Simple stereocontrolled synthesis of salinosporamide a

Details Simple stereocontrolled synthesis of salinosporamide a Simple stereocontrolled synthesis of salinosporamide a

C - Chemistry, Metallurgy

07

D

C07D 491/02 (2006.01)

Patent

CA 2570482

A simple and effective stereocontrolled synthesis of salinosporamide A (1) has been developed which follows the pathway outlined in the Figure. The process, the first total synthesis of salinosporamide A, is capable of providing the compound in substantial quantities for further biological studies. In addition to the method of Scheme I, the present invention also includes several novel synthetic intermediate compounds, several intermediate steps of the preferred synthetic process; and the uses of these compounds in the preparation of synthetic derivatives of the compound Salinosporamide A. Salinosporamide A is of special interest as a synthetic target because of its protein in vitro cytotoxic activity against many tumor cell lines (IC50 values of 10 nM or less).

L'invention porte sur un procédé de synthèse stéréocontrôlée simple et efficace de la salinosporamide A (1) conforme aux mécanismes décrits dans la figure. Ce procédé, permet la première synthèse totale de la Salinosporamide A, et sa production en quantités substantielles en vue de nouvelles études biologiques. En plus de la méthode du schéma (I), l'invention porte également sur plusieurs composés intermédiaires de synthèse nouveaux, sur plusieurs étapes intermédiaires du procédé de synthèse préféré, et sur l'utilisation des susdits composés pour la préparation de dérivés de synthèse de la Salinosporamide A, laquelle présente un intérêt spécial en tant que cible de synthèse en raison de son activité cytotoxique in vitro contre plusieurs lignées de cellules tumorales (valeurs de l'IC50 de 10 nM ou moins).

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