15937-30-1Relevant articles and documents
Novel pyridobenzimidazole derivatives exhibiting antifungal activity by the inhibition of β-1,6-glucan synthesis
Takeshita, Hiroshi,Watanabe, Jun,Kimura, Yoichi,Kawakami, Katsuhiro,Takahashi, Hisashi,Takemura, Makoto,Kitamura, Akihiro,Someya, Kazuhiko,Nakajima, Ryohei
scheme or table, p. 3893 - 3896 (2010/09/03)
Based on the HTS hit compound 1a, an inhibitor of β-1,6-glucan synthesis, we synthesized novel pyridobenzimidazole derivatives and evaluated their antifungal activity. Among the compounds synthesized, we identified the potent compound 15e, which exhibits
Alkylation of α-Formyl Esters via Their Thallium(I) Salts
Stratford, Eugene S.,Curley, Robert W.
, p. 2576 - 2579 (2007/10/02)
Treatment of the thallium(I) salt of β-diketones and β-keto esters with alkyl halides had been shown to be a useful method for the regioselective C-alkylation of these compounds.This approach,however,has apparently not been examined for α-formyl esters.In an effort to determine the applicability of this method to aldehyde substrates,the reaction with α-formyl esters which covers a range of properties for α-substituents has been examined.In addition,the effects of various solvents and Et3N catalysis on the course of the reaction were evaluated.The overall yields and ratios of C/O alkylation were determined by using 1H NMR integration.In no case did exclusive C-alkylation result and,furthermore,the results obtained indicate that previous explanations for the observed regioselectivity may not have been accurate and the preference for C-alkylation may be related to the covalent nature of the thallium salt in solution as opposed to reaction on the crystal surface.It is concluded that this method represents a useful synthetic procedure only for cases where the α-formyl ester has a relatively low enolization tendency and the steric demand of the electrophile is small.
