Processes for the preparation of 5-hydroxy-3-oxopentanoic...

Details Processes for the preparation of 5-hydroxy-3-oxopentanoic... Processes for the preparation of 5-hydroxy-3-oxopentanoic...

C - Chemistry, Metallurgy

07

C

C07C 67/343 (2006.01) C07B 49/00 (2006.01) C07C 69/716 (2006.01) C07C 253/30 (2006.01) C07C 255/21 (2006.01) C07D 319/06 (2006.01) C12P 7/62 (2006.01)

Patent

CA 2339357

Processes by which 5-hydroxy-3-oxopentanoic acid derivatives useful as intermediates of drugs can be prepared from inexpensive and easily available raw materials under noncryogenic conditions. Specifically, a process for preparing 5-hydroxy-3-oxopentanoic acid derivatives by making lithium amide act on a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative at a temperature of -20 ~C or above; and another process for preparing 5-hydroxy-3-oxopentanoic acid derivatives by treating a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative with a Grignard reagent and then making lithium amide act on the resulting mixture at a temperature of -20 ~C or above.

L'invention concerne des procédés permettant de préparer des dérivés d'acide 5-hydroxy-3-oxopentanoïque pouvant être utilisés comme intermédiaires de médicaments, à partir de matières brutes peu onéreuses et facilement disponibles, dans des conditions non cryogéniques. De manière spécifique, l'invention concerne un procédé de préparation de dérivés d'acide 5-hydroxy-3-oxopentanoïque en faisant réagir l'amide de lithium avec un mélange d'un ester d'acide acétique et un dérivé d'acide 3-hydroxypropionique à une température supérieure ou égale à 20 ·C. L'invention a pour objet un autre procédé de préparation de dérivés d'acide 5-hydroxy-3-oxopentanoïque et un dérivé d'acide 3-hydroxypropionique avec un réactif de Grignard. Ce procédé consiste ensuite à faire réagir l'amide de lithium sur le mélange obtenu à une température supérieure ou égale à -20 ·C.

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