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Unprecedented Multicomponent Organocatalytic Synthesis of Propargylic Esters via CO2 Activation
(Wiley‐VCH, 2019-02-19)
An efficient and straightforward organocatalytic method for the
direct, multicomponent carboxylation of terminal alkynes with
CO2 and organochlorides, towards propargylic esters, is reported
for the first time. ...
An umpolung strategy to react catalytic enols with nucleophiles
(Nature, 2019-11-20)
The selective synthesis of a-functionalized ketones with two similar enolizable positions can be accomplished using allylic alcohols and iridium(III) catalysts. A formal 1,3-hydrogen shift on allylic alcohols generates ...
Pd-catalyzed site-selective C(sp(2))-H radical acylation of phenylalanine containing peptides with aldehydes
(Royal Society of Chemistry, 2019-08-07)
The site-selective functionalization of C-H bonds within a peptide framework remains a challenging task of prime synthetic importance. Herein, the first Pd-catalyzed delta-C(sp(2))-H acylation of Phe containing peptides ...
Pd-catalyzed site-selective C(sp2)–H radical acylation of phenylalanine containing peptides with aldehydes
(Royal Society of Chemistry, 2019-10-14)
The site-selective functionalization of C-H bonds within a peptide framework remains a challenging task of prime synthetic importance. Herein, the first Pd-catalyzed delta-C(sp(2))-H acylation of Phe containing peptides ...
Synthesis of Heterocyclic Fused [1,5]naphthyridines by Intramolecular HDA Reactions
(MDPI, 2019-09-06)
Povarov reaction [1] can be considered as an example of HDA reactions and represents an
excellent method for the preparation of nitrogen-containing heterocyclic compounds [2]. When
aldimines, derived from aromatic amines ...
A Brønsted Acid-Catalyzed Multicomponent Reaction for the Synthesis of Highly Functionalized γ-Lactam Derivatives
(MDPI, 2019-08)
Bronsted acids catalyze a multicomponent reaction of benzaldehyde with amines and diethyl acetylenedicarboxylate to afford highly functionalized gamma-lactam derivatives. The reaction consists of a Mannich reaction of an ...
Design and Evaluation of New Phosphorus Substituted Aziridines as Antiproliferative Agents
(MDPI, 2019-08-09)
Covalent bond formation has become a safe and effective strategy applied not only by nature but also by the pharmaceutical industry to improve disease pharmacology. In the history of modern medicine, covalent drugs have ...
Synthesis of Indenes by the Tandem Gold(I)-Catalyzed Claisen Rearrangement/Hydroarylation Reaction of Propargyl Vinyl Ethers
(ACS, 2019-05-06)
The tandem gold(I)-catalyzed propargyl Claisen rearrangement/hydroarylation reaction of suitable propargyl vinyl ethers, followed by in situ reduction of the resulting carbonyl group, provides functionalized indenes in ...
Detrifluoroacetylative in Situ Generated Cyclic Fluorinated Enolatesfor the Preparation of Compounds Featuring a C−F StereogenicCenter
(American Chemical Society, 2019-11-26)
Practical methods for the preparation of selectively fluorinated compounds are in extremely high demand in nearly every sector of the pharmaceutical and agrochemical industries. Here we provided an account of the recent ...
Development of Hamari Ligands for Practical Asymmetric Synthesisof Tailor-Made Amino Acids
(American Chemical Society, 2019-11-19)
Enantiomerically pure tailor-made amino acids are in extremely high demand in nearly every sector of the health-related industries. In particular, the rapidly growing number of amino-acid-based pharmaceuticals calls for ...