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US 5,861,512 AGranted
Process for making HIV protese inhibitors
AssigneeMerck & Co., Inc.
InventorsDavid Askin, Kai Rossen, Paul Reider, Richard J. Varsolona, Ralph P. Volante, Kenneth M. Wells
Life of this patent
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Abstract
Intermediates of structural formula ##STR1## can be made by reacting a primary or secondary amine with glycosidol or an activated derivative thereof. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.
Claims5
A process for the formation and resolution of (S)-2-tert-butylcarboxamidepiperazine comprising the steps of:
- (a) contacting a solution of (S)(R)-2-tert-butylcarboxamide-piperazine with an acid selected from D or L pyroglutamic acid in an aqueous-organic solvent mixture, wherein the organic solvent is a C.sub.1-4 alcohol;
- (b) heating the mixture to dissolve any solid that forms;
- (c) cooling the mixture;
- (d) if the precipitated crystals are predominantly comprised of the (S)-antipode, separating the precipitated crystals from the mother liquor;
- and
- (e) if the mother liquor is predominantly comprised of the (S)-antipode, separating the precipitated crystals from the mother liquor and recovering the (S)-antipode from the mother liquor.
3 more elements
Dependencies are inferred from the claim text.