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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 709162Generated: October 29, 2026

1,2-Dichloroethane → 2-({[3-(4-Chlorophenyl)-4-(2-fluorobenzyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl]acetyl}-amino)-1-[2-(trifluoromethyl)phenyl]ethyl carbamate

https://huagongshe.com/reaction/709162

Reaction equation

Participants

RoleNameHCIDCharge
Reactant1,2-DichloroethaneHCID 11—
ReactantHydrochloric AcidHCID 313—
Reactant1-HydroxybenzotriazoleHCID 75771—
Reactant[3-(4-chlorophenyl)-4-(2-fluorobenzyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl]-acetic acidHCID 58012119—
Reactant2-Amino-1-[2-(trifluoromethyl)phenyl]ethyl carbamateHCID 66635627—
SolventDimethylformamideHCID 6228—
Product2-({[3-(4-Chlorophenyl)-4-(2-fluorobenzyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl]acetyl}-amino)-1-[2-(trifluoromethyl)phenyl]ethyl carbamateHCID 66634964—

Reaction Steps

A mixture of 40 mg (111 μmol) of [3-(4-chlorophenyl)-4-(2-fluorobenzyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl]acetic acid [for the preparation see Example 156A in WO 2007/134862], 33 mg (133 μmol) of the compound of Example 37A, 25 mg (133 μmol) of EDC and 21 mg (133 μmol) of HOBt in 2.4 ml of DMF was stirred at RT overnight, 1 ml of 1 M hydrochloric acid was then added and the mixture was separated directly by preparative HPLC [Method 20] into its components. This gave 53 mg (81% of theory) of the title compound.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09180120B2
Source datasetuspto-grants-2015_11
ORD IDord-9f8156dc8a244651b6b71d31edabf75c
Source noteuspto-grants-2015_11