- INHIBITORS OF MLH1 AND/OR PMS2 FOR CANCER TREATMENT
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The present invention relates to compounds of Formula (I) that target the MLH1 and/or PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process: Formula (I) wherein R1, R2, R3, R4, R6
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Paragraph 00393-00394
(2021/12/28)
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- Novel HCV virus NS3/4A inhibitor synthesizing intermediate and synthesis method
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The invention relates to a synthesis method of a medicinal intermediate, and belongs to the field of synthesis of medicines. According to the synthesis method, 4-bromoisoindoline (hydrochloride) is synthesized from 3-bromo-2-methyl-benzoic acid as a raw material. Not only is the raw material cost low, but also a preparation technology is simple, the synthesis yield is high, and industrial application and popularization values are achieved; meanwhile, the stability of the raw material of the intermediate can be improved through one-step t-butyloxycarbonylation, so that the addition amount of the raw material in the synthesis process is reduced, the cost is further reduced, and the synthesis yield is improved.
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- PROCESS AND INTERMEDIATES FOR PREPARING MACROLACTAMS
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The present invention relates to macrolactam compounds, intermediates useful in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing and modifying macrolactams. One use of the compounds and methods described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. An example of an HCV inhibitory compound that can be synthesized using the procedures described herein is Compound A and derivative thereof.
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- Synthesis of the HCV protease inhibitor Vaniprevir (MK-7009) using ring-closing metathesis strategy
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Figure Persented: A highly efficient synthesis of Vaniprevir (MK-7009) has been accomplished in nine linear steps and 55% overall yield. The key features of this synthesis include a cost-effective synthesis of the isoindoline subunit and efficient construction of the 20-membered macrocyclic core of Vaniprevir (MK-7009) utilizing ring-closing metathesis technology. A high-performing ring-closing metathesis protocol has been achieved by simultaneous slow addition of the ruthenium catalyst (0.2 mol %) and the diene substrate at a concentration of 0.13 M.
- Kong, Jongrock,Chen, Cheng-Yi,Balsells-Padros, Jaume,Cao, Yang,Dunn, Robert F.,Dolman, Sarah J.,Janey, Jacob,Li, Hongmei,Zacuto, Michael J.
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p. 3820 - 3828
(2012/06/29)
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- Synthesis of vaniprevir (MK-7009): Lactamization to prepare a 22-membered macrocycle
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Development of a practical synthesis of MK-7009, a 22-membered macrocycle, is described. A variety of ring-closing strategies were evaluated, including ring-closing metathesis, intermolecular palladium-catalyzed cross-couplings, and macrolactamization. Ri
- Song, Zhiguo J.,Tellers, David M.,Journet, Michel,Kuethe, Jeffrey T.,Lieberman, David,Humphrey, Guy,Zhang, Fei,Peng, Zhihui,Waters, Marjorie S.,Zewge, Daniel,Nolting, Andrew,Zhao, Dalian,Reamer, Robert A.,Dormer, Peter G.,Belyk, Kevin M.,Davies, Ian W.,Devine, Paul N.,Tschaen, David M.
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p. 7804 - 7815
(2011/12/14)
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- HCV NS3 PROTEASE INHIBITORS
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The present invention relates to macrocyclic compounds of formula (Ia) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
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Page/Page column 65
(2010/07/04)
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- HCV NS3 PROTEASE INHIBITORS
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The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use treating or preventing HCV infections.
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Page/Page column 33-34
(2008/12/05)
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- HCV NS3 protease inhibitors
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The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
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Page/Page column 68
(2008/06/13)
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