1254351-84-2Relevant articles and documents
Process Development and Scale-up of Fully Synthetic Tetracycline TP-2758: A Potent Antibacterial Agent with Excellent Oral Bioavailability
Zhang, Wu-Yan,Sun, Cuixiang,Hunt, Diana,He, Minsheng,Deng, Yonghong,Zhu, Zhijian,Chen, Chi-Li,Katz, Christopher E.,Niu, John,Hogan, Philip C.,Xiao, Xiao-Yi,Dunwoody, Nicholas,Ronn, Magnus
, p. 284 - 296 (2016/03/04)
Process research and development of the fully synthetic broad spectrum tetracycline TP-2758, with a chiral pyrrolidine side chain at the C-8 position, is described. The process utilizes two key intermediates, 7 and 10, in a convergent approach that allows for manufacturing of sufficient quantities of API to supply preclinical and early clinical development. The pyrrolidine moiety was introduced into the left-hand piece (LHP) 10 with high enantioselectivity using Ellman's sulfinamide chemistry, and the absolute configuration was confirmed by X-ray crystal structure analysis.
TETRACYCLINE ANALOGS
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, (2012/03/09)
The present invention is directed to a compound represented by Structural Formula (I), or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.