Dihydropyrazolopyrimidines containing benzimidazoles as KV1.5 potassium channel antagonists

Diastereoselective intramolecular aldol ring closures of threonine derivatives leading to densely functionalised pyroglutamates related to oxazolomycin

“…17 Starting from substituted acetyl chlorides 4a-d, conversion to the corresponding acylated Meldrum's acids 5a-d proceeded in excellent yield (Scheme 2) using methodology which has recently been reported. 18 Further collapse of this system with t-butanol was very efficient, giving esters 6a-d. In order to demonstrate that such intermediates could be used to perform the desired ring closing aldol reaction, one of them (6a) was hydrolysed to acid 7 and converted to malonamide 8 by DCC coupling with oxazolidine 1.…”

Dihydroazolopyrimidine Сrownophanes. Synthesis and Tuberculostatic Activity

“…[3,4] Среди дигидропиразоло[1,5-a] пиримидинов обнаружен ряд эффективных модулято-ров Ca-и K-каналов. [5][6][7][8][9][10] Триазоло[1,5-a]пиримидины оказались перспективными антагонистами аденозин A 2A рецептора при лечении болезни Паркинсона. [11] Не-которые дигидротриазоло [1,5-a]пиримидины проявили антиконвульсантную на уровне Карбамазепина [12] и анти-пролиферативную [13] клеточную активность.…”

“…-дибензо [13,14:8,9] [1,4,7]триоксацикло-тетрадецино [11,10-e]азоло [1,5-a] Azolo [1,5-a]pyrimidines are considered to be purine analogues and they form one of the most promising groups of biologically active compounds [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16] in medicinal chemistry. One of the strategies enhancing biochemical activity of azolo [1,5-a]pyrimidines is introduction of functional groups responsible for solubility and transport into their pharmacophore nucleus.…”

The Biginelli Reaction Is a Urea-Catalyzed Organocatalytic Multicomponent Reaction

“…[31][32][33][34][35][36][37][38][39] Discovered at first in 1893, 19,20 this reaction results in the condensation of three components: a urea, an aldehyde and a β-keto ester to form the 4-aryl-3,4-dihydropyrimidin-2(1H)-one (DHP) as shown in Scheme 1. …”