Reaktion #586054

Reaktionsgleichung

4,5-bis-trifluoromethyl-benzene-1,2-diamine

(RS)-3-oxo-3-{3-[2-(tetrahydro-pyran-2-yloxymethyl)-pyridin-4-yl]-phenyl}-propionic acid tert-butyl ester

TFA

→

title compound

4-[3-(2-Hydroxymethyl-pyridin-4-yl)-phenyl]-7,8-bis-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one

Lösungsmittel

toluene

CH2Cl2

Reaktionsbedingungen

Vorschrift

The title compound was prepared from 4,5-bis-trifluoromethyl-benzene-1,2-diamine [CAS-No. 30454-92-3] (244 mg, 1.0 mmol) and (RS)-3-oxo-3-{3-[2-(tetrahydro-pyran-2-yloxymethyl)-pyridin-4-yl]-phenyl}-propionic acid tert-butyl ester (Example K40) (412 mg, 1.0 mmol) in toluene (10 ml) under reflux conditions for 2 h according to the general procedure M and subsequent treatment with TFA in CH2Cl2 according to the general procedure N. Obtained as a light yellow solid (291 mg, 61%).

Quelle