- Total Synthesis of (+)-Nivetetracyclate A
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A stereoselective synthetic approach to the natural product (+)-nivetetracyclate A is reported. The tetracyclic skeleton was assembled in a convergent manner by an alkylation to a diarylmethane and subsequent Friedel-Crafts acylation. Further key steps ar
- Blitz, Michel,Heinze, Robert C.,Harms, Klaus,Koert, Ulrich
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- Process Development and Scale-up of Fully Synthetic Tetracycline TP-2758: A Potent Antibacterial Agent with Excellent Oral Bioavailability
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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.
- 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
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p. 284 - 296
(2016/03/04)
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- TETRACYCLINE COMPOUNDS
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The present invention is directed to a compound represented by Structural Formula (1): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising th
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Page/Page column 64
(2011/04/14)
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- Enantioselective synthesis of the lomaiviticin aglycon full carbon skeleton reveals remarkable remote substituent effects during the dimerization event
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A full carbon skeleton of the natural product lomaiviticin has been synthesized. The approach features anionic annulation reactions to deliver A and B rings of the natural product, and stereoselective oxidative enolate coupling to form the central C2-C2′
- Lee, Hong Geun,Ahn, Jae Young,Lee, Amy S.,Shair, Matthew D.
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p. 13058 - 13062
(2011/02/24)
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