3-Chloro-4-fluoroaniline → 2-Bromo-6-(4-chloro-3-fluoro-phenyl)-5-[5-chloro-1-(4-methoxy-benzyl)-2-oxo-1,2-dihydro-pyridin-3-yl]-1-isopropyl-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-4-one

Participants

Reaction Steps

The title compound was prepared in analogy to the procedure described for Intermediate D but in the step corresponding to Step D2,5-bromo-2-[(4-chloro-3-fluoro-phenyl)-hydroxy-methyl]-1-isopropyl-1H-pyrrole-3-carboxylic acid methyl ester (Step AZ1) and 3-amino-5-chloro-1-(4-methoxy-benzyl)-1H-pyridin-2-one (Step AH1) were used instead of 5-bromo-2-[(4-chloro-phenyl)-hydroxy-methyl]-1-isopropyl-1H-pyrrole-3-carboxylic acid methyl ester and 3-chloro-4-fluoroaniline respectively. Moreover, in this step, the procedures described for Steps H3 and H2 using 1-chloro-N,N,2-trimethylpropenylamine and Et3N were used. The title compound (containing some of the corresponding 2-chloro analog) was obtained as a yellow-brown solid. tR: 7.83 min (HPLC 2); ESI-MS: tR=1.36 min, [M+H]+ 618/620/622 (LC-MS 1); TLC: Rf=0.50 (98:2 CH2Cl2/MeOH).

Provenance & Evidence