Method for increasing the alpha to beta ratio in an...

C - Chemistry – Metallurgy – 07 – K

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C07K 5/075 (2006.01)

Patent

CA 2058932

An improved coupling step of an .alpha.-APM manufacturing process is disclosed. The solvents in the coupling step are adjusted in one of two ways to improve the .alpha.- to .beta.- isomer ratio of the product of the coupling step, .alpha.,.beta. protected L-aspartyl-L-phenylalanine or lower alkyl ester thereof. In one manner, the solvent may comprise an increased concentration of a carboxylic acid such as acetic acid alone. In the other manner, one or more additional solvents along with a carboxylic acid such as acetic acid in conventionally known concentrations are used.

Étape de couplage améliorée pour méthode de production d'alpha-APM. Dans cette étape, les solvants sont ajustés selon l'un de deux processus de façon à améliorer le rapport isomère alpha/isomère bêta du produit de l'étape de couplage, soit la L-aspartyl-L-phénylalanine protégée en alpha,bêta, ou un ester d'alkyle inf. de celle-ci. Dans un des deux processus, le solvant peut comprendre une concentration plus grande d'un acide carboxylique, comme l'acide acétique seul. Dans l'autre processus, on utilise un ou plusieurs solvants supplémentaires, avec un acide carboxylique, comme l'acide acétique, aux concentrations habituelles.

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