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HRID 1888221作成日:2026年10月27日

Cesium carbonate → HCID 178477695、化合物

https://huagongshe.com/reaction/1888221

反応式

関与物質

役割名称HCID仕込み量
反応物Cesium carbonateHCID 10796—
反応物[3-(Hydroxymethyl)phenyl]boronic acidHCID 2734662—
反応物HCID 178477691HCID 178477691—
触媒HCID 178418397HCID 178418397—
溶媒1,4-Dioxane--water (1/1)HCID 21886435—
生成物HCID 178477695HCID 17847769568%

反応手順

Following the general procedure of Example 65, a mixture of 5-bromo-3-[1-(ethylsulfonyl)-4-piperidinyl]-1H-indazole-7-carboxamide (Intermediate 13) (180 mg, 0.4337 mmols), [3-(hydroxymethyl)phenyl]boronic acid (264 mg, 1.74 mmols), cesium carbonate (282 mg, 0.868 mmol), and Pd(PPh3)4 (22 mg, 0.021 mmol) in dioxane/water (2 mL/0.7 mL) was reacted. The reaction mixture was concentrated, redissolved in methylene chloride and filtered. The filtrate was concentrated and the residue was purified by using a Gilson semi-preparative HPLC system, eluting with 10% B to 80% B, where A=H2O (0.1% trifluoroacetic acid) and B=CH3CN (0.1% trifluoroacetic acid) pumped at 25 mL/min to give the title compound (130 mg, 68%)

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08501780B2
出典データセットuspto-grants-2013_08
ORD IDord-91bccad69ec0423a9848ed98b80ae5fa
出典メモuspto-grants-2013_08