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PAT Application in the Expedited Development of a Three-Step, One-Stage Synthesis of the Dipeptide Intermediate of HCV Protease Inhibitor Faldaprevir

Autor: Jon C. Lorenz, Carl A. Busacca, Dominique Hebrault, Nizar Haddad, Chris H. Senanayake, XuWu Feng, Rich Varsolona, Simon Rea, Leen Schellekens, Heewon Lee, Max Sarvestani, Suresh R. Kapadia, Bo Qu

Publikováno v: Organic Process Research & Development. 19:132-138

A concise scalable synthesis of a chiral dipeptide acid, key substructure of the HCV protease inhibitor faldaprevir, has been developed. A green process with an E-factor of 9.2 was achieved utilizing process analytical technology (PAT) to allow effec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::51bc048075827dc233c81f0130fe6446
https://doi.org/10.1021/op400285y

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Practical Large-Scale Synthesis of the Hepatitis C Virus Protease Inhibitor BI 201335

Publikováno v: Asian Journal of Organic Chemistry. 1:80-89

A concise synthetic route for large-scale manufacture of the hepatitis C virus (HCV) protease inhibitor BI 201335 has been developed. A convergent synthetic design was achieved by using three advanced intermediates: a densely functionalized thiazole-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::707936b50f896303356fb30b8a615528
https://doi.org/10.1002/ajoc.201200014

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Large-Scale Asymmetric Synthesis of a Cathepsin S Inhibitor

Autor: Nelu Grinberg, Xudong Wei, Chris H. Senanayake, Nizar Haddad, Joe Johnson, Earl Spinelli, Suresh R. Kapadia, Heewon Lee, Carl A. Busacca, Max Sarvestani, Jon C. Lorenz, Xingzhong Zeng, Rich Varsolona, Anjan Saha, XuWu Feng

Publikováno v: The Journal of Organic Chemistry. 75:1155-1161

A potent reversible inhibitor of the cysteine protease cathepsin-S was prepared on large scale using a convergent synthetic route, free of chromatography and cryogenics. Late-stage peptide coupling of a chiral urea acid fragment with a functionalized

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b30af52e991d8b73166535a0efc21f2e
https://doi.org/10.1021/jo9022809

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Development of a Pilot-Plant Process for a Nevirapine Analogue HIV NNRT Inhibitor

Publikováno v: Organic Process Research & Development. 12:603-613

The pilot-plant synthesis of nevirapine analogue 1 is described. The compound was prepared in eight steps from substituted pyridine raw materials and 4-hydroxyquinoline. The key transformation involves a novel one-pot conversion of an arylhalide to a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5e0feca550c211e03fd8878cedde9db7
https://doi.org/10.1021/op8000756

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Development of an Asymmetric Acetate Aldol Reaction with a Trifluoromethyl Ketone

Autor: Nelu Grinberg, Jinghua Xu, Jonathan T. Reeves, Zhulin Tan, Katie Kuzmich, Jinhua J. Song, Chris H. Senanayake, Heewon Lee, Nathan K. Yee, XuWu Feng

Publikováno v: Organic Process Research & Development. 11:534-538

We describe the discovery and development of a chiral auxiliary-controlled asymmetric acetate aldol reaction with a trifluoromethyl ketone. Chiral acetate 3d was prepared efficiently from (1S,2R)-1-amino-2-indanol. Reaction of the lithium enolate of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e8942110da913efebb498c04e62fd02c
https://doi.org/10.1021/op060211+

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Efficient Large-Scale Synthesis of BILN 2061, a Potent HCV Protease Inhibitor, by a Convergent Approach Based on Ring-Closing Metathesis

Publikováno v: The Journal of Organic Chemistry. 71:7133-7145

A multistep scalable synthesis of the clinically important hepatitis C virus (HCV) protease inhibitor BILN 2061 (1) is described. The synthesis is highly convergent and consists of two amide bond formations, one etherification, and one ring-closing m

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ff05409b6030e93939b82eb046705a1
https://doi.org/10.1021/jo060285j

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Practical Stereoselective Synthesis of an α-Trifluoromethyl-α-alkyl Epoxide via a Diastereoselective Trifluoromethylation Reaction

Autor: XuWu Feng, Zhulin Tan, Fabrice Gallou, Jinhua J. Song, Jinghua Xu, Lisa Delattre, Jonathan T. Reeves, Nathan K. Yee, Ranjit Ramdas, Heewon Lee, Chris H. Senanayake, Katie Kuzmich

Publikováno v: The Journal of Organic Chemistry. 72:292-294

A practical stereoselective synthesis is reported for an alpha-trifluoromethyl-alpha-alkyl epoxide (1), which is an important pharmaceutical intermediate. The key step involves a chiral auxiliary-controlled asymmetric trifluoromethylation reaction fo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c7811c4d7e7733998fa9d75fface996
https://doi.org/10.1021/jo061839l

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