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4-(3-Methanesulfonyloxymethyl-[1,2,4]triazol-1-yl)-piperidine-1-carboxylic acid tert-butyl ester → ethyl 1-(1-(5-ethylpyrimidin-2-yl)piperidin-4-yl)-3-(trifluoromethyl)-1H-pyrazole-4-carboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-(3-Methanesulfonyloxymethyl-[1,2,4]triazol-1-yl)-piperidine-1-carboxylic acid tert-butyl ester | HCID 57708378 | — |
| 反応物 | 1-(5-Ethylpyrimidin-2-yl)piperidin-4-yl methanesulfonate | HCID 57708402 | — |
| 反応物 | HCID 178469923 | HCID 178469923 | — |
| 生成物 | ethyl 1-(1-(5-ethylpyrimidin-2-yl)piperidin-4-yl)-3-(trifluoromethyl)-1H-pyrazole-4-carboxylate | HCID 57708415 | — |
| 生成物 | ethyl 1-(1-(5-ethylpyrimidin-2-yl)piperidin-4-yl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate | HCID 57708422 | — |
反応手順
The compound was synthesized using ethyl 3-(trifluoromethyl)-1H-pyrazole-4-carboxylate and 1-(5-ethylpyrimidin-2-yl)piperidin-4-yl methanesulfonate in a manner similar to that described in Intermediate 1, Step 1. The reaction afforded two regioisomers, ethyl 1-(1-(5-ethylpyrimidin-2-yl)piperidin-4-yl)-3-(trifluoromethyl)-1H-pyrazole-4-carboxylate and ethyl 1-(1-(5-ethylpyrimidin-2-yl)piperidin-4-yl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate which were separated by flash column chromatography on silica gel.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08183381B2 |
| 出典データセット | uspto-grants-2012_05 |
| ORD ID | ord-dac830a4e18d45fe8b89dc7e1828c1af |
| 出典メモ | uspto-grants-2012_05 |