- Method of making HIV protease inhibitors
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A method of making HIV protease inhibitors of general formula (1): These HIV compounds inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optically other antiviral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
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- Processes for producing β-halogeno-α-amino-carboxylic acids and phenylcysteine derivatives and intermediates thereof
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An industrially advantageous method of producing β-halogeno-α-aminocarboxylic acids is provided. Methods are also provided of producing optically active N-protected-S-phenylcysteines having high optical purity and of intermediates thereof, respectively, in which the above production method is utilized. A method of producing β-halogeno-α-aminocarboxylic acids or salts thereof is disclosed which comprises halogenating the hydroxyl group of a β-hydroxy-α-aminocarboxylic acid (in which the basicity of the amino group in α-position is not masked by the presence of a substituent on said amino group) or a salt thereof with an acid with a halogenating agent. A method of producing optically active N-protected-S-phenylcysteines represented by the general formula (3) or salts thereof is further disclosed which comprises applying the above production method to optically active serine or a salt thereof and then carrying out treatment with an amino-protecting agent and reaction with thiophenol under a basic condition.
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- Process for S-Aryl cysteine
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The present invention provides methods for preparing S-aryl cysteines in enantiomeric excess of greater than about 96%. Specifically, the present invention provides enantioselective methods for preparing S-aryl cysteines starting from cystine, cysteine or
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- Preparation of S-aryl-cysteine and its derivatives
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The present invention provides a method for preparing S-aryl cysteine. Specifically, the present invention provides enantioselective method for preparing S-aryl cysteine starting from cystine, cysteine or serine amino acid. The methods of the present inve
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- Method for isolation of n-protected s-phenylcysteine
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This invention provides a method of isolating N-protected-S-phenylcysteine (1) of high purity, expediently, efficiently and in good yield, which comprises causing said N-protected-S-phenylcysteine to be salted out in the form of a base salt in the presence of water. wherein R1represents an amino-protecting group; R2represents a hydrogen atom or, either independently of R1or taken together with R1, represents an amino-protecting group.
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- Copper-mediated cross-coupling of aryl boronic acids and alkyl thiols
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matrix presented The cross-coupling of aryl boronic acids and alkanethiols mediated by copper(II) acetate and pyridine in anhydrous dimethylformamide affords aryl alkyl sulfides in good yield with a wide variety of substituted aryl boronic acids. The method is applicable to the synthesis of aryl sulfides of cysteine.
- Herradura, Prudencio S.,Pendola, Kathleen A.,Guy, R. Kiplin
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p. 2019 - 2022
(2007/10/03)
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- HIV protease inhibitors
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HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
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- Viracept (nelfinavir mesylate, AG1343): A potent, orally bioavailable inhibitor of HIV-1 protease
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Using a combination of iterative structure-based design and an analysis of oral pharmacokinetics and antiviral activity, AG1343 (Viracept, nelfinavir mesylate), a nonpeptidic inhibitor of HIV-1 protease, was identified. AG1343 is a potent enzyme inhibitor
- Kaldor, Stephen W.,Kalish, Vincent J.,Davies II, Jay F.,Shetty, Bhasker V.,Fritz, James E.,Appelt, Krzysztof,Burgess, Jeffrey A.,Campanale, Kristina M.,Chirgadze, Nickolay Y.,Clawson, David K.,Dressman, Bruce A.,Hatch, Steven D.,Khalil, Deborah A.,Kosa, Maha B.,Lubbehusen, Penny P.,Muesing, Mark A.,Patick, Amy K.,Reich, Siegfried H.,Su, Kenneth S.,Tatlock, John H.
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p. 3979 - 3985
(2007/10/03)
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- HIV protease inhibitors
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HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain the
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- HIV protease inhibitors
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HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
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- Inhibitors of HIV protease useful for the treatment of AIDS
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The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.
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- Intermediate and process for making
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The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.
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- A convenient, large scale synthesis of N-CBZ-(S-phenyl)-L-cysteine
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N-Cbz-(S-phenyl)-L-cysteine (3) has been prepared on a multikilogram scale in high yield and optical purity from the β-lactone of N-Cbz-L-serine.
- Marzoni,Kaldor,Trippe,Shamblin,Fritz
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p. 2475 - 2482
(2007/10/02)
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- Pummerer-type cyclization of Arnstein tripeptide analogues induced by O-silylated ketene acetals: Studies of penicillin biosynthesis
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We report the first biomimetic conversion of Arnstein tripeptide analogues (1a and 1b) into cis β-lactams (2a and 2b) using O-silylated ketene acetal (3) involving asymmetric induction from the sulfoxide sulfur to the α-carbon. The peptide 1 was treated w
- Kita, Yasuyuki,Shibata, Norio,Kawano, Noriyuki,Tohjo, Takashi,Fujimori, Chino,Ohishi, Hirofumi
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p. 5116 - 5121
(2007/10/02)
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- A total synthesis of (-)-slaframine from (+)-cis-(2R,3S)-3-hydroxyproline
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A total synthesis of the naturally occurring indolizidine (-)-Slaframine 4 has been achieved, starting from the cis-3-hydroxyproline derivative 1, in which a key step is a Julia olefination reaction using the dianion derived from the β-aminosulfone 5.
- Knight,Sibley
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p. 6607 - 6610
(2007/10/02)
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