A simple and direct synthesis of functionalized imidazoles from α-nitro-epoxides and amidines was developed.
从α-硝基环氧化物和胺酰胺直接合成官能化咪唑的简单方法被开发出来。
Cycloadditions of Noncomplementary Substituted 1,2,3-Triazines
作者:Erin D. Anderson、Adam S. Duerfeldt、Kaicheng Zhu、Christopher M. Glinkerman、Dale L. Boger
DOI:10.1021/ol502436n
日期:2014.10.3
The scope of the [4 + 2] cycloadditionreactions of substituted 1,2,3-triazines, bearing noncomplementary substitution with electron-withdrawing groups at C4 and/or C6, is described. The studies define key electronic and stericeffects of substituents impacting the reactivity, mode (C4/N1 vs C5/N2), and regioselectivity of the cycloadditionreactions of 1,2,3-triazines with amidines, enamines, and
Compounds of formula (I) and formula (II) are disclosed which are useful in the treatment bacterial infections:
1
wherein:
R
1
is C
1-4
alkyl, Ar or 2-thienyl or 3-thienyl;
R
2
is C
1-4
alkyl or Ar; and
n is 0-3;
or a pharmaceutically acceptable salt thereof.