Synthesis of protease inhibitor
First Claim
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1. A method of preparing a compound of the formula:
- ##STR4## comprising the steps of (1) providing a quantity of N-(Cis-2(R)-hydroxy-1(S)-indanyl)-5(S)-(1,1-dimethylethoxycarbonylamino)-4(S)-hydroxy-6-phenyl-2(R)-((4-(2-(4-morpholinyl)ethoxy)phenyl)methyl)-hexanamide of the formula;
##STR5## (2) incubating the compound of step (1) with Streptomyces culture #S-26-487 at temperatures ranging from about 20°
C. to about 42°
C. and at a pH in the range of from about 5.5 to 8.0 under aerobic conditions to prepare compound 1; and
(3) isolating the compound produced by step (2).
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Abstract
A dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces. It inhibits HIV protease, and is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
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Citations
1 Claim
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1. A method of preparing a compound of the formula:
- ##STR4## comprising the steps of (1) providing a quantity of N-(Cis-2(R)-hydroxy-1(S)-indanyl)-5(S)-(1,1-dimethylethoxycarbonylamino)-4(S)-hydroxy-6-phenyl-2(R)-((4-(2-(4-morpholinyl)ethoxy)phenyl)methyl)-hexanamide of the formula;
##STR5## (2) incubating the compound of step (1) with Streptomyces culture #S-26-487 at temperatures ranging from about 20°
C. to about 42°
C. and at a pH in the range of from about 5.5 to 8.0 under aerobic conditions to prepare compound 1; and(3) isolating the compound produced by step (2).
- ##STR4## comprising the steps of (1) providing a quantity of N-(Cis-2(R)-hydroxy-1(S)-indanyl)-5(S)-(1,1-dimethylethoxycarbonylamino)-4(S)-hydroxy-6-phenyl-2(R)-((4-(2-(4-morpholinyl)ethoxy)phenyl)methyl)-hexanamide of the formula;
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Current AssigneeMerck & Co., Inc.
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Original AssigneeMerck & Co., Inc.
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InventorsThompson, Wayne J., Lingham, Russell B., Arison, Byron H., Treiber, Laszlo R., Balani, Suresh K., Colwell, Lawrence F. Jr., Dezeny, Georgette
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Primary Examiner(s)NOT, DEFINED
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Assistant Examiner(s)Celsa, Bennett
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Application NumberUS07/842,814Time in Patent Office376 DaysField of Search435/253.5, 435/41, 435/71.1, 435/120, 544/60US Class Current435/41CPC Class CodesC07C 271/22 to carbon atoms of hydrocar...C12P 13/02 Amides, e.g. chloramphenico...
