Amides-buliding-blocks

Related Products of 138-41-0, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 138-41-0 name is Carzenide, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

To a solution of (3aS,6aS)-tert-butyl hexahydropyrrolo[3,4-c]pyrrole-2(lH)-carboxylate (intermediate 3; 206 mg, 970 muiotaetaomicron), N-methylmorpholine (294 mg, 2.91 mmol) and 4- sulfamoylbenzoic acid (203 mg, 970 muiotaetaomicron) in N,N-dimethylformamide (10 ml) was added 0-(7- azabenzotriazol-l-yl)-N,N,N’,N’ -tetramethyluronium hexafluoro-phosphate (369 mg, 970 muiotaetaomicron) at 0C, then after 10 min the ice-bath was removed. After 16 h the reaction mixture was partitioned between dichloromethane and sat. aq. sodium hydrogencarbonate solution. The organic layer was washed with sat. aq. ammonium chloride solution and brine, dried over magnesium sulfate, filtered and evaporated. After trituration in tert-butyl methyl ether the precipitate was collected by filtration to afford the title compound (348 mg, 91 ). Light yellow solid, MS: 396.6 (M+H)+.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, Carzenide, and friends who are interested can also refer to it.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; HERT, Jerome; HUNZIKER, Daniel; MATTEI, Patrizio; MAUSER, Harald; TANG, Guozhi; WANG, Lisha; WO2014/139978; (2014); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Synthetic Route of 4815-28-5,Some common heterocyclic compound, 4815-28-5, name is 2-Amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, molecular formula is C9H12N2OS, 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: 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide(4a;1.5 mmol) was suspended in 10 ml butanol and benzaldehydes(5a-5m;1.0 mmol). Conc HCl (0.1 ml) was added to this reaction mixture and heated at 80 C for 12 h or until TLC confirms the completion of reaction. The solid obtained was filtered, washedwith water and dried.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-Amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, its application will become more common.

Reference:
Article; Amawi, Haneen; Karthikeyan, Chandrabose; Pathak, Rekha; Hussein, Noor; Christman, Ryann; Robey, Robert; Ashby, Charles R.; Trivedi, Piyush; Malhotra, Ashim; Tiwari, Amit K.; European Journal of Medicinal Chemistry; vol. 138; (2017); p. 1053 – 1065;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

These common heterocyclic compound, 406233-31-6, name is 4-Fluoro-3-nitrobenzenesulfonamide, 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. Product Details of 406233-31-6

To a stirred solution of (4-methylmorpholin-2-yl)methanamine (400 mg, 3.07 mmol) in THF (25 mL) was added 4-fluoro-3-nitrobenzenesulfonamide (609 mg, 2.76 mmol) followed by triethylamine (1.24 g, 12.28 mmol). After stirring at rt for 16 h, the reaction was concentrated and the resulting crude was diluted with 10% MeOH-DCM (50 mL), and washed with ice-cold water (3 x 50 mL). The organic layer was dried over Na2S04, filtered and concentrated. The crude product was triturated with Et20/pentane to afford Intermediate 17 (600 mg, 65% yield) as a yellow solid. LC/MS (ESI) m/z 331.2 [M+H]+.

The synthetic route of 4-Fluoro-3-nitrobenzenesulfonamide has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ZENO ROYALTIES & MILESTONES, LLC; PINCHMAN, Joseph, Robert; HUANG, Peter, Qinhua; BUNKER, Kevin, Duane; SIT, Rakesh, Kumar; SAMATAR, Ahmed, Abdi; (236 pag.)WO2019/139902; (2019); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Adding a certain compound to certain chemical reactions, such as: 120157-96-2, name is Methyl 4-(((tert-butoxycarbonyl)amino)methyl)benzoate, 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 120157-96-2, category: amides-buliding-blocks

Reference Example 63 tert-Butyl 4-hydroxymethylbenzylcarbamate Diisobutylaluminum hydride (25.7 ml, 0.93 M hexane solution) was added dropwise to a THF solution (40 ml) of methyl 4-[N-(tert–butoxycarbonyl)aminomethyl]benzoate (2.54 g) at -78C, followed by stirring at the same temperature for 2 hours. A saturated aqueous ammonium chloride solution (10 ml) and diethyl ether were added dropwise to the reaction solution, followed by stirring at room temperature for 1 hour. Magnesium sulfate was added to the reaction solution, followed by further stirring for 1 hour. After removal of the resulting precipitate by filtration trough celite, the filtrate was concentrated, the thus obtained residue was purified by silica gel column chromatography, and the title compound (1.22 g) was obtained as a colorless oil from the fraction of the elude of n-hexane: ethyl acetate = 10:3. 1H-NMR (400 MHz, CDCl3) delta: 1.43 (9H, s), 4.29 (2H, d, J=5.6 Hz), 4.67 (2H, d, J=5.9 Hz), 4.87 (1H, bs), 7.25 (2H, d, J=8.1 Hz), 7.32 (2H, d, J=8.1 Hz).

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it.

Reference:
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1612204; (2006); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Synthetic Route of 152192-95-5, These common heterocyclic compound, 152192-95-5, name is tert-Butyl ethyl(2-hydroxyethyl)carbamate, 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.

Stage 2: [2-(1,3-Dihydroisoindol-2-yl)ethyl]ethylcarbamic acid tert-butyl ester: A solution of 10.2 g of diethyl azodicarboxylate in 60 ml of THF is added dropwise to a mixture containing 11.92 g of ethyl-(2-hydroxyethyl)carbamic acid tert-butyl ester, 15.2 g of isoindole-1,3-dione and 8.6 g of triphenylphosphine in 40 ml of THF. The medium is kept stirring overnight at room temperature and then concentrated to dryness. The medium is taken up in 100 ml of ethyl ether, the precipitate formed is removed by filtration. The filtrate is concentrated and chromatographed on a silica column (heptane in a gradient up to 3% ethyl acetate). 14 g of expected product are obtained.

Statistics shows that tert-Butyl ethyl(2-hydroxyethyl)carbamate is playing an increasingly important role. we look forward to future research findings about 152192-95-5.

Reference:
Patent; sanofi-aventis; US2008/269170; (2008); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Application of 116861-31-5, These common heterocyclic compound, 116861-31-5, name is tert-Butyl (3-chloropropyl)carbamate, 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.

S1-1 (557 mg, 2.876 mmole, 1 equiv) was dissolved in 2 mL dry DMF under inert atmosphere. To this solution, potassium thioacetate (548 mg, 3.164 mmole, 1.1 equiv) was added as a powder to the stirring reaction mixture. The reaction was allowed to go overnight and monitored for completion by TLC and LC/MS. The reaction mixture was diluted with 20 mL EtOAc and transferred to a seperatory funnel. The organic layer was washed with 3 X 20 mL saturated NaCl solution. The organic layer was dried over Na2SO4, filtered, and evaporated to dryness to afford a crude yellow oil (MW: 233.33 g/mol, 400 mg, 60% yield), which was of sufficient purity for the next step.1H NMR (400 MHz, CDCl3): 3.12 (m, 2H), 2.86 (t, J = 7.0 Hz, 2H), 2.3 (s, 3H), 1.71 (m, 2H), 1.40 (s, 9H).

The synthetic route of 116861-31-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; SHOKAT, Kevan, M.; GENTILE, Daniel; MOSS, Steven; (380 pag.)WO2018/112420; (2018); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Some common heterocyclic compound, 16066-84-5, name is tert-Butyl methylcarbamate, molecular formula is C6H13NO2, 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. HPLC of Formula: C6H13NO2

24 g (120 mmol) of 2-chloro-5-(trifluoromethoxy)pyridine, 19.1 g (150 mmol) of tert-butyl N-methylcarbamate and 17.5 g (180 mmol) of sodium tert-butoxide were dissolved in 400 ml of toluene, 2.8 g (3 mmol) of tris(dibenzylideneacetone)dipalladium(0) and 1.73 g (3 mmol) of Xantphos were added under argon, and the mixture was stirred at 100-105 C. for 12 h. Subsequently, the mixture was filtered through Celite and the solvent was distilled off under reduced pressure.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 16066-84-5, its application will become more common.

Reference:
Patent; BAYER CROPSCIENCE AKTIENGESELLSCHAFT; FISCHER, Ruediger; HAGER, Dominik; HOFFMEISTER, Laura; KAUSCH-BUSIES, Nina; WILCKE, David; WILLOT, Matthieu; GOeRGENS, Urich; ILG, Kerstin; MOSRIN, Marc; PORTZ, Daniela; TURBERG, Andreas; US2018/305353; (2018); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Application of 1314538-55-0, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 1314538-55-0 name is Potassium (((tert-butoxycarbonyl)amino)methyl)trifluoroborate, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

A mixture of 4,6-dichloro-2-(trifluoromethyl)pyrimidine (500 mg, 2.30 mmol, 1.00 equiv), potassium terf-butyl N-[(trifluoroboranuidyl)methyl]carbamate (546 mg, 2.30 mmol, 0.99 equiv), Pd(PPh3)2Cl2 (162 mg, 0.23 mmol, 0.10 equiv), and sodium carbonate (488 mg, 4.60 mmol, 1.99 equiv) in t-butanol (10 mL)/water (2 mL) was stirred for 2 h at 70 C under nitrogen. The solid was filtered off and the filtrate was diluted with water, extracted with ethyl acetate, washed with brine, dried over anhydrous sodium sulfate, and concentrated under vacuum. The residue was purified by a silica gel column eluting with ethyl acetate/petroleum ether (1/5) to afford the title compound (450 mg, 63%) as a white solid. LCMS [M+H+] 312

At the same time, in my other blogs, there are other synthetic methods of this type of compound, Potassium (((tert-butoxycarbonyl)amino)methyl)trifluoroborate, and friends who are interested can also refer to it.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; GENENTECH, INC.; VERMA, Vishal; SHORE, Daniel; VOLGRAF, Matthew; ESTRADA, Anthony A.; LYSSIKATOS, Joseph; (153 pag.)WO2018/15410; (2018); A1;,
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. 113778-69-1, name is N-Methoxy-N-methylisobutyramide, A new synthetic method of this compound is introduced below., Product Details of 113778-69-1

A 250 mL flask was charged with a solution of 2-chloro-6-methoxypyridine (20 g, 0.139 mol, 1 equiv.) in THF (300 mL) under nitrogen atmosphere. To the mixture was then added tert-butyllithium (131 mL, 0.210 mol, 1.5 equiv.), which was added dropwise with stirring at -70 C. The reaction mixture was stirred at -78 C. for 2 h. N-methoxy-N-methylisobutyramide (24 g, 0.182 mol, 1.3 equiv.) was then added dropwise. The mixture was stirred for 3.0 h at -78 C. The reaction progress was monitored by LCMS. The reaction was quenched by the addition of ammonium chloride aqueous solution and then extracted with ethyl acetate, the organic layers combined and concentrated under vacuum. The residue was applied onto a sillia gel column with PE/EA=100/1 to yield 1-(6-chloro-2-methoxypyridin-3-yl)-2-methylpropan-1-one as yellow oil. Mass spectrum (ESI, m/z): Calculated for C10H12ClNO2, 214.1 (M+H), found 214.1.

The synthetic route of 113778-69-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Janssen Pharmaceutica NV; Zhang, Xuqing; Macielag, Mark J.; (179 pag.)US2019/47959; (2019); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Related Products of 144-80-9, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 144-80-9 as follows.

Example 155N-({4-[(4-[difluoro(4-fluorophenyl)methyl]-6-{[6-(ethyloxy)-1,3-benzothiazol-2-yl]amino}-2-pyrimidinyl)amino]phenyl}sulfonyl)acetamideA mixture of N-{2-chloro-6-[difluoro(4-fluorophenyl)methyl]-4-pyrimidinyl}-6-(ethyloxy)-1,3-benzothiazol-2-amine (100mg, 0.222mmol), N-[(4-aminophenyl)sulfonyl]acetamide (95mg, 0.444mmol) and 4-toluenesulfonic acid monohydrate (50.6mg, 0.266mmol) in acetonitrile (3m L) was sealed and heated at 1200C for 4 hours in a Biotage “Initiator” microwave. The product was purified by mass-directed autopreparative HPLC (formic acid modifier) to afford the title compound (21 rmg, 0.033mmol, 20% yield) as a white solid. LCMS (Method A): Rt 1.19 minutes; m/z 629 (MH+).

According to the analysis of related databases, 144-80-9, the application of this compound in the production field has become more and more popular.

Reference:
Patent; GLAXO GROUP LIMITED; ALDER, Catherine, Mary; BALDWIN, Ian, Robert; BARTON, Nicholas, Paul; CAMPBELL, Amanda, Jennifer; CHAMPIGNY, Aurelie, Cecile; HARLING, John, David; MAXWELL, Aoife, Caitriona; SIMPSON, Juliet, Kay; SMITH, Ian, Edward, David; TAME, Christopher, John; WILSON, Caroline; WOOLVEN, James, Michael; WO2010/106016; (2010); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics