Design and Synthesis of a Conformationally Rigid Mimic of the Dihydropyrimidine Calcium Channel Modulator SQ 32,926

Abstract

Abstract:A conformationally rigid polyheterocycle (3) which mimics the putative receptorbound conformation of dihydropyridine-type calcium channel modulators is prepared in a seven-step reaction sequence based on a Biginelli-type cyclocondensation reaction.

Versatile Synthesis of Isoquinolines and Isochromenes by Pd‐Catalyzed Oxidative Carbonylation of (2‐Alkynyl)benzylideneamine Derivatives

“…Preparation of 2-Bromo-5-nitrobenzaldehyde: [13] To a stirred, cooled (5-10°C) mixture of fuming HNO 3 (4.5 mL) and concentrated H 2 SO 4 (34 mL), was added dropwise 2-bromobenzaldehyde (10.0 g, 54.1 mmol). The resulting mixture was warmed to room temp.…”

Design, synthesis and biological evaluation of new Mannich products using ethyl ammonium nitrate as reusable ionic liquid

“…As compared to other ionic liquids, ethylammonium nitrate (EAN) with acidic properties (pH=5) is cheap, easily recoverable and reusable at room temperature. Literature survey also reveals that derivatives of hydroxybenzophenone and derivatives of dihydrobenzofuran/benzofuran are used as u. v. absorber in such reactions [23][24][25][26][27][28][29] and halo derivatives of heterocyclic compounds show very good biological activities [30][31][32][33][34][35].…”

Synthesis and Biological Studies of Novel Biphenyl-3,5-dihydro-2H-thiazolopyrimidines Derivatives

“…The 3,4-dihydropyrimidin-2(1H)-ones have recently emerged as important target molecules due to their therapeutic and pharmacological properties 13 such as antiviral, 14 antimitotic, 15 anticarcinogenic, 16 antihypertensive 17,18 and noteworthy, as calcium channel modulators. 19,20 Additionally, their particular structure has been found in natural marine alkaloid batzelladine A and B which are the first low molecular weight natural products reported in the literature to inhibit the binding of HIV gp-120 to CD4 cells, so disclosing a new field towards the development of AIDS therapy. 21 Thiazoles and their derivatives are also found to be associated with various biological activities such as antibacterial, antifungal and anti-inflammatory.…”