Category: amides-buliding-blocks

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 72080-83-2 as follows. Safety of Benzyl (2-aminoethyl)carbamate

General procedure: A mixture ofcompound 10 (0.15 g, 0.772 mmol), HOBt (0.23 g,1.70 mmol), EDCI (0.37 g, 1.93 mmol), benzoic acid(0.19 g, 1.54 mmol), and TEA (0.32 mL, 2.32 mmol) indry DMF (20 mL) was stirred at 80 C for 8 h. The mixturewas quenched with water (40 mL), then extracted withethyl acetate (3 x 40 mL). The combined organic layerextracts were washed with brine, dried over anhydrousMgSO4, filtered, and concentrated under reduced pressure.The residue was purified by flash column chromatography.The desired product was obtained as white solid (0.13 g,56.4 %).

According to the analysis of related databases, 72080-83-2, the application of this compound in the production field has become more and more popular.

Reference:
Article; Abdel-Maksoud, Mohammed S.; El-Gamal, Mohammed I.; Gamal El-Din, Mahmoud M.; Kwak, Seong-Shin; Kim, Hyun-Il; Oh, Chang-Hyun; Medicinal Chemistry Research; vol. 25; 5; (2016); p. 824 – 833;,
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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 116332-54-8 as follows. category: amides-buliding-blocks

a 4-Fluoro-2-(2-methylthio-4-pyrimidyl)acetophenone nBuLi (10 ml of a 1.6 M solution in hexane; 12 mmol) is added at -78 C. to a solution of diisopropylamine (2.48 ml; 17 mmol) in THF (15 ml) and stirred for 5 min. 4-Methyl-2-(methylthio)pyrimidine (2 g; 14.5 mmol) dissolved in THF (2 ml) is added dropwise and stirred for 30 mm at -78 C. 4-Fluoro-N-methoxy-N-methylbenzamide (2.66 g; 14.5 mmol) is dissolved in THF (3 ml) and added slowly to the reaction mixture. The mixture is warmed to r.t. within 45 min. and poured on water and extracted with ethyl acetate three times. The combined organic phases are dried over Na2SO4 and evaporated to dryness to yield 2.5 g (65%) of yellow crystals after recrystallisation from tert.butyl methyl ether/hexane. 1H-NMR (200 MHz CDCl3): 3.00 (s, 3H): 6.30 (s, 1H); vinyl-H of enol); 7.00 (d, 1); 7.50 (dd, 2H); 8.20 (dd, 2H); 8.7 (d, 2H). Due to pH-dependent keto-enol tautomerism, signals may be duplicated.

According to the analysis of related databases, 116332-54-8, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Revesz, Laszlo; Schlapbach, Achim; US2002/49220; (2002); A1;,
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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. 2227-79-4, name is Benzothioamide belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below. SDS of cas: 2227-79-4

1) 2.33 g of thiobenzamide was dissolved in 20 ml of dry methanol, and 2.16 g of 1,3-dichloroacetone was added thereto at room temperature and then heated under reflux for 1 hour. The solvent was distilled off under reduced pressure, and ice water was added to the remaining product, which was then neutralized with an aqueous solution of sodium hydrogen carbonate. The resulting product was extracted with ethyl acetate, washed with saturated saline, and dried over sodium sulfate, and the solvent was distilled off under reduced pressure. The residual product was purified through silica gel column chromatography to obtain 2.03 g of 4-chloromethyl-2-phenylthiazole was obtained from the fraction eluted with chloroform/n-hexane=1/2.

The synthetic route of 2227-79-4 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Nissan Chemical Industries, Ltd.; US6063734; (2000); A;,
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Application of 40545-33-3, These common heterocyclic compound, 40545-33-3, name is 2-Amino-5-methylbenzamide, 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 a cold (0-5 C) stirred suspension of aminobenzamides 10a-c (0.016 mol) in pyridine (13 ml), 0.016 mol of the appropriate 3-phenylacryloyl chloride 11c-k was added over 30 min. After addition was complete, the solution was stirred for 24 h and then poured onto crushed ice. The precipitate was removed by filtration, washed with water, and crystallized from ethanol.

Statistics shows that 2-Amino-5-methylbenzamide is playing an increasingly important role. we look forward to future research findings about 40545-33-3.

Reference:
Article; Raffa, Demetrio; Maggio, Benedetta; Plescia, Fabiana; Cascioferro, Stella; Plescia, Salvatore; Raimondi, Maria Valeria; Daidone, Giuseppe; Tolomeo, Manlio; Grimaudo, Stefania; Di Cristina, Antonietta; Pipitone, Rosaria Maria; Bai, Ruoli; Hamel, Ernest; European Journal of Medicinal Chemistry; vol. 46; 7; (2011); p. 2786 – 2796;,
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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. 77925-80-5, name is N-(Benzyloxy)-2-nitrobenzenesulfonamide, This compound has unique chemical properties. The synthetic route is as follows., Recommanded Product: 77925-80-5

[0232] A solution of 2-nitrobenzene-1-sulfonyl chloride (500 g, 2.26 mol) in pyridine (1500 mL) was added dropwise to a solution of O-benzylhydroxylamine hydrochloride (400 g, 2.51 mol) in pyridine (1500 mL) at 0 C. The reaction mixture was then stirred at 20 C. overnight. The mixture was concentrated in vacuum, diluted with DCM and washed with HCl (10%) three times. The combined organic layer was concentrated in vacuum and re-crystallized with DCM to afford N-(benzyloxy)-2-nitrobenzenesulfonamide (485 g, 62.6%) as a yellow solid. [0233] To a solution of N-(benzyloxy)-2-nitrobenzenesulfonamide (212 g, 0.69 mol) in THF (1000 mL) was added (2S,5S)-1-tert-butyl 2-ethyl 5-hydroxypiperidine-1,2-dicarboxylate (171 g, 0.63 mol) and PPh3 (275 g, 1.05 mol), followed by dropwise addition of a solution of DEAD (195 g, 1.12 mol) in THF (500 mL). The mixture was then stirred at 20 C. overnight. The reaction mixture was then concentrated in vacuum and purified by silica gel column chromatography (3:1 petroleum ether/EtOAc) to afford (2S,5R)-1-tert-butyl 2-ethyl 5-(N-(benzyloxy)-2-nitrophenylsulfonamido)piperidine-1,2-dicarboxylate (283.8 g, 80%) as a yellow oil.

According to the analysis of related databases, 77925-80-5, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Gu, Yu Gui; He, Yong; Yin, Ning; Alexander, Dylan C.; Cross, Jason B.; Busch, Robert; Dolle, Roland E.; Metcalf, III, Chester A.; US2013/296555; (2013); A1;,
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194920-62-2, name is tert-Butyl (3-(2-(2-(3-aminopropoxy)ethoxy)ethoxy)propyl)carbamate, belongs to amides-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Recommanded Product: tert-Butyl (3-(2-(2-(3-aminopropoxy)ethoxy)ethoxy)propyl)carbamate

General procedure: Oxime 1 (20 mg, 51.5 mumol) and HOBt.H2O (7.9 mg, 51.5 mumol)were dissolved in 1.5mL of DMF and DIC (8 muL, 51.5 mmol) wasadded. It was stirred for 5 min, then tert-butyl 2-aminoethylcarbamate hydrochloride (20 mg, 102 mumol) and DIEA(18 muL, 102 mumol) were added to the solution. The mixture wasstirred at 50 C for 16 h then it was evaporated in vacuo. The crudeproduct was purified by column chromatography on silica gel 60with CHCl3-MeOH (8:2) to give 22.2 mg (81%) of 2 as yellowish oil.

The synthetic route of 194920-62-2 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Dvoracsko, Szabolcs; Keresztes, Attila; Mollica, Adriano; Stefanucci, Azzurra; Macedonio, Giorgia; Pieretti, Stefano; Zador, Ferenc; Walter, Fruzsina R.; Deli, Maria A.; Kekesi, Gabriella; Banki, Laszlo; Tuboly, Gabor; Horvath, Gyoengyi; Toemboely, Csaba; European Journal of Medicinal Chemistry; vol. 178; (2019); p. 571 – 588;,
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Synthetic Route of 127828-22-2, These common heterocyclic compound, 127828-22-2, name is tert-Butyl (2-(2-aminoethoxy)ethyl)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.

General procedure: (S)-4-(4-chlorophenyl)-6-(2-methoxy-2-oxoethyl)-3 ,9-dimethyl-6H-thieno [3,2- fj [1 ,2,4jtriazolo[4,3-aj [1 ,4jdiazepine-2-carboxylic acid (CAS 916493-82-8) (44 mg, 0.1 mmol), mono-Boc-amino-PEG-amine (1.5 eq), HATU (1.5 eq), and N,Ndiisopropylethylamine (1.5 eq) were added to DMF (0.1 M). The mixture was stirred for 4 hours at room temperature. The mixture was diluted with ethyl acetate, washed with iN NaOH and brine, dried over Na2504, filtrated and concentrated under reduced pressure. The residue was purified by flash chromatography to give mono-amides (93%). The mono-amide was dissolved into dichloromethane (0.5 M). Trifluoroacetic acid (0.5 M) was added to the solution. The mixture was stirred for 1 hour at room temperature. The mixture was diluted with dichloromethane, washed with iN NaOH, dried over Na2504, filtrated and concentrated under reduced pressure. The free amine was used for the next step without purification. The free amine, (S)-4-(4-chlorophenyl)-6-(2-methoxy-2-oxoethyl)-3 ,9-dimethyl-6H-thieno [3,2- fj [1 ,2,4jtriazolo[4,3-aj [1 ,4jdiazepine-2-carboxylic acid (CAS 916493-82-8) (1.1 eq), HATU (1.5 eq), and N,N-diisopropylethylamine (1.5 eq) were added to DMF (0.1 M). The mixture was stirred for 4 hours at room temperature. The mixture was diluted with ethyl acetate, washed with iN NaOH and brine, dried over Na2504, filtrated and concentrated under reduced pressure. The residue was purified by flash chromatography to give the titled compounds (55%, for 2 steps).

The synthetic route of 127828-22-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; DANA-FARBER CANCER INSTITUTE, INC.; BRADNER, James, E.; QI, Jun; TANAKA, Minoru; ROBERTS, Justin, M.; (314 pag.)WO2017/91673; (2017); A2;,
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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. 1103234-56-5, name is 2,6-Difluoro-3-(propylsulfonamido)benzoic acid, This compound has unique chemical properties. The synthetic route is as follows., Application In Synthesis of 2,6-Difluoro-3-(propylsulfonamido)benzoic acid

Example GN-(3 -Amino-2,4-difluorophenyl)propane- 1 -sulfonamideTo a solution of 2,6-difluoro-3-(propylsulfonamido)benzoic acid (4.078 g, 14.6 mmol) inTHF (60 mL) was added triethylamine (4.68 mL, 33.59 mmol) and diphenylphosphonic azide (3.73 mL, 16.79 mmol). The reaction mixture was stirred at room temperature for 3 hours and then warmed to 80 0C for 2 hours. Water (10 mL) was added, and the mixture stirred at 80 0C for 15 hours. The reaction mixture was diluted with 300 mL of EtOAc, and the organic layer was washed with saturated aq. NaHCO3 solution and brine. The solvent was removed under reduced pressure and the residual purified via silica gel column chromatography eluting with 30/70 EtOAc/hexane to obtain 2.03 g (55%) of the title compound. 1H NMR (400 MHz, DMSO- d6) delta 9.32 (s, IH), 6.90-6.80 (m, IH), 6.51 (td, J=8.7, 5.5 Hz, IH), 5.28 (s, 2H), 3.05-2.96 (m, 2H), 1.82-1.64 (m, 2H), 1.01-0.90 (m, 3H). LC/MS: m/z 251.1 [M+l].

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 1103234-56-5.

Reference:
Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; ALIAGAS, Ignacio; GRADL, Stefan; GUNZNER, Janet; LEE, Wendy; MATHIEU, Simon; RUDOLPH, Joachim; WEN, Zhaoyang; ZHAO, Guiling; BUCKMELTER, Alexandre J.; GRINA, Jonas; HANSEN, Joshua D.; LAIRD, Ellen; MORENO, David; REN, Li; WENGLOWSKY, Steven Mark; WO2011/25938; (2011); A2;,
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Application of 18807-71-1, 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. 18807-71-1, name is Benzyl N-(2-aminoethyl)carbamate hydrochloride belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.

EXAMPLE 178; 4-[7-(2-Oxo-imidazolidin-1-yl)-quinazolin-4-yl]-piperidine-1-carboxylic acid (4-pyrrolidin-1-yl-phenyl)-amide; a. 4-[7-(2-Oxo-imidazolidin-1-yl)-quinazolin-4-yl]-piperidine-1-carboxylic acid tert-butyl ester; To a mixture of 4-(7-fluoro-quinazolin-4-yl)-piperidine-1-carboxylic acid tert-butyl ester (458 mg, 1.38 mmol), which was prepared as described in Example 65b, and (2-amino-ethyl)-carbamic acid benzyl ester hydrochloride (446 mg, 1.93 mmol) in DMSO (1.0 mL) was added K2CO3 (1.52 g, 11.04 mmol). The mixture was stirred at 115 C. overnight and subsequently partitioned between EtOAc and water. The combined organic extracts were washed with brine, dried over Na2SO4 and evaporated. The residue was purified by flash column chromatography on silica gel (EtOAc as eluent) to afford the desired product as a white solid (400 mg, 73%). 1H NMR (CDCl3) delta 9.13 (s, 1H), 8.69 (dd, J=9.40 and 2.35 Hz, 1H), 8.08 (d, J=9.53 Hz, 1H), 7.42 (d, J=2.33 Hz, 1H), 5.25 (br, 1H), 4.31 (m, 2H), 4.09 (t, J=8.21 Hz, 2H), 3.69 (t, J=8.14 Hz, 2H), 3.63 (m, 1H), 2.95 (m, 2H), 1.77-2.04 (4H), 1.48 (s, 9H). Calcd for C21H28N5O3 (MH+) 398.3, found 398.3.

The synthetic route of Benzyl N-(2-aminoethyl)carbamate hydrochloride has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Baindur, Nand; Gaul, Michael David; Kreutter, Kevin Douglas; Baumann, Christian Andrew; Kim, Alexander J.; Xu, Guozhang; Tuman, Robert W.; Johnson, Dana L.; US2006/281772; (2006); A1;,
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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. 16695-22-0, name is (Tosylazanediyl)bis(ethane-2,1-diyl) bis(4-methylbenzenesulfonate), A new synthetic method of this compound is introduced below., Quality Control of (Tosylazanediyl)bis(ethane-2,1-diyl) bis(4-methylbenzenesulfonate)

Synthesis of Intermediate XVI. To a solution of Tritosylate XV (1 g, 0.00176 moles, 1 eq) in 6 ml of DMF was added NaBr (0.93 g, 0.009 moles, 5 eq). The resulting suspension was stirred in an oil bath at 120 C. for 4 h. After cooling to room temperature, the reaction mixture was concentrated to about 2 ml. The viscous milky product was poured into rapidly stirred mixture of ice-water (30 ml) and extracted with ethyl acetate (30 ml). The organic phase was dried (Na2SO4) and concentrated under reduced pressure. The crude product was purified by column chromatography (silica gel, 60-120 mess, 10% ethyl acetate in hexane) to leave the product XVI as a pale yellow liquid (0.34 g, 51%) 1H NMR (400 MHz, CDCl3) 2.41 (s, 3H), 3.44 (s, 8H), 7.38 (d, 4H), 7.76 (d, 4H)

The synthetic route of 16695-22-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Salituro, Francesco G.; Saunders, Jeffrey; Yan, Shunqi; US2012/172349; (2012); A1;,
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