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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1265864Generated: October 30, 2026

Trifluoroacetic acid → 4-[3-(5-Hydroxymethyl-[1,2,3]triazol-1-yl)-phenyl]-7-(isobutyl-methyl-amino)-8-methyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one

https://huagongshe.com/reaction/1265864

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
Reactant(RS)-[5-(Isobutyl-methyl-amino)-4-methyl-2-(3-oxo-3-{3-[5-(tetrahydro-pyran-2-yloxymethyl)-[1,2,3]triazol-1-yl]-phenyl}-propionylamino)-phenyl]-carbamic acid tert-butyl esterHCID 86586891—
SolventDichloromethaneHCID 6344—
Product4-[3-(5-Hydroxymethyl-[1,2,3]triazol-1-yl)-phenyl]-7-(isobutyl-methyl-amino)-8-methyl-1,3-dihydro-benzo[b][1,4]diazepin-2-oneHCID 18613191—

Reaction Steps

The title compound was prepared from (RS)-[5-(isobutyl-methyl-amino)-4-methyl-2-(3-oxo-3-{3-[5-(tetrahydro-pyran-2-yloxymethyl)-[1,2,3]triazol-1-yl]-phenyl}-propionylamino)-phenyl]-carbamic acid tert-butyl ester (Example M108) (0.33 g, 0.52 mmol) by treatment with TFA in CH2Cl2 according to the general procedure N. Obtained as a pale brown solid (188 mg, 79%).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06544985B2
Source datasetuspto-grants-2003_04
ORD IDord-952a382c62284746944ecf6ec6d0495d
Source noteuspto-grants-2003_04