40053-33-6Relevant academic research and scientific papers
Anti-AIDS agents. Part 58: Synthesis and anti-HIV activity of 1-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (1-thia-DCK) analogues
Xia, Peng,Yin, Zhi-Jian,Chen, Ying,Zhang, Qian,Zhang, Beina,Xia, Yi,Yang, Zheng-Yu,Kilgore, Nicole,Wild, Carl,Morris-Natschke, Susan L.,Lee, Kuo-Hsiung
, p. 3341 - 3343 (2007/10/03)
Two 1-thia-DCK analogues (9a and 9b) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. Compound 9a showed excellent anti-HIV activity with an EC50 value of 0.00012μM and therapeutic index of 1,408,000. Compou
Synthesis of 2H-1-Benzothiopyran-2-ones (Thiocoumarins) and Related Compounds from Benzenethiols and Diketene
Nakazumi, Hiroyuki,Asada, Akira,Kitao, Teijiro
, p. 2046 - 2049 (2007/10/02)
The products formed by the reaction of benzenethiols with diketene in the presence of H2SO4 are (E)-β-(arylthio)crotonic acids (2) and/or isomeric (Z)-β-(arylthio)crotonic acids and not, as has been reported, S-phenyl-3-oxobutanethioates (1).Compounds 1a-k, as the precursor of thiocoumarins, were prepared from benzenethiols and diketene in the presence of triethylamine.The reaction of 1 with various condensing agents has been examined to prepare 2H-1-benzothiopyran-2-ones (thiocoumarins).It is found that 4-methyl(thiocoumarins) were conveniently prepared by thereaction of 1 with anhydrous aluminium chloride in yields of 16-48percent.When 1 was treated with PPA, isomeric 2-methyl(thiochromones) were preferentially obtained in yields of 5-66percent, and compound 2 was isolated as an intermediate.The spectral characteristics of 4-methyl(thiocoumarins) have also been described.
