Search
Now showing items 91-100 of 135
Microwave-assisted Palladium catalysed C-H acylation with aldehydes. Synthesis and diversification of 3-acylthiophenes
(Royal Society of Chemistry, 2021-12-22)
The use of MW allows the efficient palladium(II)-catalysed C-3 acylation of thiophenes with aldehydes via C(sp2)-H activation for the synthesis of (cyclo)alkyl/aryl thienyl ketones (43 examples). Compared to standard thermal ...
Palladium-catalysed Heck-type alkenylation reactions in the synthesis of quinolines. Mechanistic insights and recent applications
(Royal Society of Chemistry, 2020-05-18)
Quinoline and quinolone cores are present in a wide variety of pharmaceuticals, agrochemicals and materials, as well in ligands/catalysts in asymmetric synthesis. Transition-metal catalysed based approaches have played a ...
Transannular Approach to 2,3-Dihydropyrrolo[1,2‑b]isoquinolin- 5(1H)‑ones through Brønsted Acid-Catalyzed Amidohalogenation
(ACS. American Chemical Society, 2022-07-26)
A transannular approach has been developed for the construction of pyrrolo[1,2-b]isoquinolinones starting from benzofused nine-membered enelactams. This process takes place in the presence of a halogenating agent and under ...
Enantioselective construction of the 8-azabicyclo[3.2.1]octane scaffold: application in the synthesis of tropane alkaloids
(Royal Society of Chemistry, 2021-03-15)
The 8-azabicyclo[3.2.1]octane scaffold is the central core of the family of tropane alkaloids, which display a wide array of interesting biological activities. As a consequence, research directed towards the preparation ...
An Approach to the Synthesis of a Hepatitis C Virus Inhibitor through a Proline-Catalyzed 1,3-Dipolar Cycloaddition Using Acrolein
(Thieme, 2021-09-06)
An efficient and easy protocol for performing 1,3-dipolar cycloaddition using azomethine ylides and acrolein is presented. The reaction catalyzed by d-proline allows the synthesis of C-3 unsubstituted pyrrolidines. The ...
Recent Developments in Transannular Reactions
(Thieme, 2022-07-21)
Transannular reactions have shown a remarkable performance for the construction of polycyclic scaffolds from medium- or large-sized cyclic molecules in an unconventional manner. Recent examples of transannular reactions ...
Prediction of Antileishmanial Compounds: General Model, Preparation, and Evaluation of 2‑Acylpyrrole Derivatives
(ACS, 2022-08-10)
In this work, the SOFT.PTML tool has been used to pre-process a
ChEMBL dataset of pre-clinical assays of antileishmanial compound candidates.
A comparative study of different ML algorithms, such as logistic regression
(LOGR), ...
Directed C- H Allylation of Aromatic Carboxamides with Allyl Aryl Ethers under Cp*Co(III)-Catalysis
(Wiley-VCH, 2023-11-20)
The Cp*Co(III) C−H allylation of (hetero)arenes with allyl aryl ethers has been developed using an amide as directing group (24 examples). DFT calculations have shed light on the mechanistic course and reactivity pattern, ...
Palladium-mediated synthesis and biological evaluation of C-10b substituted Dihydropyrrolo[1,2-b]isoquinolines as antileishmanial agents
(Elsevier, 2021-04-16)
The development of new molecules for the treatment of leishmaniasis is, a neglected parasitic disease, is
urgent as current anti-leishmanial therapeutics are hampered by drug toxicity and resistance. The pyrrolo[
1,2-b ...
MATEO: intermolecular α-amidoalkylation theoretical enantioselectivity optimization. Online tool for selection and design of chiral catalysts and products
(BMC, 2024-01-23)
The enantioselective Brønsted acid-catalyzed α-amidoalkylation reaction is a useful procedure is for the production
of new drugs and natural products. In this context, Chiral Phosphoric Acid (CPA) catalysts are versatile ...