Process for 5-aroylation of 1,2-dihydro-3h-...

Details Process for 5-aroylation of 1,2-dihydro-3h-... Process for 5-aroylation of 1,2-dihydro-3h-...

C - Chemistry, Metallurgy

07

D

260/299

C07D 487/04 (2006.01)

Patent

CA 1168244

ABSTRACT OF THE DISCLOSURE An improved process for 5-aroylation of 1,2-dihydro- 3H-pyrrolo[1,2-a]pyrrole-1-carboxylic esters or nitriles and for subsequent hydrolysis thereof is disclosed to produce compounds of the formula: Image (II) wherein Y is -COOR or -CN; R is hydrogen or lower alkyl; R1 is hydrogen or lower alkyl; and Ar is optionally substituted phenyl, or is selected from the group consisting of Image , Image and Image wherein X is 0 or S, R2 is hydrogen, methyl, chloro or bromo; and R3 is hydrogen or lower alkyl. In the improved process, an aroyl morpholide is reacted with the pyrrolo pyrrole system and the resultant decomposed with base.

390585

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