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Trifluoroacetic acid → 1-butyl-3-(3-cyclobutyl-1H-pyrazolo[4,3-c]pyridin-6-yl)urea
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Trifluoroacetic acid | HCID 6422 | — |
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | Butylurea | HCID 11595 | — |
| 反応物 | 1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine) | HCID 636044 | — |
| 反応物 | 6-chloro-3-cyclobutyl-1-trityl-1H-pyrazolo[4,3-c]pyridine | HCID 89525898 | — |
| 触媒 | palladium(II) acetate | HCID 167845 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 1-butyl-3-(3-cyclobutyl-1H-pyrazolo[4,3-c]pyridin-6-yl)urea | HCID 178449546 | — |
反応手順
In a manner similar to that described in Scheme 6 and Example 30, 6-chloro-3-cyclobutyl-1-trityl-1H-pyrazolo[4,3-c]pyridine was reacted with 1-butylurea, (Xantphos, Pd(OAc)2, Cs2CO3, dioxane, 80° C., overnight) and then deprotected with TFA to provide 1-butyl-3-(3-cyclobutyl-1H-pyrazolo[4,3-c]pyridin-6-yl)urea. MS ESI calc'd. for C15H21N5O[M+1]+ 288, found 288.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09023865B2 |
| 出典データセット | uspto-grants-2015_05 |
| ORD ID | ord-3e37506a019f4bb5993cea20e35b7220 |
| 出典メモ | uspto-grants-2015_05 |