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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 520608생성일: 2026년 10월 24일

Sodium Bicarbonate → 2-(6-(1H-indol-4-yl)-1-(phenylsulfonyl)-1H-indazol-4-yl)-5-((4-isopropylpiperazin-1-yl)methyl)oxazole

https://huagongshe.com/ko/reaction/520608

반응식

참여 물질

역할이름HCID투입량
반응물Sodium BicarbonateHCID 516892—
반응물1H-Indole-4-boronic acid, pinacol esterHCID 11322471—
반응물2-[1-(Benzenesulfonyl)-6-chloroindazol-4-yl]-5-[(4-propan-2-ylpiperazin-1-yl)methyl]-1,3-oxazoleHCID 59564708—
용매WaterHCID 962—
용매IsopropanolHCID 3776—
생성물2-(6-(1H-indol-4-yl)-1-(phenylsulfonyl)-1H-indazol-4-yl)-5-((4-isopropylpiperazin-1-yl)methyl)oxazoleHCID 6669575596.1%

반응 단계

A solution of sodium bicarbonate (228.0 g) in water (2.7 L) was added to a suspension of 6-Chloro-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1-(phenylsulfonyl)-1H-indazole (271.2 g) and 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole (263.2 g, available from Apollo Scientific Limited) in isopropanol (2.7 L) stirred under nitrogen at ambient temperature. After degassing, via evacuation and flushing with nitrogen, 2′-(dimethylamino)-2-biphenylyl-palladium(II) chloride dinorbornylphosphine complex (29.83 g) was added. The mixture was degassed again and was then heated to 90±3° C. and held at this temperature for 2 hours. The mixture was cooled to 20±5° C. over 25 minutes and aged at this temperature overnight. The resultant suspension was filtered, washed with water (1.35 L) and then slurried with toluene (4×1.35 L). The solid was dried under vacuum at 50° C. to give the title compound as grey solid (302.7 g).

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US09326987B2
출처 데이터셋uspto-grants-2016_05
ORD IDord-9d34cb598a6f4d57ae4a7587a97c519a
출처 메모uspto-grants-2016_05