Process for preparing 2-piperazine carboxylic acid derivatives

Details Process for preparing 2-piperazine carboxylic acid derivatives Process for preparing 2-piperazine carboxylic acid derivatives

C - Chemistry, Metallurgy

07

D

C07D 241/04 (2006.01) C07D 403/12 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2186023

The invention concerns a process for preparing 2- piperazine carboxylic acid amides of general formula (I): Image (I) wherein a piperazine carboxylic acid, N-acylated with a halogenating agent to form a piperazine carboxylic acid anhydride of general formula (IV): Image (IV) is cyclized and finally converted into the end product (I) with an amino component. The 2-piperazine carboxylic acid amides of general formula (I) are lnter alia valuable intermediate products for preparing orally active HIV-1 protease inhibitors.

L'invention concerne un procédé pour préparer des amides d'acide 2-pipérazine carboxylique de formule générale (I), dans lequel un acide pipérazine carboxylique, N-acylé avec un agent d'halogénation pour former un anhydride d'acide pipérazine carboxylique de formule générale (IV), est cyclisé et finalement transformé en le produit final avec un constituant aminé. Les amides d'acide 2-pipérazine carboxylique de formule générale (I) sont entre autres des intermédiaires précieux pour préparer des inhibiteurs de la VIH-1-protéase actifs par voie orale.

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