt (12.1 grams, 30.9 mmol) and triethylamine (10.0 mL, 72 mmol) in water (150 mL) and 1,4-dioxane (150 mL) was added 4'-fluorobiphenyl-4-sulfonyl chloride (8.8 grams, 32.5 mmol). The mixture was stirred at room temperature for 16 hours and then most of the solvent was removed by evaporation under vacuum. The mixture was diluted with ethyl acetate and was washed successively with dilute hydrochloric acid solution, water, and brine. The solution was dried over magnesium sulfate and concentrated to leave 1-(4'-fluorobiphenyl-4-sulfonylamino)cyclopentanecarboxylic acid benzyl ester as a solid, 12.33 grams (76%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06107337 |
| 出典データセット | uspto-grants-2000_08 |
| ORD ID | ord-8057c7a85fb74f4fa79730d812f72cd6 |
| 出典メモ | uspto-grants-2000_08 |