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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1402301Generated: October 31, 2026

1,2-Dichloroethane → HCID 86687143, compound

https://huagongshe.com/reaction/1402301

Reaction equation

Participants

RoleNameHCIDCharge
Reactant1,2-DichloroethaneHCID 11—
Reactant1-HydroxybenzotriazoleHCID 75771—
Reactant5-Fluoro-2-hydrazinylpyridineHCID 19916786—
Reactant(4R)-4-Fluoro-1-methyl-L-prolineHCID 55300764—
SolventWaterHCID 962—
SolventDimethylformamideHCID 6228—
SolventDichloromethaneHCID 6344—
ProductHCID 86687143HCID 8668714347.9%

Reaction Steps

A solution of (5-fluoro-pyridin-2-yl)-hydrazine (378 mg, 2.98 mmol), Intermediate 91a (600 mg, 4.08 mmol) and HOBt.H2O (44 mg, 0.12 mmol) in DCM (10 mL) and DMF (3 mL) was added EDC (628 mg, 3.28 mmol) portionwise at RT and the mixture stirred at RT for 17 h. The solution was diluted with water and extracted with DCM. The combined organics were dried and concentrated in vacuo. The residue was purified by FCC, using 0-7.5% [2M NH3 in MeOH] in DCM, to give the title compound as light orange powder (366 mg, 35%). LCMS (Method 3): Rt 0.56 min, m/z 257 [MH+].

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08907094B2
Source datasetuspto-grants-2014_12
ORD IDord-53bdc4e8627e4bcd8b71e10f5ec3f943
Source noteuspto-grants-2014_12