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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 29536Generated: October 25, 2026

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

https://huagongshe.com/reaction/29536

Reaction equation

Participants

RoleNameHCIDCharge
ReactantAzetidineHCID 10422—
ReactantBinap, (A+-)-HCID 634876—
Reactant4-Bromo-N-[4-chloro-2-(pyridine-4-carbonyl)-phenyl]-benzenesulfonamideHCID 10072530—
ReactantPotassium phosphate, tribasic, monohydrateHCID 22031701—
CatalystPalladiumHCID 23938—
SolventDimethylformamideHCID 6228—
Product4-Azetidin-1-yl-N-[4-chloro-2-(pyridine-4-carbonyl)-phenyl]-benzenesulfonamideHCID 59788572—

Reaction Steps

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.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07420055B2
Source datasetuspto-grants-2008_09
ORD IDord-2b520ac099e541fe8df3e3358a8dc94e
Source noteuspto-grants-2008_09