Category: amides-buliding-blocks

These common heterocyclic compound, 162787-61-3, name is 2-(Methylsulfonamido)benzoic acid, 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. COA of Formula: C8H9NO4S

Thereafter, 40 g of Synthesis Intermediate A, 26 g of salicylamide and 2 mL of DMF (N,N-dimethylformamide) were added to 800 mL of toluene, and 22 g of thionyl chloride was added dropwise at room temperature. This solution was stirred at 85 C. for 2 hours, and 3.9 g of p-toluenesulfonic acid monohydrate was added, followed by stirring at 130 C. for 5 hours. The resulting reaction solution was cooled to 60 C. and after adding 30 mL of triethylamine, cooled to room temperature. To this solution, 300 mL of methanol was added, and the obtained solid was filtered and washed with methanol to obtain 52 g of Synthesis Intermediate B (yield: 88%).

The synthetic route of 2-(Methylsulfonamido)benzoic acid has been constantly updated, and we look forward to future research findings.

Reference:
Patent; FUJIFILM CORPORATION; US2012/53343; (2012); A1;,
Amide – Wikipedia,
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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. 159184-15-3, name is tert-Butyl 2-(4-aminophenoxy)ethylcarbamate, This compound has unique chemical properties. The synthetic route is as follows., Safety of tert-Butyl 2-(4-aminophenoxy)ethylcarbamate

Step F. tert-Butyl 2-{4-[(1-benzyl-4-piperidinyl)amino]phenoxy}ethylcarbamate tert-Butyl 2-(4-aminophenoxy)ethylcarbamate (2.34 g, 9.27 mmol) and benzyl piperidone (2.6 g, 13.74 mmol) were dissolved in dichloroethane (40 mL). Anhydrous sodium sulfate (13.2 g) was added followed by acetic acid (2.6 mL). Stirring was continued for 1 hour. Sodium triacetoxyborohydride (3.93 g, 18.54 mmol) was added and stirring continued overnight. The mixture was filtered, diluted with dichloromethane (600 mL), and washed with 40percent sodium hydroxide, water and brine. The organic phase was dried over anhydrous magnesium sulfate. The solution was filtered and the solvent evaporated to dryness in vacuo. The residue was purified by flash chromatography on silica gel Merck-60 (eluant: 20:1 chloroform-methanol). The solvent was removed in vacuo and the resulting oil triturated with hexane to furnish the title compound (2.4 g, 5.64 mmol). MS ((+)ESI, m/z): 426 [M+H]+

According to the analysis of related databases, 159184-15-3, the application of this compound in the production field has become more and more popular.

Reference:
Patent; American Home Products Corporation; US2002/28832; (2002); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

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. 5004-88-6, name is 2-Amino-4,5-dimethoxybenzamide belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below. Recommanded Product: 2-Amino-4,5-dimethoxybenzamide

General procedure: A mixture of 2-chlorobenzoic acid (1b) (0.61 g, 3.92 mmol) and thionyl chloride (1 mL) was heated for 2 h. The excess of thionyl chloride was recovered under reduced pressure and the residue so obtained was dissolved in dry dioxane (1 mL). The solution was then dropwise added to mixture of 2-amino-4,5-dimethoxybenzamide (2) (0.7 g, 3.57 mmol) and TEA (1.2 mL, 8.92 mmol) in dry dioxane (2 mL) at 10 C. The reaction mixture was stirred at rt for another 1 h and quenched into cold water (50 mL). The precipitate formed was filtered, washed with water and dried to obtain compound 3b (0.85 g, 71%).

The synthetic route of 5004-88-6 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Yadav, Mange R.; Grande, Fedora; Chouhan, Bishram S.; Naik, Prashant P.; Giridhar, Rajani; Garofalo, Antonio; Neamati, Nouri; European Journal of Medicinal Chemistry; vol. 48; (2012); p. 231 – 243;,
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Electric Literature 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.

2.6. Tamsulosin; I IV yield 50% 11 220 g (0.88 mol) of intermediate IV and 84 g (0.79 mol) of sodium carbonate and N, N- dimethylformamide (1500 ml) are added to 208 g (0.85 mol) of intermediate I. The reaction mixture is stirred at 70 C for 5 hours. Water is added to the reaction mixture and product II is extracted with ethylacetate. The evaporation residue is stirred in ethanol and after sucking off, the yield is 173.9 g (50 %) of crude base II. The method according to CZ 291802. The yield is, for comparison, also calculated on the crude base. The reaction takes place at 60 to 70 C for 5 hours and the product is not purified with the demanding column chromatography.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route R-5-(2-Aminopropyl)-2-methoxybenzenesulfonamide, its application will become more common.

Reference:
Patent; ZENTIVA, A.S.; WO2005/75415; (2005); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

These common heterocyclic compound, 5466-88-6, name is 2H-1,4-Benzoxazin-3(4H)-one, 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. Recommanded Product: 2H-1,4-Benzoxazin-3(4H)-one

To a stirred solution of 4H-Benzo[1 ,4]oxazin-3-one (2.5 g, 16.77 mmol) in DMF (10 mL) was added potassium tert-butoxide (2.81 g, 25.16 mmol) at 0 C. After stirring for 5 min, methyl iodide (3.54 g, 25.16 mmol) was added and the reaction mixture was stirred for another 3h. The reaction was quenched by addition of water and extracted with ethyl acetate (30 x 2 ml). The organic layer was washed with water (20 mL), and evaporated to get a crude product 2.2 g.

The synthetic route of 2H-1,4-Benzoxazin-3(4H)-one has been constantly updated, and we look forward to future research findings.

Reference:
Patent; NOVARTIS AG; BEBERNITZ, Gregory Raymond; BOCK, Mark G.; BHUNIYA, Debnath; DATRANGE, Laxmikant; KURHADE, Suresh Eknath; PALLE, P. Venkata; REDDY, Dumbala Srinivas; WO2011/48148; (2011); A2;,
Amide – Wikipedia,
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Application of 2895-21-8, 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. 2895-21-8, name is N-Isopropyl-2-chloroacetamide belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.

(3) A mixed solution of the compound 4 (150 mg), the compound 5 (11 mg), and sodium carbonate (87 mg) in acetonitrile (5 mL) was stirred for 18 hours at 50C under argon atmosphere. The reaction mixture was cooled to room temperature, diluted with ethyl acetate, washed with water, and dried over Chem Elut (registered trademark). The solvent was distilled off under reduced pressure, and the resultant residue was purified by silica gel column chromatography (eluent: chloroform-methanol; gradient: 100:0-95:5). The resultant residue was suspended and washed in ethyl acetate to give the compound 6 (77 mg) as a yellow solid. MS (APCI) 366 [M+H]+

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles, N-Isopropyl-2-chloroacetamide, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Mitsubishi Tanabe Pharma Corporation; SAKAKIBARA, Ryo; USHIROGOCHI, Hideki; SASAKI, Wataru; ONDA, Yuichi; YAMAGUCHI, Minami; AKAHOSHI, Fumihiko; (69 pag.)EP3381904; (2018); A1;,
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Reference of 4141-08-6, These common heterocyclic compound, 4141-08-6, name is 2-Amino-N-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: The 2-aminobenzamide (1 equiv), the orthoester (2-3 equiv) and absolute ethanol (2-3 mL) wereplaced in a 15-mL Chemglass screw-cap pressure tube (No. CG-1880-01, Chemglass, Vineland, NJ,USA). Glacial acetic acid (3 equiv) was added, N2 was introduced to the vessel and the cap wastightened. The vessel was heated at 110 C for 12-72 h, then cooled and concentrated to give thequinazolinone, which was purified by crystallization from absolute ethanol or trituration from 5%ether in pentane. The following compounds were prepared:

The synthetic route of 4141-08-6 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Gavin, Joshua T.; Annor-Gyamfi, Joel K.; Bunce, Richard A.; Molecules; vol. 23; 11; (2018);,
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. 672-58-2, name is 3-(Trifluoromethyl)benzenesulfonamide, This compound has unique chemical properties. The synthetic route is as follows., COA of Formula: C7H6F3NO2S

General procedure: To a stirred solution of glucal (1 equiv.) and N-nucleophile (1.1 equiv.) inanhydrous 1,2-dichloroethanne (2 mL/mmol) under an atmosphere of argon was added Zn(OTf)2 (10 mol%) at 40?C. The reaction mixture was stirred untilthe complete consumption of the starting material (glycal). The solvent wasfiltered and concentrated in vacuo, and the crude residue was redissolved indichloromethane and loaded on a silica gel column. The product was purified by silica gel column chromatography using hexane/EtOAc as the eluent to affordthe 2,3-unsaturated N-glycosides. All of the products were confirmed by1H NMR, 13C NMR, and MS/HRMS spectroscopy and compared with that of literature data; characterization data of new products are outlined in the experimentalsection

According to the analysis of related databases, 672-58-2, the application of this compound in the production field has become more and more popular.

Reference:
Article; Reddy, Thurpu Raghavender; Battina, Suresh Kumar; Kashyap, Sudhir; Journal of Carbohydrate Chemistry; vol. 34; 3; (2015); p. 133 – 144;,
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. 24036-52-0, name is 6-Bromo-2H-1,4-benzoxazin-3(4H)-one, A new synthetic method of this compound is introduced below., COA of Formula: C8H6BrNO2

A mixture of 6-bromo-2H-benzo[b][1,4]oxazin-3(4H)-one (197 mg, 0.864 mmol), (S)-3-phenylmorpholine (172.7 mg, 1.058 mmol), 2-(dicylclohexylphosphino)-2′-(N,N-dimethylamino)biphenyl (11.2 mg, 0.028 mmol), tris(dibenzylideneacetone)dipalladium (0) (8.9 mg, 0.01 mmol), tetrahydrofuran (3.3 mL) and lithium bis(trimethylsilyl)amide in tetrahydrofuran (1 M, 1.93 mL, 2 mmol) was stirred at 70 C. overnight. The mixture was cooled to room temperature and saturated aqueous ammonium chloride and ethyl acetate were added. The layers were separated and the aqueous layer was extracted with ethyl acetate (3*). The organic layers were combined, dried over magnesium sulfate, filtered, and concentrated. The residue was purified by silica gel column chromatography (gradient: 0-25% ethyl acetate in heptanes) to afford the title compound (105.6 mg, 39.4%). 1H NMR (400 MHz, CHLOROFORM-d) delta ppm 3.01(1H, ddd, J=12.2, 9.3, 4.3 Hz), 3.29 (1H, m), 3.54 (1H, dd, J=11.4, 8.9 Hz), 3.92 (3H, m), 4.15 (1H, m), 4.48 (2H, s), 5.28 (1H, s), 6.37 (1H, d, J=2.5 Hz), 6.56 (1H, m), 6.72 (1 H, d, J=8.8 Hz), 7.16 (3H, m), 7.26 (1H, m), 7.24 (2H, s), 7.97 (1H, s).

The synthetic route of 24036-52-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Pfizer Inc; US2011/281854; (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. 915087-25-1, name is 4-Amino-2-fluoro-N-methylbenzamide, A new synthetic method of this compound is introduced below., category: amides-buliding-blocks

Example 3: Preparation of formula 4 TMSCN [74 g] was combined with N-methyl-2-fluro-4-aminobenzamide [formula 3, 50 g] in a clean and dried RBF. Acetic acid [250 ml] was slowly added dropwise to create frothing. Next, acetone [250 ml] was added and the reaction mass was heated to about 85 C. Heating continued until the reaction was complete. Next, the solvents were completely distilled off under vacuum (680 + 30 mm Hg). The resultant solid residue was cooled to room temperature, water [1000 ml] was added to the residue, and the reaction mass was stirred to get a free-flowing solid. The solid was filtered and washed with water to form a slurry. The slurry was then washed with tert-butyl methyl ether (TBME). The filtered cake was suck dried and the product dried under vacuum to result in formula 4.

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; MYLAN LABORATORIES LTD; WAGH, Ghanshyam; BODUPALLI, Murali; YEWALE, Sampat; DHANANJAY, Shinde; GADAKAR, Mahesh Kumar; GORE, Vinayak; DANDALA, Ramesh; (19 pag.)WO2016/38560; (2016); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics