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Synthesis and Reactivity of Sulfur-Containing Compounds
Research Guide
What is Synthesis and Reactivity of Sulfur-Containing Compounds?
Synthesis and Reactivity of Sulfur-Containing Compounds is the study of chemical methods for preparing sulfur-bearing molecules such as thioamides and their participation in reactions including thionation and multicomponent processes.
This field encompasses 31,257 published works focused on thioamide preparation via thionation, Lawesson's reagent, and elemental sulfur. Key areas include organic synthesis of heterocycles, catalytic reactions, and microwave-assisted methods. Growth data over the past five years is not available.
Topic Hierarchy
Research Sub-Topics
Lawesson's Reagent Thionation
This sub-topic covers the use of Lawesson's reagent for efficient conversion of amides, esters, and carbonyls to thioamides and thiocarbonyls. Research optimizes reaction conditions and explores substrate scope.
Thioamide Synthesis Multicomponent Reactions
Focuses on multicomponent reactions (MCRs) incorporating thioamides for one-pot heterocycle formation, emphasizing efficiency and diversity. Studies develop catalytic variants for green synthesis.
Catalytic Thioamide Formation
Investigates metal-catalyzed or organocatalytic methods using elemental sulfur or thiols for chemoselective thioamide synthesis. Research addresses stereoselectivity and functional group tolerance.
Microwave-Assisted Thioamide Synthesis
Explores microwave irradiation to accelerate thionation reactions, improving yields and reducing reaction times for thioamides. Comparative studies with conventional heating highlight scalability.
Thioamides in Heterocycle Synthesis
Studies thioamides as building blocks in constructing thiophenes, thiazoles, and other sulfur heterocycles via cyclization. Includes applications in pharmaceuticals and agrochemicals.
Why It Matters
Sulfur-containing compounds like thioamides serve as intermediates in pharmaceutical synthesis, as demonstrated by Penning et al. (1997) who synthesized 4-[5-(4-Methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide (SC-58635, Celecoxib), a selective cyclooxygenase-2 inhibitor with 1939 citations. Gewald et al. (1966) developed a one-pot reaction of methylene-active nitriles, carbonyl compounds, and sulfur to produce 2-aminothiophenes, enabling heterocycle construction used in medicinal chemistry (770 citations). These methods support chemoselective transformations in drug discovery and materials science.
Reading Guide
Where to Start
"Synthesis and Biological Evaluation of the 1,5-Diarylpyrazole Class of Cyclooxygenase-2 Inhibitors: Identification of 4-[5-(4-Methylphenyl)-3- (trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide (SC-58635, Celecoxib)" by Penning et al. (1997), as it provides a practical entry to sulfur compound applications in medicinal chemistry with clear SAR data.
Key Papers Explained
Penning et al. (1997) detail sulfonamide pyrazole synthesis leading to Celecoxib, highlighting sulfur's role in COX-2 inhibition (1939 citations). Gewald et al. (1966) introduce a foundational sulfur-mediated heterocycle synthesis from nitriles and carbonyls (770 citations), which complements later phosphorous-sulfur work. Appel (1975) expands reactivity with tertiary phosphane/tetrachloromethane for chlorination and P-N linkages involving sulfur species (912 citations), building versatile synthetic tools.
Paper Timeline
Most-cited paper highlighted in red. Papers ordered chronologically.
Advanced Directions
Current work emphasizes catalytic multicomponent reactions and microwave-assisted thionation, per the 31,257-paper cluster on thioamides and heterocycles. No recent preprints or news specify new frontiers.
Papers at a Glance
| # | Paper | Year | Venue | Citations | Open Access |
|---|---|---|---|---|---|
| 1 | Synthesis and Biological Evaluation of the 1,5-Diarylpyrazole ... | 1997 | Journal of Medicinal C... | 1.9K | ✓ |
| 2 | PYRUVIC ACID | 1943 | Journal of Biological ... | 1.9K | ✓ |
| 3 | Esters of Methanesulfonic Acid as Irreversible Inhibitors of A... | 1962 | Journal of Biological ... | 1.5K | ✓ |
| 4 | Osteoarthritis: New Insights | 2002 | Annals of Internal Med... | 1.1K | ✕ |
| 5 | BIOLOGICAL ACTIVITY OF AMINOPHOSPHONIC ACIDS | 1991 | Phosphorus, sulfur, an... | 974 | ✕ |
| 6 | Tertiary Phosphane/Tetrachloromethane, a Versatile Reagent for... | 1975 | Angewandte Chemie Inte... | 912 | ✕ |
| 7 | Heterocyclen aus CH‐aciden Nitrilen, VIII. 2‐Amino‐thiophene a... | 1966 | Chemische Berichte | 770 | ✕ |
| 8 | Aziridines and Epoxides in Organic Synthesis | 2006 | — | 710 | ✕ |
| 9 | Dynamical theory of crystal lattices | 1955 | Journal of the Mechani... | 689 | ✕ |
| 10 | Aminophosphonic and aminophosphinic acids : chemistry and biol... | 2000 | Wiley eBooks | 663 | ✕ |
Frequently Asked Questions
What role does Lawesson's reagent play in thioamide synthesis?
Lawesson's reagent converts amides to thioamides through thionation. It features in multicomponent reactions for heterocycle formation. The cluster highlights its use alongside elemental sulfur in organic synthesis.
How are 2-aminothiophenes synthesized?
Gewald et al. (1966) reported that aliphatic ketones, aldehydes, or β-dicarbonyl compounds react with methylene-active nitriles and sulfur in the presence of amines at room temperature to form 2-aminothiophenes. A variant involves sulfur acting on vinylogous methylene-active nitriles. This method yields heterocycles central to the field.
What are common applications of sulfur-containing compounds?
They function as cyclooxygenase-2 inhibitors in drugs like Celecoxib, per Penning et al. (1997). Thioamides appear in heterocycle synthesis for pharmaceuticals. Catalytic and multicomponent reactions expand their utility in organic chemistry.
What is thionation in this context?
Thionation replaces oxygen with sulfur in carbonyl compounds to produce thioamides. Reagents like Lawesson's reagent or elemental sulfur enable this. It supports chemoselective synthesis of reactive sulfur heterocycles.
How many papers address this topic?
The field includes 31,257 works on synthesis and reactivity. Coverage spans thioamides, heterocycles, and catalytic reactions. No five-year growth rate is reported.
Open Research Questions
- ? How can thionation reactions achieve higher chemoselectivity in complex molecule synthesis?
- ? What catalytic systems improve multicomponent reactions involving elemental sulfur and nitriles?
- ? Which sulfur reagents beyond Lawesson's enable mild-condition thioamide formation?
- ? How do sulfur-containing heterocycles influence biological activity in drug scaffolds?
Recent Trends
The field maintains 31,257 works with no reported five-year growth rate.
Emphasis persists on thionation via Lawesson's reagent and elemental sulfur, as in Gewald et al.
1966No recent preprints or news indicate shifts.
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