The glucuronide metabolites of benproperine were synthesized from mono-hydroxylate metabolites of benproperine that were treated with methyl （2,3,4-tri-O-acetyl-1-O-tfichloroacetimidoyl ） -α-D-glucopyranuronate wit...The glucuronide metabolites of benproperine were synthesized from mono-hydroxylate metabolites of benproperine that were treated with methyl （2,3,4-tri-O-acetyl-1-O-tfichloroacetimidoyl ） -α-D-glucopyranuronate with BF3 · Eh O as the promoter followed by basic hydrolyzation with Na2 CO3. The form of basic acceptors, the order of addition, and the promoter are all important variables in this glucuronidation. The salt form of the basic acceptor was found to be better than its free form for glucuronidation with a Lewis acid as the promoter. Two mono-hydroxylated benproperines were synthesized from 2-benzylphenol in three steps.展开更多
基金Supported by the National Natural Science Foundation of China(No. 39930180)
文摘The glucuronide metabolites of benproperine were synthesized from mono-hydroxylate metabolites of benproperine that were treated with methyl （2,3,4-tri-O-acetyl-1-O-tfichloroacetimidoyl ） -α-D-glucopyranuronate with BF3 · Eh O as the promoter followed by basic hydrolyzation with Na2 CO3. The form of basic acceptors, the order of addition, and the promoter are all important variables in this glucuronidation. The salt form of the basic acceptor was found to be better than its free form for glucuronidation with a Lewis acid as the promoter. Two mono-hydroxylated benproperines were synthesized from 2-benzylphenol in three steps.
