The synthesis of 3-(1H-imidazol-1-yl)-4H-1-benzopyran-4-ones 2 and of 2-(1H-imidazol-1-yl)-4H-1-benzopyr-an-4-ones 11 are described. The former proceeds through chromanring closure from 2-(1H-imidazol-1-yl)-2′-hydroxyacetophenones, the latter occurs reacting 3-bromo-4H-1-benzopyran-4-ones with imidazole and represents an example of a new synthesis of 2-heteroarylchromones. Compounds 2 can be easily
3-(1 H-咪唑-1-基)-4 H -1-苯并吡喃-4-酮2和2-(1 H-咪唑-1-基)-4 H -1-苯并吡喃-an的合成-4-一11被描述。前者通过2-(1 H-咪唑-1-基)-2'-羟基苯乙酮的苯并二氢吡喃环封闭而进行,后者发生的是使3-溴-4 H -1-苯并吡喃-4-酮与咪唑反应,这是一个例子。 2-杂芳基色酮的新合成方法。化合物2可以很容易地还原为先前在第1部分中描述的相应的苯并二氢吡喃酮和苯并二氢吡喃醇。
N-[2-4-(1H-Imidazol-1-yl)alkyl]-arylamides and pharmaceutical
申请人:American Cyanamid Company
公开号:US04568687A1
公开(公告)日:1986-02-04
This disclosure describes novel N-[.omega.-(1H-imidazol-1-yl)alkyl]arylamides which possess the property of inhibiting the enzyme thromboxane synthetase and are also useful in the treatment of hypertension and myocardial ischemia.
structure--activity relationships of imidazolederivatives as inhibitors of thromboxane (TX) synthetase were investigated. Introduction of various substituents (e.g., one or two methyl groups, a halogen atom, a methylidene group, unsaturated bonds, or a phenylene group) into the alpha position or other positions in the carboxy-bearing side chain of 1-(7-carboxyheptyl)imidazole (15) was found to increase the
Synthesis and Characterization of <i>cyclo</i>-Pentazolate Salts of NH<sub>4</sub><sup>+</sup>, NH<sub>3</sub>OH<sup>+</sup>, N<sub>2</sub>H<sub>5</sub><sup>+</sup>, C(NH<sub>2</sub>)<sub>3</sub><sup>+</sup>, and N(CH<sub>3</sub>)<sub>4</sub><sup>+</sup>
(N5)6(H3O)3(NH4)4Cl in which the cyclo-pentazolate anions were stabilized extensively by hydrogen bridges with the NH4+ and OH3+ cations. Significant efforts have been carried out to replace these nonenergetic cations and the Cl- anion by more energetic cations. In this paper, the metathetical syntheses of cyclo-pentazolate salts containing the simple nitrogen-rich cations NH4+, NH3OH+, N2H5+, C(NH2)3+, and