Reaktion #585779

ord-df4510a9c92a46e19a5c8c37fd01c28d

Reaktionsgleichung

Cc1cc(NC(=O)CC(=O)c2cccc(-c3cnccn3)c2)c(NC(=O)OC(C)(C)C)cc1Cl
{5-chloro-4-methyl-2-[3-oxo-3-(3-pyrazin-2-yl-phenyl)-propionylamino]-phenyl}-carbamic acid tert-butyl ester
O=C(O)C(F)(F)F
TFA
→
Cc1cc2c(cc1Cl)N=C(c1cccc(-c3cnccn3)c1)CC(=O)N2
title compound
Cc1cc2c(cc1Cl)N=C(c1cccc(-c3cnccn3)c1)CC(=O)N2
7-Chloro-8-methyl-4-(3-pyrazin-2-yl-phenyl)-1,3-dihydro-benzo[b][1,4]diazepin-2-one

Edukte

Cc1cc(NC(=O)CC(=O)c2cccc(-c3cnccn3)c2)c(NC(=O)OC(C)(C)C)cc1Cl
{5-chloro-4-methyl-2-[3-oxo-3-(3-pyrazin-2-yl-phenyl)-propionylamino]-phenyl}-carbamic acid tert-butyl ester
O=C(O)C(F)(F)F
TFA

Reagenzien

Keine

Lösungsmittel

ClCCl
CH2Cl2

Reaktionsbedingungen

Detaillierte Bedingungen
See reaction.notes.procedure_details.

Vorschrift

The title compound was prepared from {5-chloro-4-methyl-2-[3-oxo-3-(3-pyrazin-2-yl-phenyl)-propionylamino]-phenyl}-carbamic acid tert-butyl ester (Example M94) (0.38 g, 0.79 mmol) by treatment with TFA in CH2Cl2 according to the general procedure N. Obtained as an off-white solid (240 mg, 84%).

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US06949542B2uspto-grants-2005_09