110339-54-3Relevant articles and documents
Practical total synthesis of RS-15385
Rohloff,Dyson,Gardner,Alfredson,Sparacino,Robinson III
, p. 1935 - 1938 (1993)
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Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CLpro covalent inhibitors
Stille, Julia K.,Tjutrins, Jevgenijs,Wang, Guanyu,Venegas, Felipe A.,Hennecker, Christopher,Rueda, Andrés M.,Sharon, Itai,Blaine, Nicole,Miron, Caitlin E.,Pinus, Sharon,Labarre, Anne,Plescia, Jessica,Burai Patrascu, Mihai,Zhang, Xiaocong,Wahba, Alexander S.,Vlaho, Danielle,Huot, Mitchell J.,Schmeing, T. Martin,Mittermaier, Anthony K.,Moitessier, Nicolas
, (2022/01/08)
Severe diseases such as the ongoing COVID-19 pandemic, as well as the previous SARS and MERS outbreaks, are the result of coronavirus infections and have demonstrated the urgent need for antiviral drugs to combat these deadly viruses. Due to its essential role in viral replication and function, 3CLpro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral drugs. Previously reported SARS-CoV 3CLpro non-covalent inhibitors were used as a starting point for the development of covalent inhibitors of SARS-CoV-2 3CLpro. We report herein our efforts in the design and synthesis of submicromolar covalent inhibitors when the enzymatic activity of the viral protease was used as a screening platform.
Xylochemistry - Making Natural Products Entirely from Wood
Stubba, Daniel,Lahm, Günther,Geffe, Mario,Runyon, Jason W.,Arduengo, Anthony J.,Opatz, Till
supporting information, p. 14187 - 14189 (2016/01/25)
The first total synthesis of the dimeric berberine alkaloid ilicifoline (ilicifoline B) is reported. Its carbon skeleton is constructed from ferulic acid, veratrole, and methanol. The synthesis reported herein employs starting materials solely derived from wood. The natural product is thus constructed entirely from renewable resources. The same strategy is applied to a formal total synthesis of morphinan alkaloids. The use of wood-derived building blocks (xylochemicals) instead of the conventional petrochemicals represents a sustainable alternative to classical synthetic approaches.
A synthesis of dihydroimidazo[5,1-a]isoquinolines using a sequential Ugi-Bischler-Napieralski reaction sequence
Seganish, W. Michael,Bercovici, Ana,Ho, Ginny D.,Loozen, Hubert J.J.,Timmers, Cornelis M.,Tulshian, Deen
scheme or table, p. 903 - 905 (2012/03/10)
A flexible route to analogues of dihydroimidazo[5,1-a]isoquinolines is described. The synthesis hinges on a sequential Ugi coupling, followed by a Bischler-Napieralski reaction to form the imidazole isoquinoline core. This route facilitates the introduction of a range of substitutions throughout the carbon framework.
