Zr-Catalyzed Kinetic Resolution of Allylic Ethers and Mo-Catalyzed Chromene Formation in Synthesis. Enantioselective Total Synthesis of the Antihypertensive Agent (S,R,R,R)-Nebivolol

Abstract

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A New Strategy for the Aminolysis of Epoxides with Amines Under Solventfree Conditions Using Fe-Mcm-41 as a Novel and Efficient Catalyst

“…So, the challenge was to replace them by solid MCM-41, which are easier to separate from the products, and possess reusability, high acid strength, hydrophilic and hydrophobic properties. Iron catalyst supported on MCM-41 substrate was synthesized via a MOCVD technique by using ferric acetylacetonate [Fe(acac) 3 ] and MCM-41 as iron source precursor and target substrate, respectively. A total of 0.25 g Fe(acac) 3 Scheme 1 Fig.…”

“…They can also serve as good chiral ligands of some asymmetric metal complex catalysts [1]. Among them, reaction of epoxide with amines is particularly interesting, because it leads to the formation of b-aminoalcohols which are intermediates in the synthesis of biologically active natural and synthetic products, pharmaceuticals synthetic amino acids and pesticides [2][3][4][5]. They are also used as blockers, insecticidal agents and as chiral ligands in asymmetric synthesis [2].…”

Stereochemical comparison of nebivolol with other β‐blockers

“…The (1)-enantiomer shows b 1 -blocking activity and the (2)-enantiomer acts as a vasodilator. [13][14][15][16][17] Vasodilation may be achieved by NO release, as indicated by studies in animal models and in humans, with possible mechanisms including an increase in NO synthase and stimulation of P2Y-purinoceptor-mediated NO release. 18 Consideration of stereochemical properties and the application of modern analytic methods delivers deeper insights into the antihypertensive profile of nebivolol.…”

Zn(OAc)2/podand catalyzed ring opening of epoxides by aromatic amines under solvent-free conditions

“…Several clinically usefull skeletones, which exhibit a broad range of biological activities as anti-obesity [2] and anti-hypertensives [3], contains the -amino alcohol functionality. The classical method for the preparation of -amino alcohol involves heating of an epoxide in a protic solvent with excess amine.…”