Study On Synthesis Of Ketorolec And It’s Intermediates

In this paper,2-benzoylpyrrole was synthesized by using pyrrole as raw material. On that basis,1-(2-chloroethyl)-2-benzoylpyrrole,1-(3,3-diethoxycarbonylpropyl)-2-ben-zoylpyrrole, diethyl-5-benzoyl-1,2-dihydro-3H-pyrrol[1,2-a]pyrrole-1,1-dicarboxylate and5-benzoy1-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-l-carboxylic acid were synthesized and ch aracterized.Phosphorylchloride as the catalyst,2-benzoylpyrrole was synthesized by Vilsmeier-Haack reaction of pyrrole and benzamide, the yield was77%. The optimal reaction conditions were as follow:n(benzamide):n(pyrrole):n(phosphorylchloride)=1:1.2:1.8.The pilot test shows that it can be used in industrial produ-ction.Sodium hydroxide as the base,1,2-dichloroethane as solvent,1-(2-chloroet-hyl)-2-benzoylpyrrole was synthesized by the reaction of2-benzoylpyrrole and1,2-chloroetha-ne, the yield was86%～87%.1-(3,3-diethoxycarbonylpropyl)-2-benzoylpyrrole was synthesized by the reaction of1-(2-chloroethyl)-2-benzoylpyrrole and diethyl malonate. Manganese (Ⅲ)acetate was synthesized by the reaction of manganese(Ⅱ)acetate and potassium permanganate, manganese(Ⅲ) acetate was used in the synthesis of diethyl-5-benzoyl-1,2-dihydro-3H-pyrrole[1,2-a]pyrrole-1,1-dicarboxylate, then followed by hydrosis, acidization and dec-arboxylation we received ketorolec.