Category: amides-buliding-blocks

Synthetic Route of 6228-73-5, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 6228-73-5, name is Cyclopropanecarboxamide belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.

To a solution of 207.2 (0.270g, 0.79mmol, l .Oeq) in 1,4-dioxane (3mL) was added cyclopropane carboxamide (O. lOlg, 1.19mmol, 1.5eq), potassium carbonate (0.27g, 1.98mmol, 2.5eq). The reaction mixture was degassed for 10 min. under argon atmosphere, then tris(dibenzylideneacetone)dipalladium(0) (0.072g, 0.079mmol, O. leq) and 4,5-Bis(diphenylphosphino)-9,9-dimethylxanthene (0.091g, 0.158mmol, 0.2eq) were added, again degassed for 5 min. The reaction was stirred at 130C for 2h under microwave irradiation. After completion of reaction, reaction mixture was cooled to room temperature, transferred in water and product was extracted with ethyl acetate. Organic layer was combined, washed with brine solution, dried over sodium sulphate and concentrated under reduced pressure to obtain crude material. This was further purified by column chromatography using 2% methanol in dichloromethane as eluant to obtain pure 207.3 (0.250g, 81.03%). MS(ES): m/z 390.25 [M+H]+

The synthetic route of Cyclopropanecarboxamide has been constantly updated, and we look forward to future research findings.

Reference:
Patent; NIMBUS LAKSHMI, INC.; GREENWOOD, Jeremy Robert; HARRIMAN, Geraldine C.; LEIT DE MORADEI, Silvana Marcel; MASSE, Craig E.; MCLEAN, Thomas H.; MONDAL, Sayan; (401 pag.)WO2018/71794; (2018); A1;,
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Application of 128263-66-1,Some common heterocyclic compound, 128263-66-1, name is N-(4-(Aminomethyl)phenyl)methanesulfonamide hydrochloride, molecular formula is C8H13ClN2O2S, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.

Example I N-[4-[[2-Hydroxy-3-(3-methylphenoxy)propyl]aminomethyl]phenyl]methanesulfonamide hydrochloride Heat a mixture of N-[4-(aminomethyl)phenyl]methanesulfonamide hydrochloride(15.0 g, 63.4 mmol) and 1,2-epoxy-3-phenoxypropane (10.41 g, 63.4 mmol) in 63.4 mL of 1 N KOH in methanol and 10 mL of water for about 3.5 h. Remove the solvent to afford crystals of the title compound. NMR (DMSO-d6): delta=2.27(s,3), 2.85-3.15(m,2), 3.02 (s,3), 3.93(s,2), 4.14(s,2), 4.23(br s,1), 5.90(br s,1), 6.74(m,3), 7.19(m,1), 7.24(d,2), 7.53(d,2), ca. 9.35 (br s,2) and 9.97(s,1) ppm.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route N-(4-(Aminomethyl)phenyl)methanesulfonamide hydrochloride, its application will become more common.

Reference:
Patent; Schering AG; US5051423; (1991); A;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Application of 830-43-3, These common heterocyclic compound, 830-43-3, name is 4-(Trifluoromethyl)benzenesulfonamide, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.

General procedure: Pyridine (5 mol) was added to a stirred solution of corresponding amine (1.0 mol) in THF (10 v), after 5 minutes, sulfonyl chloride derivative (1.1 mol) was added, stirred at room temperature under argon atmosphere for 16 h. Then the reaction mixture was diluted with water (50 v), extracted with EtOAc (50 v X 2), evaporated the solvent in vacuo, the crude product was purified by column chromatography to afford 8/9(a-c) and 12/13(a-b) (58-86%) as solids. During thesynthesis of N-(4-(3-((3S,4S)-3,4-Dihydroxypyrrolidin-1-yl)-3-oxopropyl)phenyl)-4-(trifluoromethyl)benzenesulfonamide (13b), isolated 29% of disulphonation product N-(4-(3 N-(4-(3-((3S,4S)-3,4-Dihydroxypyrrolidin-1-yl)-3-oxopropyl)phenyl)-4-(trifluoromethyl)-N-(4-(trifluoromethyl)phenylsulfonyl)benzenesulfonamide (13c) as white solid.

Statistics shows that 4-(Trifluoromethyl)benzenesulfonamide is playing an increasingly important role. we look forward to future research findings about 830-43-3.

Reference:
Article; Kasturi, Sivaprasad; Surarapu, Sujatha; Uppalanchi, Srinivas; Anireddy, Jaya Shree; Dwivedi, Shubham; Anantaraju, Hasitha Shilpa; Perumal, Yogeeswari; Sigalapalli, Dilep Kumar; Babu, Bathini Nagendra; Ethiraj, Krishna S.; Bioorganic and Medicinal Chemistry Letters; vol. 27; 12; (2017); p. 2818 – 2823;,
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These common heterocyclic compound, 402-46-0, name is 4-Fluorobenzenesulfonamide, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. Quality Control of 4-Fluorobenzenesulfonamide

Example 44; 4-{2-[4-(4-Sulfamoylphcnyl)pipcrazin-l-yl]cthyl}pipcridinc-l-carboxylic acid tert-butyl ester hydrochloride; EPO A mixture of 4-fluorobenzenesulfonamide (1.00 g, 5.71 mmol) and piperazine (2.46 g, 28.54 mmol) in water (12 mL) was heated at 1000C for 2Oh. The resulting precipitate was collected filtration and washed with water and toluene to give 4-piperazin-l- ylbenzenesulfonamide: RT = 0.49 min; m/z (ES+) = 242.13 [M+H]+. A solution of 4-piperazin- 1-ylbenzenesulfonamide (0.46 g, 1.89 mmol) and 4-(2-oxoethyl)piperidine-l-carboxylic acid tert-butyl ester (0.43 g, 1.89 mmol) in DCM (50 mL) and THF (7 mL) with molecular sieves (0.90 g) was stirred under argon at rt for Ih. Sodium acetoxyborohydride (0.52 g, 2.46 mmol) was added and the reaction mixture was stirred for a further 2.5h. The reaction mixture was quenched with saturated NaHCO3 solution and extracted with EtOAc. The organic extracts were washed with brine, dried (MgSO4) and the solvent was removed under vacuum. The resulting solid was purified by recrystallisation (EtOAc) then dissolved in THF and 1 M HCl in dioxane (0.95 equivalents), the solvent was removed under vacuum and the resulting solid was washed with Et2O to afford the title compound: RT = 2.51 min; m/z (ES+) = 453.33 [M+H]+.

The synthetic route of 4-Fluorobenzenesulfonamide has been constantly updated, and we look forward to future research findings.

Reference:
Patent; PROSIDION LIMITED; WO2007/3964; (2007); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Reference of 5466-88-6, A common heterocyclic compound, 5466-88-6, name is 2H-1,4-Benzoxazin-3(4H)-one, molecular formula is C8H7NO2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.

4-(4-Bromobutan-1-yl)-3,4-dihydro-2H-1,4-benzoxazin-3(4H)-one from 3,4-dihydro-2H-1,4-benzoxazin-3(4H)-one and 1,4-dibromobutane

The synthetic route of 5466-88-6 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; H. Lundbeck A/S; US2003/191133; (2003); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 89979-12-4, name is 5-Chloro-2-(methylsulfonamido)benzoic acid, This compound has unique chemical properties. The synthetic route is as follows., name: 5-Chloro-2-(methylsulfonamido)benzoic acid

Mixed 5-chloro-2-(methylsulfonamido)benzoic acid (28mg, 0.109mmol) with HATU (42mg, 0.109mmol) and dissolved in anhydrous DMF (300uL). Stirred for Ihr. Dissolved hydrogenation product in anhydrous DMF (300uL) and added to the reaction. Added TEA (30uL, 0.218mmol).Stirred for 12 hrs. Diluted with acetonitrile and purified with Prep HPLC to give compound 40 (22mg, 32% yield).1H NMR (400MHz, CD3OD): delta 7.49 (m, 3H), 6.26 (m, 1H), 6.08 (m, 1H), 4.78 (m, 1H), 4.57 (m, 2H), 4.14 (m, 2H), 3.47-3.34 (m, 2H), 3.01 (m, 4H), 2.76 (s, 3H), 2.40-2.05 (m, 2H), 1.73- 1.50 (m, 4H). LC/MS (m/z): 519.2 [M+H]+

According to the analysis of related databases, 89979-12-4, the application of this compound in the production field has become more and more popular.

Reference:
Patent; GILEAD SCIENCES, INC.; BABAOGLU, Kerim; BOOJAMRA, Constantine, G.; EISENBERG, Eugene, J.; HUI, Hon Chung; MACKMAN, Richard, L.; PARRISH, Jay, P.; SANGI, Michael; SAUNDERS, Oliver, L.; SIEGEL, Dustin; SPERANDIO, David; YANG, Hai; WO2011/163518; (2011); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Adding a certain compound to certain chemical reactions, such as: 86-86-2, name is 1-Naphthaleneacetamide, belongs to amides-buliding-blocks compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 86-86-2, COA of Formula: C12H11NO

General procedure: A mixture of the amide (1, 1 mmol), alcohol (15 mL), and pulverized potassium bisulfate (1.1 g, 8 mmol) was refluxed for the specified time. The alcohol was removed in vacuo and the residue was triturated with hexanes (or other appropriate solvent such as DCM or ethyl acetate to dissolve the product). Removal of hexanes in vacuo provided the following pure products

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Reference:
Article; Sattenapally, Narsimha; Sharma, Jhanvi; Hou, Yuqing; Arkivoc; vol. 2018; 5; (2018); p. 174 – 183;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Synthetic Route of 22503-72-6, These common heterocyclic compound, 22503-72-6, name is 7-Chloro-3-methyl-3,4-dihydro-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.

General procedure: To an ice-cooled solution of 2,3-dihydrobenzothiadiazine 1 or 6-13(1.0 mmol) in CH2Cl2 (10 mL) was added dropwise an excess ofMCPBA (739 mg, 3.0 mmol, 70%) in CH2Cl2 (10 mL) previouslycooled in an ice bath. The mixture was allowed to gradually warmto r.t., with stirring, over 12 h. TLC and LC-MS analyses were usedto monitor reaction progress. The solution was then evaporated todryness, in vacuo at r.t., to give the crude material. The reactionmixture was purified by chromatography on silica gel (petroleumether-EtOAc, 60:40).

The synthetic route of 22503-72-6 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Cannazza, Giuseppe; Perrone, Serena; Rosato, Francesca; D’Accolti, Lucia; Parenti, Carlo; Troisi, Luigino; Synthesis; vol. 46; 7; (2014); p. 962 – 966;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 24451-15-8, name is Ethyl 2-((4-bromophenyl)amino)-2-oxoacetate, A new synthetic method of this compound is introduced below., Computed Properties of C10H10BrNO3

General procedure: A methanolic solution of TBAOH (1.0 M, 2.4 mmol) was addeddirectly to a one-neck round flask suspension of the correspondingN-substituted oxamate proligand (0.6 mmol) in 10 mL of acetonitrileat 60 C. Then, an aqueous solution of K2[PdCl4] (100 mg,0.3 mmol in 5 mL of water) was added dropwise to the reactionmixture and resulting basic solution was heated at 60 C for 10 hunder continuous stirring. The solution was allowed to evaporateat room temperature. X-ray quality yellow prisms were grownup after two weeks (2) and a couple of days (3 and 4). Their formulaswere determined by X-ray diffraction on single crystals.2: Yield: 90%

The synthetic route of 24451-15-8 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Fortea-Perez, Francisco Ramon; Neve, Francesco; Armentano, Donatella; De Munno, Giovanni; Stiriba, Salah-Eddine; Julve, Miguel; Inorganica Chimica Acta; vol. 443; (2016); p. 267 – 273;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Related Products of 563-83-7, A common heterocyclic compound, 563-83-7, name is Isobutyramide, molecular formula is C4H9NO, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.

General procedure: A mixture of cobalt(II) oxalate dihydrate(Sigma-Aldrich, 0.294 mmol), Cs2CO3 (2.94 mmol), pyrrolidinoneor aliphatic amide (1.47 mmol), DMEDA (0.588 mmol),distilled H2O (0.3 mL) and aryl halide (2.205 mmol) were addedto an 8.0-mL reaction vial fitted with a Teflon-sealed screw cap.The reaction mixture was stirred under air in a closed system at120 C and 130 C, respectively for 24 h. The heterogeneousmixture was subsequently cooled to r.t. and diluted withCH2Cl2. The combined organic extracts were dried over anhydNa2SO4, filtered and the solvent was removed under reducedpressure. The crude product was loaded into the column usingminimal amounts of CH2Cl2 and was purified by silica gel column chromatography to afford the N-arylated product. Theidentity and purity of products were confirmed by 1H NMR and13C NMR spectroscopic analysis.

The synthetic route of 563-83-7 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Tan, Bryan Yong-Hao; Teo, Yong-Chua; Synlett; vol. 26; 12; (2015); p. 1697 – 1701;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics