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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1024921Generated: October 30, 2026

Cesium carbonate → ethyl (2R)-2-({6-[({5-[(tert-butylamino)carbonyl]-2-furyl}sulfonyl)amino]-2-[(2,3-difluorobenzyl)thio]pyrimidin-4-yl}oxy)propanoate

https://huagongshe.com/reaction/1024921

Reaction equation

Participants

RoleNameHCIDCharge
ReactantCesium carbonateHCID 10796—
Reactant5-(aminosulfonyl)-N-(tert-butyl)-2-furamideHCID 47323401—
Reactant2-[[6-chloro-2-[[(2,3-difluorophenyl)methyl]thio]-4-pyrimidinyl]oxy](2R)-propanoic acid ethyl esterHCID 86619870—
CatalystBis(dibenzylideneacetone)palladiumHCID 9811564—
Solvent1,4-DioxaneHCID 31275—
Productethyl (2R)-2-({6-[({5-[(tert-butylamino)carbonyl]-2-furyl}sulfonyl)amino]-2-[(2,3-difluorobenzyl)thio]pyrimidin-4-yl}oxy)propanoateHCID 53628366—

Reaction Steps

The subtitle compound was prepared according to the procedure outlined in example 1 step (iv) using a mixture of 5-(aminosulfonyl)-N-(tert-butyl)-2-furamide (0.25 g), tris(dibenzylideneacetone)dipalladium (0) (58 mg), 2-dicyclohexylphosphino-2′,4′,6′-tri-isopropyl-1,1′-diphenyl (XPHOS) (30 mg), cesium carbonate (0.65 g) and 2-[[6-chloro-2-[[(2,3-difluorophenyl)methyl]thio]-4-pyrimidinyl]oxy]-(2R)-propanoic acid ethyl ester (product of Example 11 step i) (0.26 g) in dioxane (10 mL). Purification was trituration with Et2O to give the subtitle compound as a white solid. Yield: 0.25 g

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08722883B2
Source datasetuspto-grants-2014_05
ORD IDord-7fb8488b13d1485495029ec047123d28
Source noteuspto-grants-2014_05