Synthesis of synthons for the manufacture of bioactive...

C - Chemistry – Metallurgy – 12 – Q

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C12Q 1/00 (2006.01) C12N 9/00 (2006.01) C12N 9/88 (2006.01) C12P 1/00 (2006.01) C12P 17/06 (2006.01) C12P 33/00 (2006.01)

Patent

CA 2479247

The present invention is based on the discovery that 2-deoxyribose-5-phosphate aldolase (DERA, EC 4.1.2.4) and variants thereof can be used to catalyze sequential asymmetric aldol reactions between a wide variety of donor and acceptor aldehydes. The reaction products typically contain at least two new stereogenic centers and can be produced in enantiomerically pure form. As such, DERA catalyzed asymmetric aldol chemistry can be exploited to produce synthons for the synthesis of a variety of bioactive molecules.

la présente invention procède de la découverte que la 2-désoxyribose-5-phosphate aldolase (DERA, EC 4.1.2.4) et ses variants peut s'utiliser pour catalyser des réactions aldol asymétriques séquentielles entre une multiplicité d'aldéhydes donneurs et accepteurs. En général, les produits de réaction comprennent au moins deux nouveaux centres stéréogéniques et peuvent être produits sous une forme pure au plan énantiomère. Dans cette optique, la chimie aldol asymétrique à catalyse par DERA peut être exploitée en vue de la production de synthons pour la synthèse de diverses molécules bioactives.

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