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HRID 531621作成日:2026年10月24日

Diisopropylethylamine → (S)-1-(4-(4-(3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperidin-1-yl)propan-2-ol

https://huagongshe.com/ja/reaction/531621

反応式

関与物質

役割名称HCID仕込み量
反応物DiisopropylethylamineHCID 81531—
反応物(2S)-2-MethyloxiraneHCID 146262—
反応物3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-5-(4-(piperidin-4-yl)phenyl)-1-tosyl-1H-pyrrolo[2,3-b]pyridine hydrochlorideHCID 118524085—
溶媒EthanolHCID 702—
生成物(S)-1-(4-(4-(3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperidin-1-yl)propan-2-olHCID 9003058899.4%

反応条件

温度85 °C

反応手順

Seal tube containing 3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-5-(4-(piperidin-4-yl)phenyl)-1-tosyl-1H-pyrrolo[2,3-b]pyridine hydrochloride (product of step-iii of example 82) (125 mg, 0.194 mmol), (S)-2-methyloxirane (23 mg, 0.389 mmol), DIPEA (100 mg, 0.778 mmol) and ethanol were heated at 85° C. for 3 hours and distilled the solvent on rotavapor to get 128 mg (99% yield) of the titled compound. MS: m/z=664.4 (M+1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09353107B2
出典データセットuspto-grants-2016_05
ORD IDord-5b1e7f2d9137400cba991c412ca8d5a9
出典メモuspto-grants-2016_05