Deconjugation and epimerization process

Details Deconjugation and epimerization process Deconjugation and epimerization process

C - Chemistry, Metallurgy

07

D

260/210, 260/228

C07D 493/22 (2006.01) C07F 7/18 (2006.01) C07H 17/08 (2006.01) C07H 19/01 (2006.01)

Patent

CA 1282061

ABSTRACT There are disclosed novel methods of preparing pentacyclic macrolides having sixteen member lactone rings. Earlier synthetic approaches gave unpredictable variation of the desired products and hence much reduced biological activities, attributed to the final steps of conjugation, deconjugation, and epimerization. An improved two step route has been devised, involving epimerization subsequent to deconjugation, yielding products of higher and more consistent purity. The .DELTA.2- isomer is first deconjugated to the 2-epi form which is then epimerized to the desired end product. This process is generally applicable to the pentacyclic sixteen member lactone ring macrolides, including the avermectins, milbemycins, and related compounds. These compounds possess broad spectrum antiparasitic activity against, e.g., nematodes.

540623

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