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Hydrochloric Acid → 3-{1-(1,3-Benzodioxol-5-yl)-2-[(2-ethyl-4-methylphenyl)sulfonamido]-2-oxoethyl}-6-(hydroxymethyl)-1-methyl-1h-indole
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Hydrochloric Acid | HCID 313 | — |
| 反応物 | Ethanaminium, N,N,N-triethyl-, fluoride (1:1) | HCID 69582 | — |
| 反応物 | 3-{1-(1,3-Benzodioxol-5-yl)-2-[(2-ethyl-4-methylphenyl)sulfonamido]-2-oxoethyl}-6-(triisopropylsilyloxymethyl)-1-methyl-1h-indole | HCID 22467246 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 3-{1-(1,3-Benzodioxol-5-yl)-2-[(2-ethyl-4-methylphenyl)sulfonamido]-2-oxoethyl}-6-(hydroxymethyl)-1-methyl-1h-indole | HCID 22467245 | 84.5% |
反応手順
Tetraethylammonium fluoride (312 mg, 2.18 mmol) was added to a stirred solution of the compound of step (g) (380 mg, 0.55 mmol) in acetonitrile (6 ml) at room temperature under a nitrogen atmosphere. After 12 H the mixture was poured into 1M hydrochloric acid (50 ml) and extracted into ethyl acetate (2×50 ml). The organic fractions were combined, dried (MgSO4) and concentrated in vacuo to give a yellow foam. Flash column chromatography (eluting with 98% dichloromethane/2% methanol) gave the product as a white solid (242 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06306852B1 |
| 出典データセット | uspto-grants-2001_10 |
| ORD ID | ord-23cd5a78594f423b8c469eb4457657cd |
| 出典メモ | uspto-grants-2001_10 |