211555-30-5Relevant articles and documents
A 5 (4H)-pyridone combines furazane oxide synthesis method
-
Paragraph 0037-0038, (2017/04/11)
The invention discloses a synthesis method of 4H-pyridofuroxan-5-one (III, also known as 4H, 5H-(1, 2, 5) oxadiazole (3, 4-b) pyridin-5-one-1-oxide). The synthesis method comprises the following steps (see the following reaction formula): enabling 2-amino-3-nitro-6-chloropyridine (I) to react with potassium (or sodium and the like) fluoride in a water-containing alcohol type solution, or enabling I to react with a nitrite in acetone to prepare 2-amino-3-nitro-6-hydroxypyridine (II); then performing oxidation and condensation reaction under alkaline conditions to prepare III. The synthesis process disclosed by the invention is simple and convenient to operate, and suitable for relatively large-scale production of III; a new way is provided for preparing anti-virus and anti-tumor compounds with the effect of releasing nitric oxide (NO).
Non-standard nucleoside analogs with reduced epimerization
-
, (2011/11/13)
This invention relates to nucleoside, nucleotide, and oligonucleotide analogs that incorporate non-standard nucleobase analogs, defined to be those that present a pattern of hydrogen bonds to a paired nucleobase analog in a complementary strand that is different from the pattern presented by adenine, guanine, cytosine, and thymine. The invention is specifically concerned with compositions of matter that present the donor-donor-acceptor, donor-acceptor-donor, and acceptor-donor-donor non-standard hydrogen bonding patterns on pyrimidine analogs, where nucleoside analogs bearing these pyrimidine analogs do not epimerize as easily as those known in the art. The heterocycles on these nucleoside analogs are diaminopyridines and aminopyridones that have electron withdrawing groups attached to the position analogous to the 5-position of the ring in standard pyrimidines, including nitro, cyano, and carboxylic acid derivatives.
Novel non-benzimidazole chk2 kinase inhibitors
McClure, Kelly J.,Huang, Liming,Arienti, Kristen L.,Axe, Frank U.,Brunmark, Anders,Blevitt, Jon,Guy Breitenbucher
, p. 1924 - 1928 (2007/10/03)
In a recent paper, [Arienti, K. L.; Brunmark, A.; Axe, F. U.; McClure, K. M.; Lee, A.; Blevitt, J.; Neff, D. K.; Huang, L.; Crawford, S.; Chennagiri, R. P.; Karlsson, L.; Brietenbucher, J. G. J. Med. Chem. 2005, 48, 1873], we described the discovery of a class of benzimidazole chk2 kinase inhibitors, exemplified by compound 1, which had radio-protective effects in human T-cells subjected to ionizing radiation. Here, a series of non-benzimidazole analogs intended to define the scope of the SAR about this new series of inhibitor, and allow for refinement of the binding model of these compounds to the chk2 kinase is described.