Amides-buliding-blocks

Related Products of 35303-76-5, A common heterocyclic compound, 35303-76-5, name is 4-(2-Aminoethyl)benzenesulfonamide, molecular formula is C8H12N2O2S, 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: One equivalent (eq) of starting dichlorotriazinyl benzenesulfonamide(1, 2 or 3) [3] was dissolved in DMF as a solvent. Then 1 eq of solid anhydrous potassium carbonate was added in portions. After 10 min of stirring 1 eq of the appropriate nucleophile was addedalso in portions. Reaction was stirred at 35°C until disappearance of starting material (monitored by TLC: CH3OH was used as eluent,detection with UV light and ninhydrin). After completion of the reaction was crushed ice added to the reaction mixture and the precipitate formed was collected by filtration. Purification of a crude product was made by its solution in acetone and pure product was precipitated by addition of isopropyl alcohol.

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference:
Article; Havrankova, Eva; Csoellei, Jozef; Vullo, Daniela; Garaj, Vladimir; Pazdera, Pavel; Supuran, Claudiu T.; Bioorganic Chemistry; vol. 77; (2018); p. 25 – 37;,
Amide – Wikipedia,
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Application of 154350-29-5, 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 154350-29-5 as follows.

A mixture of 2-(3-fluoro-5-pyrrolidin-1-yl-phenyl)-3,3-dimethyl-1,2,3,4-tetrahydro-quinoline-6-carboxylic acid (50 mg, 0.14 mmol), 1-3-dimethylaminopropyl-3-ethylcarbodiimide hydrochloride (39 mg, 0.20 mmol), 4-dimethylaminopyridine (24.4 mg, 0.20 mmol), cyclopropanesulfonic acid amide (51 mg, 0.42 mmol) in dichloromethane (3 mL) was heated for 12 hours at 60° C. Removal of the solvent afforded an oil residue. Purification by Waters automated flash system (column: Xterra 30 mm.x.100 mm, sample manager 2767, pump 2525, detector: ZQ mass and UV 2487, solvent system: acetonitrile and 0.1percent formic acid in water) afforded cyclopropanesulfonic acid [2-(3-fluoro-5-pyrrolidin-1-yl-phenyl)-3,3-dimethyl-1,2,3,4-tetrahydro-quinoline-6-carbonyl]-amide (13 mg, 20percent) as a light yellow solid: LC/MS m/e calcd for C25H30FN3O3S (M+H)+: 472.6, observed: 472.2.

According to the analysis of related databases, 154350-29-5, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Chen, Li; Feng, Lichun; Huang, Mengwei; Liu, Yongfu; Wu, Guolong; Wu, Jim Zhen; Zhou, Mingwei; US2011/257151; (2011); 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. 1520-70-3, name is Ethanesulfonamide, A new synthetic method of this compound is introduced below., HPLC of Formula: C2H7NO2S

Example 19: 5-(4-CHLOROPHENYL)-6-CYCLOHEXYL-N-(ETHYLSULFONYL)-4-(2- MORPHOLIN-4-YL-2-OXOETHYL)-4H-THIENO [3, 2-B] PYRROLE-2-CARBOXAMIDE; A solution (0.015 M) of 5- (4-CHLOROPHENYL)-6-CYCLOHEXYL-4- (2-MORPHOLIN-4- YL-2-OXOETHYL)-4H-THIENO [3, 2-B] PYRROLE-2-CARBOXYLIC acid in THF at RT was treated with CDI (1. 1 eq. ) and DMAP (1.1 eq. ). After stirring for 1H at RT, ETHANESULFONAMIDE (2 eq. ) and DBU (2 eq. ) were added. The mixture was heated to reflux for 5 h then cooled down and diluted with AcOEt. The organic phase was washed with aqueous HC1 (0.1 N) and dried. Evaporation of the solvent under reduced pressure gave a residue which was purified by RP-HPLC (Conditions : Waters X-TERRA MS C18,10 micron, 19 x 100 mm ; flow : 20 ML/MIN ; Gradient : A: H20 + 0.05percent TFA ; B : MECN + 0.05percent TFA ; 50percent A isocratic for 1 min then linear to 20percent A in 9 min) to afford the title compound (17percent) as a solid. ‘H NMR (400 MHz, DMSO-d6, 300 K) 8 1. 1-1.3 (m, 7H), 1.5-1. 8 (m, 8H), 2.44 (m, 1H), 3.4-3. 6 (m, 8H), 4.83 (s, 2H), 7.33 (d, J = 8.0 Hz, 2H), 7.61 (d, J = 8. 0 Hz, 2H), 8. 07 (s, 1H), 11.91 (bs, 1H); MS (ES+) M/Z 578, 580 (M+H) +.

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference:
Patent; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPA; WO2005/23819; (2005); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Synthetic Route of 207405-68-3, 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. 207405-68-3, name is tert-Butyl endo-3-amino-8-azabicyclo[3.2.1]octane-8-carboxylate belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.

To a solution of compound ii-35a (5.00 g, 22.19 mmol) in methanol (100 mL) and water (10 mL) were added ammonium formate (13.99 g, 222 mmol) and 10%-palladium/carbon (2.362 g) in turn. The resultant was stirred at room temperature for 2 days. Celite was used to filtrate the reaction liquid, and then the filtrate was diluted with chloroform, washed with an aqueous sodium hydroxide solution and a saturated salt solution, and dried over magnesium sulfate. Magnesium sulfate was filtrated off, and then the liquid was concentrated under reduced pressure to yield compound ii-35b (5.60 g). Compound ii-35b yielded was used as it was, without being purified, in the next reaction.The total amount of compound ii-35b yielded was dissolved in methanol (50 mL) and acetic acid (5 mL). Thereto were then added a 36% aqueous formalin solution (8.49 mL, 111 mmol) and hydrogenated sodium triacetoxyborate (9.41 g, 44.4 mmol) in turn. The resultant was stirred at room temperature for 1 hour. To the reaction liquid was added an 8 N aqueous sodium hydroxide solution to set the pH thereof to 10. Thereafter, this liquid system was subjected to extraction with chloroform. To the organic phase was added a 0.5 N aqueous hydrochloric acid solution, and then the liquid-system was separated to two phases. Thereafter, the water phase was made into basicity, and then subjected to extraction with chloroform. The organic phase was washed with a saturated salt solution, and dried over magnesium sulfate. Magnesium sulfate was filtrated off, and then the organic phase was concentrated under reduced pressure to yield compound ii-35c (2.43 g, 43%).1H-NMR (CDCl3) delta: 4.16 (2H, d, J = 29.04 Hz), 2.22 (6H, s), 2.12-1.59 (9H, m), 1.46 (9H, s).

The synthetic route of tert-Butyl endo-3-amino-8-azabicyclo[3.2.1]octane-8-carboxylate has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Shionogi & Co., Ltd.; HISAKAWA, Shinya; HASEGAWA, Yasushi; AOKI, Toshiaki; KUSANO, Hiroki; SANO, Masayuki; SATO, Jun; YAMAWAKI, Kenji; EP2557082; (2013); 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. 42137-88-2, name is N,N-Bis(2-chloroethyl)-4-methylbenzenesulfonamide, This compound has unique chemical properties. The synthetic route is as follows., Recommanded Product: N,N-Bis(2-chloroethyl)-4-methylbenzenesulfonamide

3.4 g (0.0156 mole) of levorotatory (-)-(4-chlorophenyl)phenylmethylamine(prepared in accordance with Example 1.1 of U.S. Patent No. 5478941 ) and 5.1 g(0.0172 mol) of N,N-bis(2-chloroethyl)-4-methylbenzenesulfonamide (prepared inExample 2.3 of U.S. Patent No. 5478941 ) in 6 ml_ (4.4 g or 0.0343 mol) of ethyldiisopropylamine are mixed in a 25 ml_ round-bottomed flask. The mixture is heated under reflux (127 0C) for 4 hours and then cooled, with stirring, to 86 0C and 13.8 ml_ of methanol are added at once. The mixture is then cooled in an ice bath and still stirred for 1 hour. The precipitate which forms is filtered off, washed with 10 ml_ of methanol and dried under vacuum at 40 0C. The product is recrystallized from a 3:1 (v/v) mixture of methanol and acetone. 6 g of levorotatory(-)-1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl)sulfonyl]piperazine are obtained.M. P: 171.1 0C. Yield: 87.2%.[alpha]D25: -40.68 (c=1 , toluene)Optical purity: 100%Analysis for C24H25CIN2O2S in %:CaIc: C 65.37, H 5.71 , N 6.35, Cl 8.04, S 7.27Found: C 65.95, H 5.80, N 6.60, Cl 8.12, S 7.33

According to the analysis of related databases, 42137-88-2, the application of this compound in the production field has become more and more popular.

Reference:
Patent; DR. REDDY’S LABORATORIES LTD.; DR. REDDY’S LABORATORIES, INC.; RAMAYYA, Vaddadi Pattabhi; WO2009/62036; (2009); A2;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Related Products of 85006-25-3,Some common heterocyclic compound, 85006-25-3, name is tert-Butyl (tert-butoxycarbonyl)oxycarbamate, molecular formula is C10H19NO5, 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.

Tert-butyl (tert-butoxycarbonyl)oxycarbamate (70 mg) and 1- (bromomethyl) -2-fluorobenzene (56.7 mg) were dissolved in CH 2Cl 2(7 ml) . The mixture was added 1M NaOH (0.33 ml) and tetrabutylammonium bromide(4.83 mg) , and stirred at room temperature for overnight. The resulting mixture was washed with water and dried with Na 2SO 4, concentrated in vacuo and purification by silica gel chromatography to give tert-butyl ( (tert-butoxycarbonyl) oxy) (2-fluorobenzyl) carbamate (82 mg, 80%) . 1HNMR (400 MHz, CDCl 3): delta 7.31-7.37 (m, 4H) , 4.52(s, 2H) , 1.46 (s, 9H) , 1.44 (s, 9H) .

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route tert-Butyl (tert-butoxycarbonyl)oxycarbamate, its application will become more common.

Reference:
Patent; SU, Yaning; SIRONAX LTD; ZHANG, Zhiyuan; YANG, Yi; WANG, Guozheng; LIU, Wendong; MA, Yongfen; REN, Yan; (74 pag.)WO2020/103859; (2020); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

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 35303-76-5 as follows. name: 4-(2-Aminoethyl)benzenesulfonamide

To solid reagents 4-(2-aminoethyl)benzenesulfonamide (2.00 g, 9.99 mmol) and dihydrofuran-2,5-dione (0.999 g, 9.99 mmol) was added THF (30 mL). The reaction mixture was stirred at 60 C for 7 hrs. Solvent was evaporated under reduced pressure to give 4-oxo-4-((4- sulfamoylphenethyl)amino)butanoic acid (3.00 g, 9.99 mmol, 100 % yield) as a white solid.1H NMR (400 MHz, DMSO-d6) delta 12.09 (s, 1H), 7.96 (t, J = 5.6 Hz, 1H), 7.72 (d, J = 8.1 Hz, 2H), 7.38 (d, J = 8.1 Hz, 2H), 7.29 (s, 2H), 3.26 (q, J = 6.8 Hz, 2H), 2.76 (t, J = 7.2 Hz, 2H), 2.40 (t, J = 6.9 Hz, 2H), 2.27 (t, J = 6.9 Hz, 2H); MS (ESI), 301.1 (M+H)+.

According to the analysis of related databases, 35303-76-5, the application of this compound in the production field has become more and more popular.

Reference:
Patent; WAVE LIFE SCIENCES LTD.; ZHANG, Jason Jingxin; SHIVALILA, Chikdu Shakti; VARGEESE, Chandra; IWAMOTO, Naoki; (469 pag.)WO2019/75357; (2019); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Application of 112101-81-2,Some common heterocyclic compound, 112101-81-2, name is R-5-(2-Aminopropyl)-2-methoxybenzenesulfonamide, molecular formula is C10H16N2O3S, 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.

Into a 4-necked 500ml round bottom flask, equipped with Dean-stark apparatus 150.0ml of toluene, 24.4gms of (R)-5-(2-aminopropyl)-2-methoxy benzene sulfonamide of the formula-IV and 12.4gms (0.1mole) of 4-fluorobenzaldehyde are charged. The reaction is effected azeotropically and the water 1.8ml (0.1mole) is separated. Then the toluene is distilled off completely under vacuum at temp max 80C. Cooled 25-35C and released the vacuum under nitrogen atmosphere – 25.0gm of thick oily compound of 2-methoxy-5-(2R)-2-{[(1-E/Z-4-fluorophenylpmethylene)amino] propyl} benzenesulfonamide of formula-IIId is obtained. Recrystallized sample (from IPA) has the following characteristics MR : 140-148C 1H NMR : (200MHz, CDCl3+DMSO-d6) delta 1.01-1.04 (d, 3H), 2.80-2.88 (t, 2H), 3.14 – 3.18 (m, 1H), 3.88 (s, 3H), 6.0, (broad, 2H), 7.12-7.57 (aromatic, 7H), 8.20 (s, imine, 1H) IR : (KBr), 3385, 3315, 2948, 1643, 1606, 1576, 1495, 1404, 1334, 1249, 1154, 1074, 1114, 518, 471cm-1

The synthetic route of 112101-81-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; NATCO PHARMA LIMITED; WO2004/16582; (2004); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Electric Literature of 116861-31-5, 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 116861-31-5 as follows.

Synthesis of compound 22: the aforementioned compound 20 (0.120 g, 0.00049 mol, 1 eq) was solubilised in DMF (3 ml). To the solution was added the aforementioned compound 21 (0.104 g, 0.00054 mol, 1.1 eq) solubilised in DMF (2 ml). The reaction mixture was stirred under reflux for 6 hours. The structure of the product was evaluated by TLC CH2Cl2 9/MeOH 1/NH4OHaq 33% 0.03. The solvent was evaporated, and the oily residue was purified by flash chromatography using a mixture of CH2Cl2 9/MeOH 1/NH4OHaq 33% 0.03 as the eluent phase. 0.084 mg of a yellow oil were obtained. Yield 42.71%. 1H NMR (400 MHz, CDCl3) delta 0.87 (d, 6H, J=6.8 Hz), 1.43 (s, 18H), 1.57-1.61 (m, 7H), 1.98-2.01 (m, 2H), 2.31-2.35 (m, 2H), 2.38-2.42 (m, 2H), 3.10-3.12 (m, 2H), 3.16-3.18 (m, 2H), 4.72 (brs, 1H, exch D2O), 5.69 (brs, 1H, D2O exch.).

According to the analysis of related databases, 116861-31-5, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Giuliani, Giammaria; Paus, Ralf; Benedusi, Anna; Marzani, Barbara; Baroni, Sergio; US2015/202132; (2015); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Adding a certain compound to certain chemical reactions, such as: 6325-93-5, name is 4-Nitrobenzenesulfonamide, 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 6325-93-5, COA of Formula: C6H6N2O4S

Step 1 – Tert-butyl N-(4-nitrophenyl)sulfonylcarbamate (0596) [00375] To a solution of 4-nitrobenzenesulfonamide (5.00 g, 24.7 mmol) in anhydrous dichloromethane (40 mL) was added triethylamine (5.00 g, 49.4 mmol) and catalytic amount of N,N-dimethylpyridin-4-amine. The mixture was cooled to 0 C and di-tert-butyl dicarbonate (5.67 g, 25.9 mmol) was added over 10 min. Then the mixture was warmed to 18 C and stirred for 50 min. On completion, the reaction mixture was quenched with ice water (40 mL). Afterwards, the organic phase was separated, washed with brine (20 mL), dried over anhydrous sodium sulfate and concentrated in vacuo to give a residue. The residue was purified by column chromatography (petroleum ether:ethyl acetate = 3:1 to 1:1) to give the title compound.1H NMR (400MHz, CDCl3) delta = 8.44 – 8.40 (m, 2H), 8.28 – 8.24 (m, 2H), 1.43 (s, 9H).

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; RAZE THERAPEUTICS, INC.; MAINOLFI, Nello; MOYER, Mikel P.; SAIAH, Eddine; (264 pag.)WO2017/156181; (2017); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics