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Ethyl 4-(chlorosulfonyl)benzoate → 4-{3-Chloro-4-[2-(2-chloro-pyridin-4-yl)-3,3,3-trifluoro-2-hydroxy-1-methyl-propyl]-phenylsulfamoyl}-benzoic acid ethyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Ethyl 4-(chlorosulfonyl)benzoate | HCID 3667622 | — |
| 反応物 | 3-(4-Amino-2-chloro-phenyl)-2-(2-chloro-pyridin-4-yl)-1,1,1-trifluoro-butan-2-ol | HCID 86629109 | — |
| 溶媒 | Pyridine | HCID 1049 | — |
| 生成物 | 4-{3-Chloro-4-[2-(2-chloro-pyridin-4-yl)-3,3,3-trifluoro-2-hydroxy-1-methyl-propyl]-phenylsulfamoyl}-benzoic acid ethyl ester | HCID 86645951 | — |
反応手順
4-Chlorosulfonyl-benzoic acid ethyl ester (CAS Reg. No. 10486-51-8, 15 mg) was added to a solution of 3-(4-amino-2-chloro-phenyl)-2-(2-chloro-pyridin-4-yl)-1,1,1-trifluoro-butan-2-ol (Example 68 step 4, 20 mg) in pyridine (0.8 ml). The solution was stirred for 30 min at room temperature. The mixture was purified by prep. HPLC (C18-column, solvent gradient 20-98% CH3CN in 0.1% HCOOH[aq]) to give the title compound (18 mg) as a light yellow foam. MS (m/e)=577.1 [M+H+].
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08138189B2 |
| 出典データセット | uspto-grants-2012_03 |
| ORD ID | ord-e04d08561a9344fcbc94adbffc17fee3 |
| 出典メモ | uspto-grants-2012_03 |