116324-66-4Relevant articles and documents
Total Synthesis of (+)-Nivetetracyclate A
Blitz, Michel,Heinze, Robert C.,Harms, Klaus,Koert, Ulrich
, p. 785 - 788 (2019)
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
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 COMPOUNDS
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Page/Page column 64, (2011/04/14)
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
Enantioselective synthesis of the lomaiviticin aglycon full carbon skeleton reveals remarkable remote substituent effects during the dimerization event
Lee, Hong Geun,Ahn, Jae Young,Lee, Amy S.,Shair, Matthew D.
supporting information; scheme or table, p. 13058 - 13062 (2011/02/24)
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′