- Merging lithium carbenoid homologation and enzymatic reduction: A combinative approach to the HIV-protease inhibitor Nelfinavir
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An effective stereocontrolled synthesis of the HIV protease inhibitor Nelfinavir is reported. Two transformations were identified crucial for achieving success: the formation of a densely functionalized α-chloroketone via the homologation of a Weinreb ami
- Castoldi, Laura,Ielo, Laura,Hoyos, Pilar,Hernáiz, María J.,De Luca, Laura,Alcántara, Andrés R.,Holzer, Wolfgang,Pace, Vittorio
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p. 2211 - 2217
(2018/03/28)
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- Intermediates useful in the synthesis of HIV-protease inhibitors and methods for preparing the same
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Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.
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Page/Page column 19
(2008/06/13)
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- INTERMEDIATES USEFUL IN THE SYNTHESIS OF HIV-PROTEASE INHIBITORS AND METHODS FOR PREPARING THE SAME
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Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed (Formula I).
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- Method of making a HIV-Protease inhibitor
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The present invention is directed to a method of making the HIV-protease inhibitor nelfinavir mesylate.
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Page/Page column 28
(2010/11/30)
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- (1S)-1-[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]-2-hydroxyethylammonium benzoate, a versatile building block for chiral 2-aminoalkanols: Concise synthesis and application to nelfinavir, a potent HIV-protease inhibitor
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A concise synthesis of a versatile chiral C4 building block for 2- aminoalkanols, (1S)-1-[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]2- hydroxyethylammonium benzoate (1a), was described. 1 (1a and its enantiomener 1b) acted as four stereoisomers of optically active 2-amino-1,3,4- butanetriol. The versatility of 1 was demonstrated by its application to the practical synthesis of nelfinavir (2), a potent HIV-protease inhibitor, as well as by the stereospecific synthesis of three diastereomers of 2.
- Inaba, Takashi,Yamada, Yasuki,Abe, Hiroyuki,Sagawa, Shoichi,Cho, Hidetsura
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p. 1623 - 1628
(2007/10/03)
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- Production of amide derivatives and intermediate compounds therefor
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A method for producing an amide derivative of the formula ?XV! STR1 wherein each symbol is as defined in the specification, and an enantiomer thereof, a novel intermediate useful for producing said compound and a production method thereof. The production method of the present invention is extremely easy and simple as compared to the conventional methods, and enables effective production of compound ?XV! at high yields, which includes compound ?XVI! having an HIV protease inhibitory action. In addition, the novel intermediates of the present invention are extremely useful as intermediates for producing not only the aforementioned compound ?XVI! but also compounds useful as X-ray contrast media.
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- Process for preparing oxiranemethanamine derivatives
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A process for preparing oxiranemethane derivatives which are useful as intermediates for preparing aspartyl protease inhibitors comprising the steps of activating an aminodiol, acylating the aminodiol and reacting the acylated aminodiol with a base to form an epoxy compound.
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