Development and large-scale preparation of an oral TACE inhibitor

Organic Process Research and Development

Volumn 13, Issue 3, 2009, Pages 510-518

  Savage, Scott A ^a   Waltermire, Robert E ^a   Campagna, Silvio ^a   Bordawekar, Shailendra ^a   Toma, Joan Dalla Riva ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 66249098858     PISSN: 10836160     EISSN: 1520586X     Source Type: Journal    
DOI: 10.1021/op800308t     Document Type: Article

References (19)

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2. Duan, J. J.- W.; Chen, L.; Lu, Z.; Wasserman, Z. R.; Maduskuie, T. P.; Liu, R.- Q.; Covington, M. B.; Vaddi, K. G.; Qian, M.; Voss, M. E.; Xue, C.-B.; Hardman, K. D.; Ribadeneira, M. D.; Newton, R. C.; Magolda, R. L.; Christ, D. D.; Decicco, C. P. Abstracts of Papers; 224th ACS National Meeting, Boston, MA, U.S.A., August 18-22, 2002, American Chemical Society: Washington, DC, 2002, MEDI-426.
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13. This work was conducted before BSE/TSE issues became a concern. If this process is to be utilized for commercial manufacture, a further screen of enzymes will be conducted to identify one lacking this concern.
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19. This preparation was conducted in the late 1990s using PLE certified to originate from food-grade animals. As the issue of TSE/BSE emerged, a new synthesis that eliminated the need for PLE was devised to support further clinical studies. This new synthesis will be the subject of a future communication.