- Synthesis and anti-influenza evaluation of polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives.
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Polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives on a poly-L-glutamine backbone are described. Aiming for a longer retention time of 4-guanidino-Neu5Ac2en (zanamivir) in bronchi and lungs, we focused on supermolecules bearing 4-gu
- Masuda, Takeshi,Yoshida, Shuku,Arai, Masami,Kaneko, Satoru,Yamashita, Makoto,Honda, Takeshi
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- METHOD FOR PRODUCING NEURAMINIC ACID DERIVATIVE
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The present invention provides methods for manufacturing neuraminic acid derivatives. [Means for solution] Methods for manufacturing compounds represented by the formula (I) : [wherein R1 represents a C1-C19 alkyl group], or a pharmacologically acceptable salt thereof, using N-acetylneuraminic acid dihydrate as a starting raw material are provided.
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- Organocatalytic and scalable synthesis of the anti-influenza drugs zanamivir, laninamivir, and CS-8958
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Zanamivir, laninamivir, and CS-8958 are three neuraminidase inhibitors that have been clinically used to combat influenza. We report herein a novel organocatalytic route for preparing these agents. Only 13 steps are needed for the assembly of zanamivir and laninamivir from inexpensive d-araboascorbic acid by this synthetic route, which relies heavily on a thiourea-catalyzed enantioselective Michael addition of acetone to tert-butyl (2-nitrovinyl)carbamate and an anti-selective Henry reaction of the resulting Michael adduct with an aldehyde prepared from d-araboascorbic acid. The synthetic procedures are scalable, as evident from the preparation of more than 3.5 g of zanamivir.
- Tian, Junshan,Zhong, Jiankang,Li, Yunsheng,Ma, Dawei
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p. 13885 - 13888
(2015/04/16)
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- DRUG FOR TREATMENT OF INFLUENZA
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A therapeutic or prophylactic for H5N1 influenza is provided. Specifically disclosed is a therapeutic or prophylactic for H5N1 influenza comprising as an active ingredient a compound represented by the general formula (I): wherein R1 and R2 represent H or alkanoyl; X represents a halogen atom, OH, alkoxy or alkanoyloxy; and R3 represents H or alkyl; PROVIDED THAT compounds of formula (I) wherein each of R1 and R2 is H, X is OH, and R3 is H are excluded.
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Page/Page column 9
(2009/12/07)
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- METHOD FOR MANUFACTURING NEURAMINIC ACID DERIVATIVES
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A method for manufacturing neuraminic acid derivatives is provided, also synthetic intermediates of the neuraminic acid derivatives and methods for their manufacture, and neuraminic acid derivatives having high purity. [Means for solution] A synthetic intermediate compound represented by the formula (7) is provided: [wherein R3 represents alkyl; R4 and R5 each represents H, alkyl, phenyl, or together represent tetramethylene, pentamethylene, oxo].
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Page/Page column 77
(2008/12/08)
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