Solid supported synthesis of sulfonated 2-oxopiperazines

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 241/08 (2006.01) C07D 209/00 (2006.01) C07D 241/00 (2006.01) C07D 243/08 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2328934

The subject invention involves processes for making 2-oxopiperazine and homologous compounds using a solid support resin by (a) removing the protecting group from a N-protected amino acid ester of the resin (if present), (b) reacting the resulting unprotected resin ester with a sulfonyl chloride, (c) reacting the resulting intermediate with a N-protected amino alcohol, (d) removing the N-protecting group from the N from the amino alcohol, and (e) cleaving/cyclizing the product from the resin.

La présente invention concerne des procédés qui permettent de fabriquer des composés de 2-oxopipérazine et homologues au moyen d'un résine support solide et qui consistent à: (a) retirer le groupe protecteur de l'ester d'aminoacide protégé N (le cas échéant), (b) faire réagir la résine non protégée qui en résulte avec un chlorure de sulfuryle, (c) faire réagir le produit intermédiaire avec un alcool amino N-protégé, (d) retirer le groupe de protection-N de N de l'alcool amino et (e) séparer le produit de la résine.

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