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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1357160Generated: October 25, 2026

Acetic Acid → (2Rs,5rs)-4-[5-(4-fluoro-phenyl)-1-(toluene-4-sulfonyl)-pyrrolidin-2-yl]-n-butyramidine

https://huagongshe.com/reaction/1357160

Reaction equation

Participants

RoleNameHCIDCharge
ReactantAcetic AcidHCID 176—
ReactantHCID 178427370HCID 178427370—
SolventEthanolHCID 702—
Product(2Rs,5rs)-4-[5-(4-fluoro-phenyl)-1-(toluene-4-sulfonyl)-pyrrolidin-2-yl]-n-butyramidineHCID 2225042476.6%

Reaction Steps

(2RS,5RS)-4-[5-(4-Fluoro-phenyl)-1-(toluene-4-sulfonyl)-pyrrolidin-2-yl]-N-hydroxy-butyramidine (1.1 g, 2.62 mmol) was dissolved in EtOH (50 ml) and acetic acid (5 ml) and hydrogenated on Ra—Ni at room temperature for 2 h. The catalyst was filtered off, the filtrate evaporated and the crude product crystallized from saturated NaHCO3 solution to give (2RS,5RS)-4-[5-(4-fluoro-phenyl)-1-(toluene-4-sulfonyl)-pyrrolidin-2-yl]-N-butyramidine (0.81 g, 76%) as a light brown solid.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06589978B2
Source datasetuspto-grants-2003_07
ORD IDord-a7147016ce574350872aa95bfe2435b5
Source noteuspto-grants-2003_07