117048-62-1Relevant articles and documents
Heterobimetallic Pd/Mn and Pd/Co complexes as efficient and stereoselective catalysts for sequential Cu-free Sonogashira coupling–alkyne semi-hydrogenation reactions
Baweja, Saral,Clauss, Reike,Gelman, Dmitri,Hey-Hawkins, Evamarie
, p. 1344 - 1356 (2022/02/03)
A series of heterobimetallic PdII/MII complexes (MII = Mn, Co) were synthesised and tested as precatalysts for sequential Sonogashira coupling–alkyne semi-hydrogenation reactions to form Z-aryl alkenes. The carbometalated heterobimetallic PdII/CoII complex CoPdL3′ demonstrated an apparent cooperative effect compared to the corresponding monometallic counterparts. This compound was identified as a potent single-molecule catalyst for the one-pot Cu-free Sonogashira coupling of aryl bromides with terminal alkynes followed by chemo- and stereoselective semi-hydrogenation of the alkyne intermediate using NH3·BH3 as a hydrogen source. Furthermore, different aromatic substrates have been tested to show the generality of the reaction for the synthesis of Z-alkenes, including biologically active combretastatin A-4. In addition, the homogeneous nature of the catalytically active species was demonstrated.
Orchid heterocyclic derivative as well as preparation method and application thereof
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, (2021/10/16)
The invention relates to a lansamine heterocyclic derivative as well as a preparation method and application thereof. Wherein, X is O or NH. R Is one of a furanyl heterocyclic substituent, a thiophenyl heterocyclic substituent, a thiazolyl heterocyclic substituent, a pyrimidinyl heterocyclic substituent, a pyridazinyl heterocycle substituent, an indolyl heterocyclic substituent, and an indolyl heterocyclic substituent. The preparation method comprises the following steps: carrying out condensation reaction on crude orchid and a carboxylic acid compound containing the substituent R. Or, 4 - methoxy -3 - nitrobenzaldehyde and 3,trimethoxy - triphenyl benzyl bromide salt is used as a raw material, and after Wittig reaction and reduction reaction, the tetracarboxylic acid compound containing the substituent R is subjected to a condensation reaction. Compared with the prior art, heterocyclic compounds such as crude orchid and nicotinic acid are connected through an ester bond to form a twin medicine, and a new way is provided for improving the pharmacological activity of the crude orchid.
Synthesis and Cytotoxicity Studies of Stilbene Long-Chain Fatty Acid Conjugates
Brown, David P.,Chen, Zhe-Sheng,Narayanan, Silpa,Wong, Thomas
, (2020/04/20)
A series of 16 conjugates of the tubulin polymerization inhibitor combretastatin A4 (CA-4) and other functionally related stilbene with four 18-carbon fatty acids, namely, stearic, oleic, linoleic, and linolenic acids, have been synthesized in good yields. These new derivatives have been evaluated against the KB-3-1 (human epidermoid carcinoma), NCI-H460 (human lung cancer), HEK293 (human embryonic kidney), and MCF-7 (human breast adenocarcinoma) cell lines for antiproliferative activity, with the exhibited cytotoxic activities comparable with those of CA-4 and colchicine. Compounds 22 and 23, CA-4 conjugates of linoleic and linolenic acids, respectively, were determined to have exhibited the most active in vitro assays, with compound 23 exhibiting very similar activity to the parent compound against the NCI-H460 cell line. Our studies further delineated the structurally required Z-geometry of the stilbene moiety and that conjugation of the less active E-stilbenes with the most active fatty acid had minimal or no improvement in their respective activities.
