http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-101544630-A

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publicationDate 2009-09-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-101544630-A
titleOfInvention Hydroxylated indinavir, preparation method of hydroxylated indinavir, and application of hydroxylated indinavir in preparation of antimalarials
abstract The present invention provides hydroxylated indinavir represented by general formula (12). The present invention further provides a preparation method of hydroxylated indinavir, which employs cheap and widely available indene as the raw material, and comprises the following steps: dihydroxylate and protect the indene, oxidize the benzyl to introduce carbonyl, and then transform the carbonyl into amido, to obtain the required reaction intermediate; prepare the other molecular block from indinavir, carry out hydrolytic reaction, and protect the hydroxyl; then, carry out acidamide condensation with the reaction intermediate, remove the protection, to obtain the target product. The present invention further provides an application of hydroxylated indinavir in preparation of antimalarials, especially combination with chloroquini phosphas to treat malaria. The hydroxylated indinavir provided in the present invention has favorable in-vivo and in-vitro activity in inhibition of malarial parasite; when used in combination with chloroquini phosphas, it can works with chloroquini phosphas to inhibit malarial parasite that is resistant or sensitive to chloroquini phosphas in vitro and in vivo. The hydroxylated indinavir can be used to develop antimalarials and compound antimalarials, sets a basis for reapplying the economical and practical chloroquini phosphas in treatment of malaria, and has excellent application prospects.
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priorityDate 2009-05-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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