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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1265930Generated: November 2, 2026

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

https://huagongshe.com/reaction/1265930

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
Reactant3-Oxo-3-[3-[4-(tetrahydro-pyran-2-yloxymethyl)-oxazol-2-yl]-phenyl]-propionic acid tert-butyl esterHCID 69688022—
ReactantCarbamic acid,[2-amino-4-methyl-5-(methylpropylamino)phenyl]-,1,1-dimethylethyl esterHCID 69688441—
SolventDichloromethaneHCID 6344—
Product4-[3-(4-Hydroxymethyl-oxazol-2-yl)-phenyl]-8-methyl-7-(methyl-propyl-amino)-1,3-dihydro-benzo[b][1,4]diazepin-2-oneHCID 18613406—

Reaction Steps

The title compound was prepared from [2-amino-4-methyl-5-(methyl-propyl-amino)-phenyl]-carbamic acid tert-butyl ester (0.21 g) (Example J24) and 3-oxo-3-[3-[4-(tetrahydro-pyran-2-yloxymethyl)-oxazol-2-yl]-phenyl]-propionic acid tert-butyl ester (Example K11) (0.31 g) according to the general procedure M. The obtained material was deprotected and cyclized by treatment with TFA in CH2Cl2 according to the general procedure N. Obtained as a yellow solid (0.16 g).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06544985B2
Source datasetuspto-grants-2003_04
ORD IDord-b2205f3caaab433d8e40e30f66d89c9b
Source noteuspto-grants-2003_04