21382-82-1Relevant articles and documents
Close the ring to break the cycle: Tandem quinolone-alkyne-cyclisation gives access to tricyclic pyrrolo[1,2-: A] quinolin-5-ones with potent anti-protozoal activity
Szamosvári, Dávid,Sylvester, Kayla,Schmid, Philipp,Lu, Kuan-Yi,Derbyshire, Emily R.,B?ttcher, Thomas
, p. 7009 - 7012 (2019)
Expanding the chemical space of quinolones led to a tandem quinolone-alkyne-cyclisation reaction allowing chemoselective control of the synthesis of tricyclic pyrrolo[1,2-a]quinolin-5-ones. Importantly, we discovered anti-protozoal activity against Plasmodium and Toxoplasma with specific potency of one of the compounds against the liver stage of the malaria parasite in the nanomolar range.
Total Synthesis of (-)-Hymenosetin
Kauhl, Ulrich,Andernach, Lars,Weck, Stefan,Sandjo, Louis P.,Jacob, Stefan,Thines, Eckhard,Opatz, Till
, p. 215 - 228 (2016)
The 3-decalinoyltetramic acid (-)-hymenosetin and its N-methyl analogue were prepared in 11 and 8 steps, respectively, from (+)-citronellal using an intramolecular Diels-Alder reaction as the key step. This method represents the first example for the synthesis of a 3-decalinoyltetramic acid with a free NH moiety. The stereochemistry of the title compound, an unnatural diastereomer, and of a decalin building block was studied in detail using circular dichroism spectroscopy in the IR and UV/VIS freqeuncy range. This allowed to determine the absolute configuration of the natural product and to plan the synthetic route.
Preparation method of zeatin
-
Paragraph 0059-0061, (2020/09/23)
The invention provides a preparation method of zeatin, which relates to the technical field of organic synthesis, the preparation method comprises the following steps: reducing 6-trans-(3-methyl-2-alkene-4-butyrate)group-aminopurine to prepare zeatin; according to the brand-new zeatin synthesis route provided by the invention, 6-trans-(3-methyl-2-alkene-4-butyrate)-aminopurine is used as a raw material, is a relatively good solid, is easy to treat, relatively few in synthesis route steps, relatively high in yield and easy to produce and amplify, and further can realize industrial production.
Metal-Free Transfer Hydroiodination of C-C Multiple Bonds
Chen, Weiqiang,Walker, Johannes C. L.,Oestreich, Martin
, p. 1135 - 1140 (2019/01/11)
The design and a gram-scale synthesis of a bench-stable cyclohexa-1,4-diene-based surrogate of gaseous hydrogen iodide are described. By initiation with a moderately strong Br?nsted acid, hydrogen iodide is transferred from the surrogate onto C-C multiple bonds such as alkynes and allenes without the involvement of free hydrogen iodide. The surrogate fragments into toluene and ethylene, easy-to-remove volatile waste. This hydroiodination reaction avoids precarious handling of hydrogen iodide or hydroiodic acid. By this, a broad range of previously unknown or difficult-to-prepare vinyl iodides can be accessed in stereocontrolled fashion.