Process for preparing a keto-phosphonate intermediate useful in preparing HMG-CoA reductase inhibitors

A process is provided for preparing the keto-phosphonate n enantiomerically homogeneous form, by reacting the anhydride with S- alpha -methylbenzylamine to effect diastereoselective opening of the anhydride to give a mixture of amides separating the amides, for example, by fractional crystallization...

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Bibliographic Details
Main Author KARANEWSKY; DONALD S
Format Patent
LanguageEnglish
Published 14.02.1989
Edition4
Subjects
ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
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Summary:A process is provided for preparing the keto-phosphonate n enantiomerically homogeneous form, by reacting the anhydride with S- alpha -methylbenzylamine to effect diastereoselective opening of the anhydride to give a mixture of amides separating the amides, for example, by fractional crystallization, and converting the desired amide IVA (which is obtained in high yield from the anhydride) to enantiomerically homogeneous ketophosphonate in high yield and on a large scale. The so-formed ketophosphonate is useful in the synthesis of compactin as well as 7-substituted-(3,5-dihydroxy)-hept-6-enoic and -heptanoic acid HMG-CoA reductase inhibitors.
Bibliography:Application Number: US19880188564