1601-20-3Relevant articles and documents
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Ellis et al.
, p. 488 (1963)
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Synthesis method of indometacin and analogues thereof
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, (2020/04/29)
The invention belongs to the technical field of indometacin synthesis, and discloses a synthesis method of indometacin and analogues thereof. The synthesis method of indometacin and analogues thereofcomprises the following steps: directly introducing alkyl, aromatic ring or heteroaromatic ring to the C2 position of indole through palladium catalyzed reaction; introducing a carboxylic acid fragment to the C3 position of the indole; and introducing an aroyl group to the N1 position of the indole. The method solves the problems that most of existing indometacin synthesis methods carry out modification by constructing an indole ring, simple structure change of indometacin molecules based on the synthesis strategy often needs de novo synthesis and synthesis steps for later modification and structure-activity relationship research of the indometacin molecules are tedious.
Ortho-Carbaborane derivatives of indomethacin as cyclooxygenase (COX)-2 selective inhibitors
Scholz, Matthias,Blobaum, Anna L.,Marnett, Lawrence J.,Hey-Hawkins, Evamarie
supporting information; experimental part, p. 4830 - 4837 (2012/09/22)
A series of novel indomethacin analogues with carbaboranes as three-dimensional substitutes for the chlorophenyl ring have been prepared. Their cyclooxygenase (COX) inhibition and enzyme selectivity has been tested and compared to the corresponding adamantyl analogues. Surprisingly, only the ortho-carbaborane derivatives were active compounds. Preliminary biological studies gave an interesting insight into the validity of employing carbaboranes as pharmacophores.
