104568-72-1Relevant academic research and scientific papers
Visible-light-induced formal [3+2] cycloaddition for pyrrole synthesis under metal-free conditions
Xuan, Jun,Xia, Xu-Dong,Zeng, Ting-Ting,Feng, Zhu-Jia,Chen, Jia-Rong,Lu, Liang-Qiu,Xiao, Wen-Jing
, p. 5653 - 5656 (2014/06/10)
A photocatalytic formal [3+2] cycloaddition of 2H-azirines with alkynes has been achieved under irradiation by visible light in the presence of organic dye photocatalysts. This transformation provides efficient access to highly functionalized pyrroles in good yields and has been applied to the synthesis of drug analogues. A primary trial of photocascade catalysis merging energy transfer and redox neutral reactions was shown to be successful. Photo(chemistry) op: A photocatalytic formal [3+2] cycloaddition of 2H-azirines with alkynes has been established under the irradiation of visible light in the presence of an organic dye. This transformation provides efficient access to highly functionalized pyrroles in good yields and has been applied to the formal synthesis of an inhibitor for HMG-CoA reductase.
Inhibitors of Cholesterol Biosynthesis. 3. Tetrahydro-4-hydroxy-6--2H-pyran-2-one Inhibitors of HMG-CoA Reductase. 2. Effects of Introducing Substituents at Positions Three and Four of the Pyrrole Nucleus
Roth, B. D.,Blankley, C. J.,Chucholowski, A. W.,Ferguson, E.,Hoefle, M. L.,et al.
, p. 357 - 366 (2007/10/02)
A series of trans-tetrahydro-4-hydroxy-6--2H-pyran-2 ones and their dihydroxy acids were prepared and tested for their ability to inhibit the enzyme HMG-CoA reductase in vitro.Inhibitory potency was found to increase subtantially when substituents were introduced into positions three and four of the pyrrole ring.A systematic exploration of structure-activity relationships at these two positions led to the identification of a compound ((+)-33, (+)-(4R)-trans-2-(4-fluorophenyl)-5-(1-methylethyl)-N,3-diphenyl-1- -1H-pyrrole-4-carboxamide) with five times the inhibitory potency of the fungal metabolite compactin.
