Recent Developments in the Synthetic Uses of Silyl-protected Enoldiazoacetates for Heterocyclic Syntheses

2014 ◽  
Vol 67 (3) ◽  
pp. 365 ◽  
Author(s):  
Xinfang Xu ◽  
Michael P. Doyle
Keyword(s):  
Heterocyclic Compounds ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Diazo Compounds ◽  
Cycloaddition Reactions ◽  
Insertion Reactions ◽  
Active Compounds ◽  
The Core ◽  
Recent Developments ◽  
Metal Catalyzed

Diazo compounds have been used as precursors to a wide variety of heterocyclic compounds that represent the core structural subunits in many biologically active compounds. Various methodologies have been established for their synthesis via metal-catalyzed carbene transformations. Although the advantages of vinyldiazoacetates have been known for many years, realization of the synthetic use of enoldiazoacetates has been more recent. This review covers advances in the utility of silyl-protected enoldiazoacetates in heterocycle syntheses that include X–H insertion reactions, ylide rearrangements, formal [3+3]- and [4+3]-cycloaddition reactions, and other traditional and unusual metal carbene transformations.

scholarly journals 2,3-Dihydroquinazolin-4(1H)-one as a privileged scaffold in drug design

RSC Advances ◽  
2018 ◽  
Vol 8 (37) ◽  
pp. 20894-20921 ◽  
Author(s):  
Mariateresa Badolato ◽  
Francesca Aiello ◽  
Nouri Neamati
Keyword(s):  
Drug Design ◽  
Structural Component ◽  
Heterocyclic Compounds ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Privileged Scaffold

2,3-Dihydroquinazolin-4-one (DHQ) belongs to the class of nitrogen-containing heterocyclic compounds representing a core structural component in various biologically active compounds.

Recent advances in the catalytic synthesis of 3-aminooxindoles: an update

2020 ◽  
Vol 18 (25) ◽  
pp. 4692-4708 ◽  
Author(s):  
Jasneet Kaur ◽  
Banni Preet Kaur ◽  
Swapandeep Singh Chimni
Keyword(s):  
Natural Products ◽  
Catalytic Synthesis ◽  
Biologically Active Compounds ◽  
Core Structure ◽  
Biologically Active ◽  
Active Compounds ◽  
The Core ◽  
Recent Advances

3-Substituted-3-aminooxindoles are versatile scaffolds and these motifs constitute the core structure of number of natural products and biologically active compounds.

Electrophile Promoted Cyclization of ortho-Aryl Substituted Ynamides: Construction of 3-Amino-4-Halo- or 4-Seleno-Isocoumarin Derivatives

2021 ◽  
Author(s):  
Isabelle Gillaizeau ◽  
Loic Habert ◽  
Iryna Diachenko ◽  
Pascal Retailleau
Keyword(s):  
Medicinal Chemistry ◽  
Building Blocks ◽  
Biologically Active Compounds ◽  
Core Structure ◽  
Biologically Active ◽  
Active Compounds ◽  
The Core

Isocoumarins are important building blocks in medicinal chemistry. They are widespread in the core structure of biologically active compounds. Here we report the development of an efficient and highly reactive...

scholarly journals Recent Advances on Quinazoline Derivatives: A Potential Bioactive Scaffold in Medicinal Chemistry

2021 ◽  
Vol 5 (4) ◽  
pp. 73
Author(s):  
Ram Karan ◽  
Pooja Agarwal ◽  
Mukty Sinha ◽  
Neelima Mahato
Keyword(s):  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Diverse Range ◽  
Important Group ◽  
Quinazoline Derivatives

This paper intended to explore and discover recent therapeutic agents in the area of medicinal chemistry for the treatment of various diseases. Heterocyclic compounds represent an important group of biologically active compounds. In the last few years, heterocyclic compounds having quinazoline moiety have drawn immense attention owing to their significant biological activities. A diverse range of molecules having quinazoline moiety are reported to show a broad range of medicinal activities like antifungal, antiviral, antidiabetic, anticancer, anti-inflammatory, antibacterial, antioxidant and other activities. This study accelerates the designing process to generate a greater number of biologically active candidates.

Nickel(0)-Catalyzed Linear-Selective Hydroarylation of Unactivated Alkenes and Styrenes with Arylboron Acids

2018 ◽  
Author(s):  
Honggui Lv ◽  
Li-Jun Xiao ◽  
Dongbing Zhao ◽  
Qi-Lin Zhou
Keyword(s):  
Butyric Acid ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Highly Efficient ◽  
Organoboronic Acids

Herein, we realized the first linear-selective hydroarylation of unactivated alkenes and styrenes with organoboronic acids by introducing directing groupon alkenes. Our method is highly efficient and scalable, and provides a modular route to assemble structurally diverse alkylarenes, especially for γ-aryl butyric acid derivatives, which have been widely utilized as chemical feedstocks to access multiple marketed drugs, and biologically active compounds.<br>

SOME DIRECTIONS IN THE MODIFICATION OF AZOLES

2020 ◽  
Vol 5 (443) ◽  
pp. 85-91
Author(s):  
Ibrayev M.K., ◽  
◽  
Takibayeva A.T., ◽  
Fazylov S.D., ◽  
Rakhimberlinova Zh.B., ◽  
...  
Keyword(s):  
13C Nmr Spectroscopy ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Synthesis Conditions ◽  
Alkaloid Cytisine ◽  
Azole Ring ◽  
Cyclic Compounds ◽  
New Compounds ◽  
Derivatives Of

This article presents studies on the targeted search for new derivatives of azoles, such as benzthiazole, 3,5-dimethylpyrazole, 1,3,4-oxadiazole-2-thione, 1,3,4-thiadiazole. The possibility of combining in one molecule of the azole ring with other cyclic compounds: the alkaloid cytisine, morpholine, furan and some arenes has been studied. To obtain new compounds, the reactions of bromination, acylation, and interaction with isothiocyanates were studied. Optimal synthesis conditions were studied for all reactions. It was found that the reaction of 4-bromo-3,5-dimethylpyrazole with isothiocyanates, in contrast to the previously written derivatives of anilines, takes a longer time and requires heating the reaction mixture. The combination of a pirasol fragment with halide substituents often results in an enhanced therapeutic effect. The synthesized 2-bromine-N-(6-rodanbenzo[d]thiazole-2-yl)acetamide, due to the alkylbromide group, is an important synth in the synthesis of new benzthiazole derivatives. Its derivatives combine in one molecule the rest of rhodanbenzthiazole with alkaloid cytisine and biogenic amine morpholine and are potentially biologically active compounds, since the molecule structure contains several pharmacophoric fragments: benzthiazole and alkaloid (amine) heterocycles, rhodane and urea groups. The mechanism of formation of 1,3,4-oxadiazole-2-tyons from hydrazides under action on them by carbon disulfide was studied and assumed. It was shown that dithiocarbamates in acidic medium decompose with the release of hydrogen sulfide and the formation of highly reactive isothiocyanate group. Then, intra-molecular cyclization occurs, with the formation of end products - 1,3,4-oxadiazole-2-thions. The structures of the synthesized compounds were studied by 1H and 13C NMR spectroscopy. All synthesized substances are potentially biologically active compounds, since they contain several pharmacophore fragments in their structure.

Sign in / Sign up

Export Citation Format

Share Document