152120-54-2Relevant articles and documents
Synthesis and characterization of 4(R)-epimer impurities of zanamivir and laninamivir octanoate
Bi, Siju,Chen, Liang,Duan, Chuanqi,Lin, Kuaile,Liu, Weiyuan,Pan, Jing,Zhou, Ting,Zhou, Weicheng
, (2021/12/09)
The synthesis and characterization of compounds 7c and 8d, the 4(R)-epimer impurities of zanamivir and laninamivir octanoate, were reported for the first time. Their structures were confirmed by NMR and MS and distinguished from their corresponding active pharmaceutical ingredient (API) by coupling constant in 1H NMR and HPLC spectra. This work is of great significance for the drug-related substances analysis in zanamivir and laninamivir octanoate.
RADIOIODINATED COMPOUNDS
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Page/Page column 39, (2015/12/08)
This disclosure relates to reagents and methods useful in the synthesis of aryl iodines, for example, in the preparation of iodine labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.
Structure-activity relationship study on α1 adrenergic receptor antagonists from beer
Wakimoto, Toshiyuki,Nitta, Makoto,Kasahara, Kana,Chiba, Taketo,Yiping, Ye,Tsuji, Kuniro,Kan, Toshiyuki,Nukaya, Haruo,Ishiguro, Masaji,Koike, Minako,Yokoo, Yoshiaki,Suwa, Yoshihide
scheme or table, p. 5905 - 5908 (2010/06/13)
Hordatine A and aperidine have been previously isolated from beer as active ingredients, which bind to muscarinic M3 receptor. In addition, these compounds have exhibited antagonist activity against the α1A adrenoceptor. Although the relative structures of these two molecules have previously been determined, the absolute stereochemistry was unclear. Hence, to elucidate the absolute stereochemistry of natural hordatine A, we synthesized each enantiomer of hordatine A and aperidine from optically pure dehydrodi-p-coumaric acid. Several additional related compounds were also synthesized for structure-activity relationship studies. Chiral column HPLC analysis demonstrated that the absolute stereochemistry of natural hordatine A is (2S,3S), while based on the isomerization mechanism, the stereochemistry of aperidine is (2R,3S). The α1A adrenoceptor binding activity of (2R,3R)-hordatine A is the most potent among the enantiomeric pairs of hordatines and aperidines. Furthermore, the related, synthetic compound, (2R,3R)-methyl benzofurancarboxylate exhibits antagonist activity against the α1A adrenoceptor at a lower concentration than that of hordatine A.