- Synthesis and characterization of 4(R)-epimer impurities of zanamivir and laninamivir octanoate
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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.
- Duan, Chuanqi,Liu, Weiyuan,Bi, Siju,Chen, Liang,Pan, Jing,Zhou, Ting,Lin, Kuaile,Zhou, Weicheng
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p. 569 - 576
(2021/12/09)
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- RADIOIODINATED COMPOUNDS
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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.
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Page/Page column 38
(2015/12/08)
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- Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities
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A series of acylguanidine-modified zanamivir analogs were synthesized and their inhibitory activities against the NAs of avian influenza viruses (H1N1 and H3N2) were evaluated. In particular, zanamivir derivative 3j, with a hydrophobic naphthalene substituent, exhibits the best inhibitory activity against group-1 NA with an IC50 of 20 nM. The Royal Society of Chemistry 2013.
- Lin, Chien-Hung,Chang, Tsung-Che,Das, Anindya,Fang, Ming-Yu,Hung, Hui-Chen,Hsu, Kai-Cheng,Yang, Jinn-Moon,Von Itzstein, Mark,Mong, Kwok Kong T.,Hsu, Tsu-An,Lin, Chun-Cheng
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supporting information
p. 3943 - 3948
(2013/07/05)
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- PYRROLOPYRIMIDINE AND PURINE DERIVATIVES
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The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
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Paragraph 0827; 0828
(2013/04/10)
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- Preparation of N-alkyl-N′-carboalkoxy guanidines: unexpected effective trans-alkoxylation transforming the 2,2,2-trichloroethoxycarbonyl into various carbamates
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A range of N-alkyl-N′-Boc guanidines was simply synthezized from monoprotected Boc-1H-pyrazole-1-carboxamidine by reaction with primary amines. Synthesis of the hindered (R)-N-methylbenzyl-N′-Troc guanidine was achieved from the corresponding thiourea by
- Schroif-Grégoire, Cosima,Barale, Karine,Zaparucha, Anne,Al-Mourabit, Ali
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p. 2357 - 2359
(2007/10/03)
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- Total synthesis of miraziridine A and identification of its major reaction site for cathepsin B
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The synthesis of miraziridine A, a pentapeptide derivative isolated from marine sponge, and its truncated analogs has been achieved. To construct the backbone of miraziridine A, a side-chain-unprotected vinylogous arginine was condensed with an aziridine-
- Konno, Hiroyuki,Kubo, Kanako,Makabe, Hidefumi,Toshiro, Emi,Hinoda, Naoyuki,Nosaka, Kazuto,Akaji, Kenichi
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p. 9502 - 9513
(2008/02/12)
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- Optimisation of the synthesis of guanidines from amines via nitroguanidines using 3,5-dimethyl-N-nitro-1H-pyrazole-1-carboxamidine
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The synthesis of the useful reagent for the preparation of guanidines, 3,5-dimethyl-N-nitro-1-pyrazole-1-carboxamidine (DMNPC), has been optimised. A detailed protocol for using this reagent for the preparation in pure form of a range of guanidines via nitroguanidines is described. A comparison has been made regarding efficiency between DMNPC and the guanidinylating reagents N,N′-bis-Boc-1-pyrazole-1-carboxamidine (2) and N,N′-bis-Boc- N′-triflylguanidine (3).
- Castillo-Melendez, Joel A.,Golding, Bernard T.
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p. 1655 - 1663
(2007/10/03)
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- Efficient introduction of protected guanidines in boc solid phase peptide synthesis.
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[reaction: see text] Reaction of primary amines with pyrazole 1 results in rapid and efficient guanidinylation, either in solution or on solid phase. The reaction affords sulfonamide-protected products required for BOC solid phase peptide synthesis (SPPS)
- Zhang,Kennan
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p. 2341 - 2344
(2007/10/03)
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- Transfection particles
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Transfection particles for delivery of nucleic acid into higher eucaryotic cells in vitroand in vivocomprises one or more nucleic acid molecules condensed by organic cationic molecules. The discrete and stable particles are obtained by complexing the nucleic acid molecules with identical or different organic cationic precursor molecules without crosslinking nucleic acid molecules, and covalently linking the precursor molecules to each other on the nucleic acid template. For specific cellular targeting, the particles may carry targeting molecules, e.g. sugars. Preferred cationic precursor molecules are lipophilic detergents that are linked to form lipids. The particles contain preferably only one nucleic acid molecule which makes them useful for gene therapy and for delivery of large DNA molecules.
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- An efficient method for the preparation of ω,ω'-bis-urethane protected arginine derivatives
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Fmoc-Arg(ω,w')(Boc)2-OH and Boc-Arg(ω,w')(Cbz)2-OH were prepared in two steps: Guanylation of Cu(II)-ornithine complex at N(δ) with N,N'-bis urethane protected derivatives of 1-guanylpyrazole, followed by N(α)-protection using either 9-fluorenylmethyl succinimidylcarbonate or di-t-butyl-dicarbonate in the presence of EDTA. The overall yields of these products (2 steps) were 65% and 73%.
- Wu,Matsueda,Bernatowicz
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p. 3055 - 3060
(2007/10/02)
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- Urethane protected derivatives of 1-guanylpyrazole for the mild and efficient preparation of guanidines
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Bis-urethane protected derivatives of 1-guanylpyrazole were prepared and found to readily react with relatively amines at room temperature to produce bis-protected guanidines in good yields. Simultaneous removal of both protecting groups from these products efficiently produced monosubstituted guanadines.
- Bernatowicz, Michael S.,Wu, Youling,Matsueda, Gary R.
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p. 3389 - 3392
(2007/10/02)
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