Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Earl Spinelli"'
Autor:
Earl Spinelli, Yin-Chao Tseng, Jonathan T. Reeves, Jinhua J. Song, Herbert Nar, Soojin Kim, John A. Smoliga, Nathan K. Yee, Varsolona Richard J, Zhibin Li, Chris H. Senanayake, Heewon Lee
Publikováno v:
Organic Process Research & Development. 17:540-548
A phosphoric acid cocrystal of a drug substance candidate at Boehringer Ingelheim was identified from the standard salt form screen and was characterized and shown to have desirable physicochemical properties, stability characteristics, and improved
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6efd6b7404046a2f46cd235d1ae2f313
https://doi.org/10.1021/op300239h
https://doi.org/10.1021/op300239h
Autor:
Bikshandarkoil A. Narayanan, Bing-Shiou Yang, Wenjun Tang, Alexander Sienkiewicz, Max Sarvestani, Denis Byrne, Zhibin Li, Laurence J. Nummy, Earl Spinelli, Ashish Chitroda, Nathan K. Yee, Soojin Kim, Shengli Ma, Heewon Lee, Nelu Grinberg, Xudong Wei, Nitinchandra D. Patel, Chris H. Senanayake
Publikováno v:
Organic Process Research & Development. 17:382-389
A facile and economical five-step process for the synthesis of a sodium–hydrogen exchange type I inhibitor (NHE-1) was developed from readily available starting materials in 43% overall yield. Key transformations included a highly efficient copper-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::953111085e2433d613ead94be7df06ff
https://doi.org/10.1021/op300331b
https://doi.org/10.1021/op300331b
Autor:
Carl A. Busacca, Scot Campbell, XuWu Feng, Nelu Grinberg, Varsolona Richard J, Paul-James Jones, Xudong Wei, Nizar Haddad, Oliver Niemeier, Chris H. Senanayake, Wendelin Samstag, Heewon Lee, Juergen Schroeder, Jana Vitous, Vittorio Farina, Nina C. Gonnella, Thilo Berkenbusch, Earl Spinelli, John A. Smoliga, Jon C. Lorenz, Suresh R. Kapadia, Zhibin Li, Max Sarvestani, Anjan Saha
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
https://doi.org/10.1002/ajoc.201200014
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
https://doi.org/10.1021/jo9022809
Autor:
Earl Spinelli, Mo Jiang, Zhibin Li, Chris H. Senanayake, Bing-Shiou Yang, Magnus C. Eriksson, Nathan K. Yee
Publikováno v:
Organic Process Research & Development. 13:1307-1314
Pharmaceutical cocrystals could be used to improve the physicochemical properties of active pharmaceutical ingredients. Here, a practical solid form screen approach to identify pharmaceutical cocrystals in the early development stage is proposed. Thi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ea19704dba03078496ed8dafd14c87e6
https://doi.org/10.1021/op900137j
https://doi.org/10.1021/op900137j
Autor:
Lana Louise Smith-Keenan, Paul Kreye, Wendelin Samstag, Thomas Nicola, Victor Fuchs, XuWu Feng, Jinghua Xu, Jana Vitous, Earl Spinelli, Rogelio P. Frutos, Jonathan Tan, Eric Winter, Robert D. Simpson, Li Zhang, Fabrice Gallou, Michael D. Ridges, Nathan K. Yee, Vittorio Farina, Marvin Johnson, Xiao-Jun Wang, Nizar Haddad, Ioannis N. Houpis, Xudong Wei, Michael Brenner, Kai Donsbach, Yibo Xu
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
https://doi.org/10.1021/jo060285j
Autor:
Shengli Ma, Elias I. Franses, Heewon Lee, Nelu Grinberg, Nathan K. Yee, Hung-Wei Tsui, Nien-Hwa Linda Wang, Carl A. Busacca, Ling Wu, Nina Gonella, Chris H. Senanayake, Keith R. Fandrick, Earl Spinelli
Publikováno v:
Journal of chromatography. A. 1362
Allenes are cumulenes with three contiguous carbons linked together through double bonds. 1,3-disubstituted allenes are not superimposable on their mirror image; as a consequence they are chiral. Chiral allenes are increasingly important in organic s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dad3171596cef3f9304d7f669f6a25a7
https://pubmed.ncbi.nlm.nih.gov/25193169
https://pubmed.ncbi.nlm.nih.gov/25193169
Autor:
Heewon Lee, Larry Nummy, Nathan K. Yee, Thomas Fachinger, Shengli Ma, Daniel R. Fandrick, Jonathan T. Reeves, Frank Roschangar, Denis Byrne, Max Sarvestani, Sherry Shen, Chris H. Senanayake, Bikshandarkoil A. Narayanan, Jinhua J. Song, Bo Qu, Phil DeCroos, Victor Fuchs, Nelu Grinberg, Zhibin Li, Burkhard Jäger, Ashish Chitroda, Jon C. Lorenz, Oliver Niemeier, Earl Spinelli, Soojin Kim, Nizar Haddad, Michael Brenner, Zhulin Tan, Xiufeng Sun, Varsolona Richard J, Sonia Rodriguez, Ajith Premasiri, Scot Campbell, Nina C. Gonnella
Publikováno v:
The Journal of organic chemistry. 78(8)
The development of a large scale synthesis of the glucocorticoid agonist BI 653048 BS H3PO4 (1·H3PO4) is presented. A key trifluoromethyl ketone intermediate 22 containing an N-(4-methoxyphenyl)ethyl amide was prepared by an enolization/bromine-magn
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::417034dc1c222b56e6e25fded0bb5608
https://pubmed.ncbi.nlm.nih.gov/23544738
https://pubmed.ncbi.nlm.nih.gov/23544738
Publikováno v:
Tetrahedron Letters. 37:2935-2938
Condensation of the triisobutylaluminum complex of cysteamine HCl with a variety of carboxylic esters furnishes thiazolines in one step. This new method has been applied to chiral α-aminoesters to give α-amino thiazolines of high optical purity, ye
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5e60a4ca50c3beff6bdcf6de4b9401d7
https://doi.org/10.1016/0040-4039(96)00451-0
https://doi.org/10.1016/0040-4039(96)00451-0
Publikováno v:
ChemInform. 27
Condensation of the triisobutylaluminum complex of cysteamine HCl with a variety of carboxylic esters furnishes thiazolines in one step. This new method has been applied to chiral α-aminoesters to give α-amino thiazolines of high optical purity, ye
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ec63732c7c595dedd11d14cbd7726b47
https://doi.org/10.1002/chin.199633143
https://doi.org/10.1002/chin.199633143