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HRID 29536作成日:2026年10月25日

Azetidine → 4-Azetidin-1-yl-N-[4-chloro-2-(pyridine-4-carbonyl)-phenyl]-benzenesulfonamide

https://huagongshe.com/reaction/29536

反応式

関与物質

役割名称HCID仕込み量
反応物AzetidineHCID 10422—
反応物Binap, (A+-)-HCID 634876—
反応物4-Bromo-N-[4-chloro-2-(pyridine-4-carbonyl)-phenyl]-benzenesulfonamideHCID 10072530—
反応物Potassium phosphate, tribasic, monohydrateHCID 22031701—
触媒PalladiumHCID 23938—
溶媒DimethylformamideHCID 6228—
生成物4-Azetidin-1-yl-N-[4-chloro-2-(pyridine-4-carbonyl)-phenyl]-benzenesulfonamideHCID 59788572—

反応手順

The title compound was prepared according to the general procedure for the synthesis of heterocyclyl and heteroaryl substituted phenylsulfonyl derivatives previously described, using 4-Bromo-N-[4-chloro-2-(pyridine-4-carbonyl)-phenyl]-benzenesulfonamide 0.3 g (0.66 mmol), potassium phosphate tribasic monohydrate 0.91 g (3.96 mmol), rac-2,2′-bis (diphenylphosphino)-1,1′-binaphthyl 0.12 g (0.198 mmol), azetidine 0.18 g (3.3 mmol) and Pd (dba)3 60 mg (0.066 mmol) in 3 ml DMF, followed by workup and HPLC purification.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07420055B2
出典データセットuspto-grants-2008_09
ORD IDord-2b520ac099e541fe8df3e3358a8dc94e
出典メモuspto-grants-2008_09