Synthesis and antihypertensive activity of substituted trans-4-amino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3-ols
作者:John M. Evans、Charles S. Fake、Thomas C. Hamilton、Robert H. Poyser、Eric A. Watts
DOI:10.1021/jm00365a007
日期:1983.11
position. Exceptions to this were the 7-nitro-4-pyrrolidine analogue and the 6-nitro-3-chloropropylamine, which retained marked antihypertensiveactivity. All of these compounds were direct vasodilators and had comparable antihypertensiveactivity to hydralazine and to the calcium antagonist, nifedipine. The synthetic route to these compounds involves cyclization of of propargyl ethers to 2H-1-benzopyrans
Copper(I) Iodide: A Catalyst for the Improved Synthesis of Aryl Propargyl Ethers
作者:David Bell、Mark R. Davies、Graham R. Geen、Inderjit S. Mann
DOI:10.1055/s-1995-3977
日期:1995.6
Copper(I) iodide catalyses the reaction between phenols and dialkylpropargyl chlorides to give aryl 1,1-dialkylpropargyl ethers 5a-k and 7a-e in good yields and purity. These ethers are important as precursors to the 2H-1-benzopyrans 8a-l and 9a-e.
The invention relates to certain cis and trans benzopyrans having substituted benzamides at position C-4 and to their use in treating and/or preventing certain CNS disorders.
Total Synthesis and Absolute Configuration Determination of the α-Glycosidase Inhibitor (3<i>S</i>,4<i>R</i>)-6-Acetyl-3-hydroxy-2,2-dimethylchroman-4-yl (<i>Z</i>)-2-Methylbut-2-enoate from <i>Ageratina grandifolia</i>
Herein, we report the first totalsynthesis of α-glycosidase inhibitor (3R, 4S)-6-acetyl-3-hydroxy-2,2-dimethylchroman-4-yl (Z)-2-methylbut-2-enoate as well as its enantiomer. Our synthesis confirms the chromane structure separately proposed by Navarro-Vazquez and Mata, on the basis of DFT computations. Furthermore, our synthesis allowed us to determine the absoluteconfiguration of the natural compound
在此,我们报道了α-糖苷酶抑制剂(3 R , 4 S )-6-乙酰基-3-羟基-2,2-二甲基苯并二氢吡喃-4-基( Z )-2-甲基丁-2-烯酸酯的首次全合成:及其对映体。我们的合成证实了 Navarro-Vazquez 和 Mata 在 DFT 计算的基础上分别提出的色烷结构。此外,我们的合成使我们能够确定天然化合物的绝对构型为 (3 S , 4 R ) 而不是 (3 R , 4 S )。
NOVEL COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT