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HRID 237977作成日:2026年10月26日

Sodium Carbonate → 3-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-N-(4,5-dihydrothiazol-2-yl)benzamide

https://huagongshe.com/reaction/237977

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium CarbonateHCID 10340—
反応物3-iodo-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amineHCID 24905337—
反応物(3-((4,5-Dihydrothiazol-2-yl)carbamoyl)phenyl)boronic acidHCID 44119636—
触媒HCID 178418397HCID 178418397—
溶媒EthanolHCID 702—
溶媒1,2-DimethoxyethaneHCID 8071—
生成物3-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-N-(4,5-dihydrothiazol-2-yl)benzamideHCID 2490515467%

反応条件

温度80 °C

反応手順

A solution of [3-((4,5-dihydrothiazol-2-yl)carbamoyl)phenyl]boronic acid (19 mg, 0.08 mmol) in EtOH (3.3 ml) was added to a solution of 3-iodo-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine (20 mg, 0.07 mmol) in DME (12 ml). Pd(PPh3)4 (16 mg, 0.014 mmol) and saturated Na2CO3 (1.9 ml) were added and the reaction was heated to 80° C. under an argon atmosphere overnight. After cooling, the reaction was extracted with saturated NaCl and CH2Cl2. Organic phases were combined, concentrated in vacuo and purified by RP-HPLC (MeCN:H2O:0.1% TFA) to yield BA30 (17.8 mg, 67% yield).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08642604B2
出典データセットuspto-grants-2014_02
ORD IDord-18586207bec2439f9379b006e80ffb62
出典メモuspto-grants-2014_02