93196-73-7

Upstream product

• 75-15-0 carbon disulfide 
• 2129-20-6 bis(dimethylamino)sulfide 
• 128-04-1 sodium dimethyldithiocarbamate 
• 60-29-7 diethyl ether 
• 598-64-1 dimethylammonium dimethyldithiocarbamate 
• 98-09-9 benzenesulfonyl chloride 
• 14548-16-4 Dimethyl-(1-phenyl-vinyl)-amine 
• 16601-12-0 S-(4-toluenesulfonyl) 4-toluenethiosulfonate 
• 506-59-2 N,N-dimethylammonium chloride 
• 74109-49-2 Ditetraethylammoniumperthiodicarbonat 
• 84402-28-8 O-benzoyl-2,3-dibromo-2-methylpropanal oxime 
• 79-45-8 N,N-dimethyldithiocarbamic acid 
• 200336-83-0 2,3-dimethylbut-2-en-1-yl dimethyltrithiopercarbamate 
• 51-82-1 dimethyl-dithiocarbamic acid dimethylaminomethyl ester 

Downstream Products

• 23839-29-4 2-(dimethylaminothiocarbonylthio)cyclohexanone 
• 55436-15-2 2,6-Di-(dimethylamino-thiocarbonylmercapto)-cyclohexanon 
• 17709-95-4 N,N-dimethyl-2-phenylethanethioamide 
• 55436-11-8 2-(dimethylaminothiocarbonylthio)desoxybenzoin 
• 59679-12-8 1-Dimethylthiocarbamoylsulfanyl-cyclohexanecarboxylic acid ethyl ester 
• 59679-11-7 Dimethyl-dithiocarbamic acid 1-formyl-cyclohex-3-enyl ester 
• 23846-99-3 trans-Styrol-dimethyldithiocarbamat 
• 16906-70-0 phenyl N,N-dimethyl dithiocarbamate 
• 2741-13-1 3,3-dimethyl-1-(4-methylphenyl)thiourea 
• 2212-17-1 N,N-dimethyl-N'-p-chlorophenylthiourea 
• 23839-34-1 2-oxo-2-phenylethyl dimethylcarbamodithioate 
• 2741-14-2 N'-benzyl-N,N-dimethylthiourea 
• 24070-58-4 N-cyclohexyl-N',N'-dimethylthiourea 
• 15482-60-7 N,N-dimethylthiobenzamide 

Relevant academic research and scientific papers

Method for preparing tetraalkyl thiuram disulfide through photocatalytic oxidation

The invention relates to a method for preparing tetraalkyl thiuram disulfide by photocatalytic oxidation. The method comprises the following steps: carrying out mixed reaction on secondary amine, carbon disulfide and a catalyst in a medium to generate an intermediate product; and carrying out catalytic oxidation reaction on the intermediate product under illumination to obtain tetraalkyl thiuram disulfide. According to the invention, the method is high in reaction speed and mild in condition, and energy conservation and efficiency improvement are achieved; the used medium and catalyst can be recycled, so that the resource utilization rate is improved; and the method does not produce inorganic salt by-products, and the product has high yield and high purity.

Continuous-flow step-economical synthesis of thiuram disulfidesviavisible-light photocatalytic aerobic oxidation

A continuous-flow photocatalytic synthesis of the industrially important thiuram disulfides has been developed, utilizing O2as the oxidant and Eosin Y as the photoredox catalyst. This highly atom- and step-economical method features much reduced reaction time as well as excellent product yield and purity, making it a sustainable and potentially scalable process for industrial production.

Microfluidic electrosynthesis of thiuram disulfides

An electrolytic approach to sodium dithiocarbamates based on a microfluidic reactor is proposed for the green synthesis of thiuram disulfides, which are versatile free radical initiators. The electro-oxidation reactions avoid the over-oxidation of sodium dithiocarbamates and the generation of waste salts, which have perplexed the industry for a long time. This microfluidic electrolysis method prevents solid deposition by introducing liquid-liquid Taylor flow into the microchannel, and promotes the synthesis efficiency of thiuram disulfides with the enlargement of the electrode-specific surface area. The highest yield of thiuram disulfide was 88% in the experiment without any oxidation by-products. The Faraday efficiencies of most reactions are higher than 96%, showing the excellent electronic utilization. In addition to improving the environmental friendliness of sodium dithiocarbamate oxidation, the electrosynthesis method helps to create a cyclic technology of thiuram disulfide synthesis via the combination of sodium dithiocarbamate generation in a packed bed reactor. The cyclic technology finally achieved >99% atom utilization in thiuram disulfide synthesis from secondary amines and carbon disulfide. This journal is

Development of disulfide-derived fructose-1,6-bisphosphatase (FBPase) covalent inhibitors for the treatment of type 2 diabetes

Fructose-1,6-bisphosphatase (FBPase), as a key rate-limiting enzyme in the gluconeogenesis (GNG) pathway, represents a practical therapeutic strategy for type 2 diabetes (T2D). Our previous work first identified cysteine residue 128 (C128) was an important allosteric site in the structure of FBPase, while pharmacologically targeting C128 attenuated the catalytic ability of FBPase. Herein, ten approved cysteine covalent drugs were selected for exploring FBPase inhibitory activities, and the alcohol deterrent disulfiram displayed superior inhibitory efficacy among those drugs. Based on the structure of lead compound disulfiram, 58 disulfide-derived compounds were designed and synthesized for investigating FBPase inhibitory activities. Optimal compound 3a exhibited significant FBPase inhibition and glucose-lowering efficacy in vitro and in vivo. Furthermore, 3a covalently modified the C128 site, and then regulated the N125–S124–S123 allosteric pathway of FBPase in mechanism. In summary, 3a has the potential to be a novel FBPase inhibitor for T2D therapy.

Photocatalytic H2-Evolution by Homogeneous Molybdenum Sulfide Clusters Supported by Dithiocarbamate Ligands

Irradiation at 460 nm of [Mo3(μ3-S)(μ2-S2)3(S2CNR2)3]I ([2a]I, R = Me; [2b]I, R = Et; [2c]I, R = iBu; [2d]I, R = CH2C6H5) in a mixed aqueous-polar organic medium with [Ru(bipy)3]2+ as photosensitizer and Et3N as electron donor leads to H2 evolution. Maximum activity (300 turnovers, 3 h) is found with R = iBu in 1:9 H2O:MeCN; diminished activity is attributed to deterioration of [Ru(bipy)3]2+. Monitoring of the photolysis mixture by mass spectrometry suggests transformation of [Mo3(μ3-S)(μ2-S2)3(S2CNR2)3]+ to [Mo3(μ3-S)(μ2-S)3(S2CNR2)3]+ via extrusion of sulfur on a time scale of minutes without accumulation of the intermediate [Mo3S6(S2CNR2)3]+ or [Mo3S5(S2CNR2)3]+ species. Deliberate preparation of [Mo3S4(S2CNEt2)3]+ ([3]+) and treatment with Et2NCS21- yields [Mo3S4(S2CNEt2)4] (4), where the fourth dithiocarbamate ligand bridges one edge of the Mo3 triangle. Photolysis of 4 leads to H2 evolution but at ～25% the level observed for [Mo3S7(S2CNEt2)3]+. Early time monitoring of the photolyses shows that [Mo3S4(S2CNEt2)4] evolves H2 immediately and at constant rate, while [Mo3S7(S2CNEt2)3]+ shows a distinctive incubation prior to a more rapid H2 evolution rate. This observation implies the operation of catalysts of different identity in the two cases. Photolysis solutions of [Mo3S7(S2CNiBu2)3]+ left undisturbed over 24 h deposit the asymmetric Mo6 cluster [(iBu2NCS2)3(μ2-S2)2(μ3-S)Mo3](μ3-S)(μ3-η2,η1-S′,η1-S″-S2)[Mo3(μ2-S)3(μ3-S)(S2CNiBu2)2(μ2-S2CNiBu2)] in crystalline form, suggesting that species with this hexametallic composition and core topology are the probable H2-evolving catalysts in photolyses beginning with [Mo3S7(S2CNR2)3]+. When used as solvent, N,N-dimethylformamide (DMF) suppresses H2-evolution but to a greater degree for [Mo3S4(S2CNEt2)4] than for [Mo3S7(S2CNEt2)3]+. Recrystallization of [Mo3S4(S2CNEt2)4] from DMF affords [Mo3S4(S2CNEt2)4(η1,κO-DMF)] (5), implying that inhibition by DMF arises from competition for a Mo coordination site that is requisite for H2 evolution. Computational assessment of [Mo3S4(S2CNMe2)3]+ following addition of 2H+ and 2e- suggests a Mo(H)-μ2(SH) intermediate as the lowest energy species for H2 elimination. An analogous pathway may be available to the Mo6 cluster via dissociation of one end of the μ2-S2CNR2 ligand, a known hemilabile ligand type, in the [Mo3S4]4+ fragment.

Synthetic method of tetramethylthiuram disulfide drug intermediate

The invention discloses a synthetic method of a tetramethylthiuram disulfide drug intermediate. The synthetic method comprises the following steps: adding a dimethylamine solution and a sodium nitratesolution into a reaction container, controlling the solution temperature to be 20 to 24 DEG C, controlling the stirring speed to be 230 to 260 rpm, adding a 1-pentanethiol solution, adding a thiophane solution in batches within 30 to 50 min, and continuously reacting for 80 to 120 min; then adding nickel bromide powder, controlling the solution temperature to be 15 to 18 DEG C, adding lead tetraacetate, continuously reacting for 2 to 4 h, standing for 30 to 50 min, adding a potassium chloride solution, layering the solution to separate an oil layer, washing with a 2-heptanone solution for 20to 40 min, carrying out recrystallization in a 1-chloropropane solution, and carrying out dehydration of a dehydrating agent so as to obtain the finished product tetramethylthiuram disulfide.

High-efficiency green synthesis method for thiram

The invention discloses a high-efficiency green synthesis method for thiram. The high-efficiency green synthesis method comprises the following steps: by taking water as a reaction solvet, adding a dimethylamine solution and carbon disulfide so as to synthesize an intermediate; adding hydrogen peroxide for oxidation synthesis, performing solid-liquid separation, and drying, thereby obtaining the thiram. The reaction of the method is implemented in water, the thiram is synthesized by using a one-pot method through two steps, no organic solvent is needed, inorganic alkali or organic alkali is not needed, sewage can be easily recycled and reused, the method has the characteristics of simple process and easy operation, and the purity of the thiram can be greater than 98%. The mother liquor used in the method is subjected to reverse osmosis treatment and is recycled and reused, so that the method is small in water amount, free of waste salt and very environmental-friendly and economic.

Pyruvate dehydrogenase kinase inhibitor and application thereof

The invention provides a pyruvate dehydrogenase kinase inhibitor and an application thereof, specifically a compound as shown in a formula I described in the specification or pharmaceutically acceptable salts thereof. The compound has excellent effects of inhibiting pyruvate dehydrogenase kinase activity and resisting tumors. The invention also provides a pharmaceutical composition containing the compound provided by the invention and the application thereof in the aspect of inhibiting pyruvate dehydrogenase kinase.

Role of disulfide linkage in action of bis(dialkylaminethiocarbonyl)disulfides as potent double-Edged microbicidal spermicide: Design, synthesis and biology

Trichomoniasis and candidiasis are amongst the most common morbidity-causing reproductive tract infections, generally treated by Metronidazole and Fluconazole respectively. Poor vaginal efficacy, drug-resistance and non-spermicidal nature limit their use as topical microbicidal contraceptives. Bis(dialkylaminethiocarbonyl)disulfides (4-38) were designed as dually active, non-surfactant molecules capable of eliminating Trichomonas vaginalis and Candida strains as well as irreversibly immobilizing 100% human sperm instantly, at doses non-cytotoxic to human cervical epithelial cells and vaginal microflora in vitro. Compounds 12, 16, 17 were fifty times more active than nonoxynol-9, OTC vaginal spermicide, and compounds 12 and 17 have shown remarkable in vivo activity in rabbit model. Most promising compound 17 has shown promise for further development as a double-edged vaginal microbicide due to their improved activity and safety along with notable in vivo trichomonicidal activity. Role of disulfide group was established by loss of spermicidal activity on chemical modifications (39-56). These disulfides might be targeting thiol groups present over cell membrane of human sperm and Trichomonas as shown by fluorescence labeling of free thiols.

Cerium ammonium nitrate-catalyzed aerobic oxidative coupling of dithiocarbamates: Facile synthesis of thioureas and bis(aminothiocarbonyl)disulfides

Diverse disubstituted and trisubstituted thioureas were synthesized by the condensation of dithiocarbamate TEA (or DABCO) salts and amines using cerium ammonium nitrate (CAN) as a catalyst in high yields at room temperature. It is a one-pot method and it is unnecessary to isolate isothiocyanates. This reaction probably took place through nucleophilic addition of amines to isothiocyanates, which were generated by oxidative coupling of dithiocarbamates and the following decomposition of bis(aminothiocarbonyl)disulfides. When secondary amines and CS2served as the reactants, bis(aminothiocarbonyl)disulfides were obtained via tandem nucleophilic addition/oxidative coupling reactions in moderate to excellent yields. In all the coupling reactions, the oxidant was air and CAN possibly acted as an SET catalyst.