Back
HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1265929Generated: November 1, 2026

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

https://huagongshe.com/reaction/1265929

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
ReactantCarbamic acid,[2-amino-4-methyl-5-(methylpropylamino)phenyl]-,1,1-dimethylethyl esterHCID 69688441—
Reactant3-Oxo-3-[3-[4-(tetrahydro-pyran-2-yloxymethyl)-thiazol-2-yl]-phenyl]-propionic acid tert-butyl esterHCID 69688492—
SolventDichloromethaneHCID 6344—
Product4-[3-(4-Hydroxymethyl-thiazol-2-yl)-phenyl]-8-methyl-7-(methyl-propyl-amino)-1,3-dihydro-benzo[b][1,4]diazepin-2-oneHCID 18613261—

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)-thiazol-2-yl]-phenyl]-propionic acid tert-butyl ester (Example K27) (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 (0.09 g).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06544985B2
Source datasetuspto-grants-2003_04
ORD IDord-f20139d650cc42e2889f6236c1ac80ef
Source noteuspto-grants-2003_04