197516-57-7Relevant articles and documents
Pyridine derivative, composition thereof and application of pyridine derivative and composition as anti-influenza virus drug
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Paragraph 0127-0129, (2019/08/02)
The invention belongs to the antiviral field of medical chemistry and relates to a novel pyridine derivative shown in a formula (I), a stereisomer, pharmaceutical salt, a solvent compound or a crystalof the pyridine derivative and an application of the pyridine derivative and the stereisomer, pharmaceutical salt, the solvent compound or the crystal in preparing drugs for preventing or treating viral infection diseases such as influenza A and/or influenza B, particularly in preparing a cap dependent endonuclease inhibitor in preventing or treating influenza A and/or influenza B viral infectiondiseases. The compound has remarkable activity for inhibiting influenza endonuclease and influenza DNA, can be independently used or can be combined with a neuraminidase inhibitor, nucleoside medicines, a PB2 inhibitor, a PB1 inhibitor, an M2 inhibitor or other anti-influenza drugs, the influenza infection time is notably shortened, the death rate is remarkably reduced, and the pyridine derivative has very good clinical application prospects.
Regioselectivity of the Base-Induced Ring Cleavage of 1-Oxygenated Derivatives of Cyclobutabenzene
Gokhale, Abha,Schiess, Peter
, p. 251 - 267 (2007/10/03)
Oxy anions 3 generated from 1,2-dihydrocyclobutabenzen-1-ones 1 through addition of a charged nucleophile or from 1-hydroxy-1,2-dihydrocyclobutabenzenes 2 by deprotonation with base lead to stable products through distal and/or proximal cleavage of the strained four-membered ring via benzyl carbanion 4 and/or aryl carbanion 5. A systematic study of this process reveals the relative stability of the two isomeric carbanions 4 and 5 as a key factor in determining the course of the ring-cleavage reaction. While benzyl carbanions 4 can be trapped with carbon electrophiles, attempts at trapping aryl carbanions 5 with electrophiles other than H+ failed. In protic solvents, the magnesium salt of the tertiary alcohol 2 shows an increased rate of proximal cleavage as compared to its alkali salts. From this, we conclude that, in contrast to benzyl carbanions 4, free aryl carbanions 5 are of transient existence only. Proximal C,C-bond cleavage seems to occur either through protonation of 5 from a fast, reversible equilibrium 3?5 in which 3 strongly predominates, or in protic solvents possibly even through a rate-limiting protonation of 3 at the aromatic C-atom, bypassing free anion 5 altogether. Thus, additional factors other than just the relative stability of isomeric carbanions 4 and 5 are of importance in determining the regiochemistry of the base-induced C,C-bond cleavage in ketones 1 and in alcohols 2.
