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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 859547Generated: October 30, 2026

Trifluoroacetic acid → 8-(4-Fluoro-phenylethynyl)-4-(3-tetrazol-1-yl-phenyl)-1,3-dihydro-benzo[b][1,4]diazepin-2-one

https://huagongshe.com/reaction/859547

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
Reactant[2-Amino-4-(4-fluoro-phenylethynyl)-phenyl]-carbamic acid tert-butyl esterHCID 69486641—
Reactant3-Oxo-3-(3-tetrazol-1-yl-phenyl)-propionic acid ethyl esterHCID 69592791—
SolventDichloromethaneHCID 6344—
Product8-(4-Fluoro-phenylethynyl)-4-(3-tetrazol-1-yl-phenyl)-1,3-dihydro-benzo[b][1,4]diazepin-2-oneHCID 9845127—

Reaction Steps

Prepared from [2-amino-4-(4-fluoro-phenylethynyl)-phenyl]-carbamic acid tert.-butyl ester (Example G33) and 3-oxo-3-(3-tetrazol-1-yl-phenyl)-propionic acid ethyl ester (Example H15) according to the general procedure K. The obtained material was deprotected and cyclized by treatment with TFA in CH2Cl2 according to the general procedure M. Obtained as a beige powder (5.5 mg).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07151098B2
Source datasetuspto-grants-2006_12
ORD IDord-b68747766c3343d6829ef30b248f3956
Source noteuspto-grants-2006_12