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HRID 1888249作成日:2026年10月27日

Potassium Carbonate → 5-{3-[(methylsulfonyl)amino]phenyl}-3-(1-{[3-(1-pyrrolidinyl)propyl]sulfonyl}-4-piperidinyl)-1H-indazole-7-carboxamide

https://huagongshe.com/reaction/1888249

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium CarbonateHCID 11430—
反応物3-Methylsulfonylaminophenylboronic acidHCID 2773535—
反応物5-bromo-3-(1-{[3-(1-pyrrolidinyl)propyl]sulfonyl}-4-piperidinyl)-1H-indazole-7-carboxamideHCID 178513509—
触媒HCID 178418397HCID 178418397—
溶媒1,4-Dioxane--water (1/1)HCID 21886435—
生成物5-{3-[(methylsulfonyl)amino]phenyl}-3-(1-{[3-(1-pyrrolidinyl)propyl]sulfonyl}-4-piperidinyl)-1H-indazole-7-carboxamideHCID 17850501218%

反応手順

Following the general procedure of Example 66, a mixture of 5-bromo-3-(1-{[3-(1-pyrrolidinyl)propyl]sulfonyl}-4-piperidinyl)-1H-indazole-7-carboxamide (Intermediate 27) (24 mg, 0.048 mmols), {3-[(methylsulfonyl)amino]phenyl}boronic acid (31 mg, 0.144 mmols), potassium carbonate (40 mg), and Pd(PPh3)4 (3 mg) in dioxane/water (3/1, 4 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 (5 mg, 18%)

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-63b123b10ca94cb29e9a36ae0c90af9c
出典メモuspto-grants-2013_08