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HRID 38464作成日:2026年10月23日

Potassium Phosphate, Tribasic → methyl 4-(8-cyclopropyl-2-{[6-(1-methyl-1H-pyrazol-4-yl)-4-oxospiro[chroman-2,4'-piperidin]-1'-yl]carbonyl}quinolin-4-yl)benzoate

https://huagongshe.com/ja/reaction/38464

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium Phosphate, TribasicHCID 62657—
反応物4-Methoxycarbonylphenylboronic acidHCID 2734369—
反応物8-cyclopropyl-2-{[6-(1-methyl-1H-pyrazol-4-yl)-4-oxospiro[chroman-2,4'-piperidin]-1'-yl]carbonyl}quinolin-4-yl trifluoromethanesulfonateHCID 58208674—
触媒Tetrabutylammonium BromideHCID 74236—
触媒Bis(cyclopenta-1,4-dien-1-yl(diphenyl)phosphane);dichloropalladium;iron(2+)HCID 178418228—
溶媒AcetonitrileHCID 6342—
生成物methyl 4-(8-cyclopropyl-2-{[6-(1-methyl-1H-pyrazol-4-yl)-4-oxospiro[chroman-2,4'-piperidin]-1'-yl]carbonyl}quinolin-4-yl)benzoateHCID 58208703—

反応条件

温度90 °C

反応手順

K3PO4 (109 mg, 0.515 mmol) was added to a stirred mixture of TBAB (8.30 mg, 0.0260 mmol), PdCl2(dppf) (18.9 mg, 0.0260 mmol), 8-cyclopropyl-2-{[6-(1-methyl-1H-pyrazol-4-yl)-4-oxospiro[chroman-2,4′-piperidin]-1′-yl]carbonyl}quinolin-4-yl trifluoromethanesulfonate (165 mg, 0.258 mmol) and [4-(methoxycarbonyl)phenyl]boronic acid (55.6 mg, 0.309 mmol) in MeCN (2 ml) and the mixture was stirred at 90° C. overnight. The mixture was filtered, washing with CHCl3 and the solvent was evaporated under reduced pressure. The residue was purified by silicagel column chromatography (hexane/EtOAc) to give intended compound as a yellow solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08524730B2
出典データセットuspto-grants-2013_09
ORD IDord-db8cf70bebfe4a1e9f524a59f6376d5c
出典メモuspto-grants-2013_09