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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1678501Generated: November 1, 2026

Water → {4'-[4-(4-Dimethylsulfamoyl-piperazin-1-ylmethyl)-phenylcarbamoyl]-6-trifluoromethoxy-biphenyl-3-yl}-carboxylic acid tert-butyl ester

https://huagongshe.com/reaction/1678501

Reaction equation

Participants

RoleNameHCIDCharge
ReactantWaterHCID 962—
Reactant4-MethylmorpholineHCID 7972—
Reactant1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 15908—
Reactant1-HydroxybenzotriazoleHCID 75771—
Reactant4-(4-Amino-benzyl)-piperazine-1-sulfonic acid dimethylamideHCID 28273552—
Reactant5'-tert-Butoxycarbonylamino-2'-trifluoromethoxy-biphenyl-4-carboxylic acidHCID 59822341—
SolventDimethylformamideHCID 6228—
Product{4'-[4-(4-Dimethylsulfamoyl-piperazin-1-ylmethyl)-phenylcarbamoyl]-6-trifluoromethoxy-biphenyl-3-yl}-carboxylic acid tert-butyl esterHCID 67373671—

Reaction Steps

A mixture of 5′-tert-butoxycarbonylamino-2′-trifluoromethoxy-biphenyl-4-carboxylic acid (300 mg), 4-(4-amino-benzyl)-piperazine-1-sulfonic acid dimethylamide (226 mg), EDAC (144 mg) and HOBT (103 mg) in dry DMF (3 ml) containing N-methyl morpholine (0.166 ml) was stirred for 16 h. The mixture was then added to water (12 ml) and the resulting solid collected by filtration and dried and used in the following step without purification (558 mg)

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08008303B2
Source datasetuspto-grants-2011_08
ORD IDord-ea056892380d44d4bf87895aaf8d113c
Source noteuspto-grants-2011_08