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Diisopropylethylamine → (R)-1-(4-(4-(3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperazin-1-yl)propan-2-ol
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | (R)-1,2-Epoxypropane | HCID 146261 | — |
| 反応物 | 3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-5-(4-(piperazin-1-yl)phenyl)-1-tosyl-1H-pyrrolo[2,3-b]pyridinehydrochloride | HCID 90031507 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 生成物 | (R)-1-(4-(4-(3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperazin-1-yl)propan-2-ol | HCID 90030866 | 97.5% |
反応手順
Using similar reaction conditions as described in step-i of example-82A, 3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-5-(4-(piperazin-1-yl)phenyl)-1-tosyl-1H-pyrrolo[2,3-b]pyridine hydrochloride (step 1 example 103) (150 mg. 0.606 mmol) was alkylated using (R)-2-methyloxirane (22 mg, 0.371 mmol), DIPEA (96 mg, 0.74 mmol) and ethanol (3 mL) to get 160 mg (97.5% yield) of the titled compound. MS: m/z=665.3 (M+1).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09353107B2 |
| 出典データセット | uspto-grants-2016_05 |
| ORD ID | ord-262c47d2e67d43bcae9ece83e0700f53 |
| 出典メモ | uspto-grants-2016_05 |