856906-36-0Relevant articles and documents
Process Research and Development of TP-808: A Key Intermediate for the Manufacture of Synthetic Tetracyclines
Zhang, Wu-Yan,Chen, Chi-Li,He, Minsheng,Zhu, Zhijian,Hogan, Philip,Gilicky, Olga,Dunwoody, Nicholas,Ronn, Magnus
, p. 377 - 386 (2017)
Process research, development, and manufacture of TP-808 (1), a key intermediate for the discovery and manufacture of tetracycline analogues, is described. The process used for the preparation of 1 avoids chromatographic purifications and has been substan
SYNTHESIS OF TETRACYCLINES AND INTERMEDIATES THERETO
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Page/Page column 122/251, (2010/11/17)
The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
