Amides-buliding-blocks

Application of 117009-97-9,Some common heterocyclic compound, 117009-97-9, name is Benzyl 1,4-diazepane-1-carboxylate, molecular formula is C13H18N2O2, 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.

Compound BB-18-3 (1.8g crude) was dissolved in dilute hydrochloric acid (6M, 40mL) was stirred until uniform, slowly under nitrogenwas added dropwise sodium nitrite solution (2N, 17mL), then stirred at room temperature for 1 hour, 50mL of water was added, extracted with ethyl acetate(60mL ¡Á 3).The combined organic phases with saturated brine (20 mL), dried over anhydrous sodium sulfate, the solvent was removed under reduced pressure to give the titlecompound BB-18-4 (2g crude) was used directly in the next step without further purification.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route Benzyl 1,4-diazepane-1-carboxylate, its application will become more common.

Reference:
Patent; Changzhou Yin Sheng Pharmaceutical Co., Ltd.; Sichuan University; Zhang, Yang; Fu, Zhifei; Li, Jian; Chen, Shuhui; Wei, Yuquan; Tao, Xin; (65 pag.)CN105732602; (2016); A;,
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Application of 154350-29-5,Some common heterocyclic compound, 154350-29-5, name is Cyclopropanesulfonamide, molecular formula is C3H7NO2S, 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.

To a solution of (22E)-3-oxo-4,6,22-cholatrien-24-oic acid (2.00 g, 5.43 mmol) in CH2CI2(40 mL) was added EDCI (1.69 g, 10.9 mmol) and DMAP (1.33 g, 10.9 mmol).Cyclopropane sulfonamide (1.97 g, 16.3 mmol) was added and the reaction was stirred at room temperature for 22 h. Water (25 mL) was added and the layers were separated. The aqueous layer was extracted with CH2CI2 (2 x 25 mL) and the combined organics were washed with 2 M aq HCI (20 mL), 10percent aq. NaCI (10 mL), dried over sodium sulfate andconcentrated under reduced pressure. The residue was purified by column chromatography on silica gel (0-10percent acetone in toluene) to give the desired product (1.68 g, 66percent) asan off-white solid. OH (400 MHz, CDCI3); 8.90 (1H, s, NH), 6.95 (1H, dd, J15.5,9.0, 023-OH), 6.11 (2H, brs, 06-OH and 07-OH), 5.86 (1H, dd, J15.5, 0.5, 022-OH), 5.68 (1H, s, 04-OH), 3.00 (1H, dddd, J 12.8, 9.5, 8.1, 4.8, SO2OH), 2.64 (1H, ddd, J 18.1, 14.4,5.4, O2OHaHb), 2.51-2.41 (1H, m, 02-OHaHb), 2.40-2.28 (1H, m), 2.25-2.15 (1H, m), 2.09-1.96 (2H, m), 1.85-1.64 (3H, m), 1.63-1.52 (1H, m), 1.51-1.17 (9H, m), 1.17-1.07 (5H, m),1.12 (3H, s, 019-OH3), 0.80 (3H, s, 018-OH3); 00 (100 MHz, 0D013); 200.0, 164.2, 164.1,155.5, 141.3, 127.9, 123.6, 119.4,54.7, 53.2, 50.6, 43.8, 39.8, 39.3, 37.8, 36.1, 33.9, 33.9,31.5, 28.1, 23.7, 20.6, 19.1, 16.3, 12.2, 6.3, 6.3.

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

Reference:
Patent; NZP UK LIMITED; WEYMOUTH-WILSON, Alexander Charles; KOMSTA, Zofia; WALLIS, Laura; EVANS, Timothy; (139 pag.)WO2017/199036; (2017); A1;,
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Reference of 75178-90-4,Some common heterocyclic compound, 75178-90-4, name is tert-Butyl (5-hydroxypentyl)carbamate, molecular formula is C10H21NO3, 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.

To a stirred mixture of tert-butyl 5-hydroxypentylcarbamate (2)(9.8 g, 48.2 mmol) and triethyl amine (13.44 mL, 96.0 mmol) in DCM (85 mL) at-10 oC was added methanesulfonyl chloride (4.5 mL, 57.9 mmol) in adropwise fashion and the resulting solution was stirred at the same temperaturefor 3h. The reaction was quenched with the addition of water (5 mL). Theorganic phase was washed with water, brine, dried over MgSO4,filtered and evaporated under reduced pressure to afford the title compound asyellow oil (13.16g, 97%). The product was directly taken to next step withoutany further purification. 1H NMR(CDCl3) d 4.22 (t, 2H, J = 6.42 Hz), 3.09 (m, 2H), 1.82 (m, 4H), 1.56-1.40(m, 11H). 13C NMR (75 MHz, CDCl3) d 155.8, 79.3, 70.0,41.8, 37.9, 29.8, 28.3, 22.5. IR: 2981, 1707, 1516, 1354, 1171 cm-1. MS m/z (ESI) 304.26 (M +Na+).

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 (5-hydroxypentyl)carbamate, its application will become more common.

Reference:
Article; Maharvi, Ghulam M.; Bharucha, Adil E.; Fauq, Abdul H.; Bioorganic and Medicinal Chemistry Letters; vol. 23; 9; (2013); p. 2808 – 2811;,
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Related Products of 2675-89-0,Some common heterocyclic compound, 2675-89-0, name is 2-Chloro-N,N-dimethylacetamide, molecular formula is C4H8ClNO, 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: Under molecular oxygen atmosphere, to a mixture of Pd(OAc)2 (1.3 mg, 0.006 mmol) and bpy (0.9 mg, 0.006 mmol), toluene (2.0 mL) was added. Then aniline (0.2 mmol), amide (2.0 mmol), PivOH (40.9 mg, 0.4 mmol), and BF3Et2O (42.6 mg, 0.3 mmol) were added to the mixture. The mixture was heated to 120 C and it stirred at 120 C for 24 h. After completion, the mixture was cooled to room temperature and diluted with ethyl acetate. Washed withaq NaHCO3, water, and aq NaCl. Dried over MgSO4 and filtered. Aftere vaporation of the solvent, the residue was purified by preparative thin-layer chromatography on silica gel with PE/EtOAc (1/1) as aneluent to give the product 3.

The synthetic route of 2675-89-0 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Gu, Da-Wei; Guo, Xun-Xiang; Tetrahedron; vol. 71; 48; (2015); p. 9117 – 9122;,
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6228-73-5, name is Cyclopropanecarboxamide, 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. Application In Synthesis of Cyclopropanecarboxamide

The product from step 1 (30 mg, 0.080 mmol), cyclopropanecarboxamide (13.59 mg, 0.160 mmol), Xantphos (9.24 mg, 0.016 mmol)And cesium carbonate (78 mg, 0.239 mmol)The mixture in dioxane (0.8 mL) was purged for 5 min,Then Pd2 (dba) 3 (7.31 mg, 7.98 mumol)And the reaction was placed in a preheated chamber at 130 C for 1 h. The reaction mixture was then cooled and diluted with DMSO and purified by reverse phase preparative LCMS using the following conditions: Column: Waters XBridge C18, 19 x 200 mm, 5 mum particles; mobile phase A: 5: 95 acetonitrile: water MM ammonium acetate); mobile phase B: 95: 5 acetonitrile: water (with 10 mM ammonium acetate); gradient: 0-100% B over 20 minutes and then at 100% B for 0 min; flow rate: 20 mL / min The The fractions containing the desired product are combined and dried by centrifugal evaporation. The yield of the product was 26.3 mg (69%).

The synthetic route of 6228-73-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; MOSLIN,, RYAN M.; WEINSTEIN,, DAVID S.; WROBLESKI,, STEPHEN T.; ZHANG,, YANLEI; TOKARSKI,, JOHN S.; MERTZMAN,, MICHAEL E.; LIU,, CHUNJIAN; (124 pag.)TWI582077; (2017); B;,
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Electric Literature of 111300-06-2, 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. 111300-06-2, name is tert-Butyl (trans-4-hydroxycyclohexyl)carbamate belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.

To a mixture of lithium aluminium hydride (9 g, 0.23 mol) in tetrahydrofuran (425 mL) was added slowly tert-butyl (trans-4-hydroxycyclohexyl)carbamate (intermediate 1, 10 g, 0.046 mol). The mixture was refluxed overnight. Once the mixture was cooled to room temperature, 9 ml of water, 9 ml of 4N NaOH solution and 18 ml of water were carefully and successively dropped. The organic solvent was removed under reduced pressure and the crude obtained was dissolved with chloroform and dried over magnesium sulphate. The filtrate was evaporated to dryness and co evaporated with hexane to give the title compound as a white solid (89%). This intermediate is also described in . 1H NMR (300 MHz, CHLOROFORM-d) delta ppm 1.04 – 1.20 (m, 2 H) 1.25 – 1.40 (m, 2 H) 1.97 (br. s., 4 H) 2.27 – 2.40 (m, 1 H) 3.57 – 3.70 (m, 1 H)

The synthetic route of tert-Butyl (trans-4-hydroxycyclohexyl)carbamate has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Almirall, S.A.; Aiguade Bosch, Jose; Gual Roig, Silvia; Prat Quinones, Maria; Puig Duran, Carlos; EP2592077; (2013); 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. 53844-02-3, name is Benzyl (2-bromoethyl)carbamate belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below. Recommanded Product: 53844-02-3

Step 2 Synthesis of 3-(2-aminoethoxy)benzonitrile hydrobromide: 8 g of benzyl-N-(2-bromoethyl)carbamate, 3.7 g of 3-hydroxybenzonitrile, 4.3 g of calcium carbonate, 5.1 g of potassium iodide and 1.1 g of tetrabutylammonium iodide were stirred in dimethylformamide at 60C. After the treatment with ethyl acetate as the extractant in an ordinary manner, the product was purified by the silica gel column chromatography to obtain 3-[2-(benzyloxycarbonylamino)ethoxy]benzonitrile.

The synthetic route of 53844-02-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Ajinomoto Co., Inc.; EP976722; (2000); A1;,
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These common heterocyclic compound, 174799-52-1, name is tert-Butyl (2-(benzylamino)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. category: amides-buliding-blocks

86.63 mg diphenyl cyanocarbonimidate, 52.1 mg isoquinolin-6-amine, and 6 ml THF were added to a reaction bottle with thermal reflux for 3.5 hrs. After removing THF by vacuum, the residue was added to 10 ml EA. The precipitated solid was filtered to obtain 32.9 mg 1-cyano-3-(isoquinolin-6-yl)-2-phenylisourea. The intermediate was reacted with equivalent tert-butyl-2-(benzylamino)ethylcarbamate and 20 mg of DIPEA in 5 ml DMF at 110 C. for 18 hrs. After cooling, 1N NaOH was added and extracted twice with EA. After the combined EA layer was dried and concentrated by Na2SO4, 26.4 mg intermediate product was eluted out by a SiO2 column (EA/Hexane 4:1). The intermediate was added to 1.5 ml 6N HCl at room temperature with stirring overnight. After the reaction solution was evaporated under reduced pressure, 2 ml acetone/methanol (10:1) was added. The precipitate was filtered and washed with acetone, and then the solid was taken and evaporated in vacuum to give 18.7 mg of product.

The synthetic route of tert-Butyl (2-(benzylamino)ethyl)carbamate has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Industrial Technology Research Institute; CHEN, Chih-Hung; CHEN, Yi-Hsun; HUANG, Jui-Wen; HUANG, Kuo-Kuei; LIU, Chih-Peng; HWANG, Chrong-Shiong; (22 pag.)US2019/194137; (2019); A1;,
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Reference of 108723-79-1, These common heterocyclic compound, 108723-79-1, name is 2-Amino-N,N-diethylacetamide hydrochloride, 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.

To a stirred mixture of 2-amino-N,N-diethylacetamide hydrochloride (64.0 mg, 0.38 mmol) and triethylamine (77.7 mg, 0.77 mmol) in i-PrOH (3 mL) was added 4-chloro-5-[2-methyl-6-(trifluoromethyl)pyridin-4-yl]-6-phenylpyrimidin-2-amine (140.1 mg, 0.38 mmol) at room temperature. After stirring for 16 h at 110 C, the reaction mixture was cooled and concentrated. The residue was purified by Prep-HPLC to afford 2-((2- amino-5-(2-methyl-6-(trifluoromethyl)pyridin-4-yl)-6-phenylpyrimidin-4-yl)amino)-N,N- diethylacetamide (61 mg, 34.6%) as an off-white solid. ES-MS (m/z) [M+l]+ = 459.1.

The synthetic route of 108723-79-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; NIKANG THERAPEUTICS, INC.; LOU, Yan; FU, Jiping; HE, Yigang; (0 pag.)WO2020/14332; (2020); A1;,
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Electric Literature of 19982-07-1, 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. 19982-07-1, name is N-(3,5-Dimethyladamantan-1-yl)acetamide, This compound has unique chemical properties. The synthetic route is as follows.

l-Acetamido-3,5-dimethyladamantane (44 gm) as obtained in example 1, sodium hydroxide and diethylene glycol are added, and heated to reflux. Then, the contents were maintained for 6 hours at reflux and water (1 175 ml) was added under stirring. The reaction mass was cooled to below 20 C and then added methylene chloride (750 ml), and stirred for 15 minutes at 20C. The layers were separated and the organic layer was distilled off completely under vacuum at below 45C to obtain a residue. The residue was dissolved in ethyl acetate (700 ml). Ethyl acetate hydrochloride (160 ml) was added to the reaction mass and stirred for 5 hours at 25 to 30C. The reaction mass was cooled to 0 to 5C and stirred for 1 hour at 0 to 5 C. The separated solid was filtered and dried at 50C for 2 hours to obtain 87 gm of memantine hydrochloride containing l-amino-3,5,7-trimethyladamantane hydrochloride and l-amino-3-methyladamantane hydrochloride impurity.Memantine hydrochloride: 99.3%;The combined contents of l-amino-3,5,7-trimethyladamantane hydrochloride and 1- amino-3-methyladamantane hydrochloride impurity: 0.5%.

The chemical industry reduces the impact on the environment during synthesis N-(3,5-Dimethyladamantan-1-yl)acetamide. I believe this compound will play a more active role in future production and life.

Reference:
Patent; HETERO RESEARCH FOUNDATION; PARTHASARADHI REDDY, Bandi; RATHNAKAR REDDY, Kura; MURALIDHARA REDDY, Dasari; RAJI REDDY, Rapolu; RAMAKRISHNA REDDY, Matta; VAMSI KRISHNA, Bandi; WO2011/125062; (2011); A1;,
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