PENTACYCLINE DERIVATIVES FOR THE TREATMENT OF INFECTIONS
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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetra-cycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-pro liferative agents in the treatment of diseases of humans or other animals.
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(2020/07/02)
Process Research and Development of TP-808: A Key Intermediate for the Manufacture of Synthetic Tetracyclines
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
Zhang, Wu-Yan,Chen, Chi-Li,He, Minsheng,Zhu, Zhijian,Hogan, Philip,Gilicky, Olga,Dunwoody, Nicholas,Ronn, Magnus
p. 377 - 386
(2017/03/24)
SYNTHESIS OF TETRACYCLINES AND INTERMEDIATES THERETO
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.
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(2010/11/17)
SYNTHESIS OF ENONE INTERMEDIATE
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 a more efficient route for preparing the enone intermediate.
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(2008/12/08)
A practical, enantioselective synthetic route to a key precursor to the tetracycline antibiotics
A practical, enantioselective synthetic route to a key precursor to the tetracycline antibiotics is reported. The route proceeds in nine steps (21% yield) from the commercial substance methyl 3-hydroxy-5-isoxazolecarboxylate. Key steps in the route involve enantioselective addition of divinylzinc to 3-benzyloxy-5-isoxazolecarboxaldehyde and an endo-selective intramolecular furan Diels-Alder cycloaddition reaction. The route described has provided more than 40 g of chromatographically pure 1 with 93% ee.
Brubaker, Jason D.,Myers, Andrew G.
p. 3523 - 3525
(2008/02/11)
SYNTHESIS OF TETRACYCLINES AND ANALOGUES THEREOF
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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.
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Page/Page column 94-95
(2008/06/13)
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