Back
HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 14333Generated: October 25, 2026

1,2-Dichloroethane → HCID 86594207, compound

https://huagongshe.com/reaction/14333

Reaction equation

Participants

RoleNameHCIDCharge
Reactant1,2-DichloroethaneHCID 11—
Reactant1-HydroxybenzotriazoleHCID 75771—
Reactant4-[((1S,2R)-1-(3,5-difluorobenzyl)-3-{[1-(3-ethylphenyl)cyclopropyl)amino}-2-hydroxypropyl)amino]-4-oxobutanoic acidHCID 57512111—
SolventDimethylformamideHCID 6228—
ProductHCID 86594207HCID 8659420769.7%

Reaction Conditions

Temperature45 °C

Reaction Steps

To a solution of S-aminoquinuclidine (0.086 g, 0.434 mmol) TEA (0.302 ml, 2.17 mmol), and anhydrous DMF (2.5 ml) was added 4-[((1S,2R)-1-(3,5-difluorobenzyl)-3-{[1-(3-ethylphenyl)cyclopropyl]amino}-2-hydroxypropyl)amino]-4-oxobutanoic acid (0.200 g, 0.434 mmol), EDC (0.125 g, 0.651 mmol), and HOBT (0.088 g, 0.651 mmol) under nitrogen, with stirring at 45° C. overnight. Reaction mixture was quenched with 10% sodium bicarbonate (aq.) then extracted with ethyl acetate then concentrated in vacuo, yielding product (0.093 g). Prep-HPLC yielded the product as its formate salt. (ES+: 569.3)

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07727997B2
Source datasetuspto-grants-2010_06
ORD IDord-aa78d5986adc4125922ae35908a743c5
Source noteuspto-grants-2010_06