Amides-buliding-blocks

147962-41-2, name is N-Propylsulfamide, 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. HPLC of Formula: C3H10N2O2S

1, 8 ml of N, N-dimethylformamide, 100 g (724 mmol) of N-propylsulfamide, 26 g (1083 mmol) of sodium hydride were added to the 1 L three-necked reaction flask, and the mixture was stirred at 10 to 15 C for 30 min, (724 mmol) of 4-bromophenyl-4,6-dichloropyrimidine was stirred at 20-25 C for 8 h and then stirred at 35-40 C for 1 h, cooled to 10-15 C,22.3 g (35.9 mmol) of ethylene glycol was added,And p-toluenesulfonyl chloride (137 g, 71.9 mmol) were added and the temperature was raised to 85-95 C. The reaction was continued for 9 h, cooled to 0-10 C. The solution was crystallized by adding 10 wt% citric acid aqueous solution. The filter cake was washed with purified water neutral,The solid was collected and dried at 40-50 C under vacuum (vacuum ? 0.08 MPa) for 8 h to give 212.5 g of crude impurities and 73.9% yield. 2, to 212.5g impurity crude addition of ethyl acetate 700ml, 75-85 C heating and stirring dissolved, hot filter, the filtrate plus methanol 3000ml crystallization, filtration, filter cake with methanol amount of washing, collecting solid,At 40-50 under reduced pressure (vacuum ? 0.08MPa) dry 8h,A mixture of 1,2-bis [[N- [5- (4-bromophenyl)] – N’-propylsulfonamide-6-oxo] pyrimidinyl] ethyl dithioate was obtained in a yield of 76.5 %.

The synthetic route of 147962-41-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Hefei Jiunuo Medical Technology Co., Ltd.; Wu, Biao; Tang, Shengguo; Tan, Hongchun; (10 pag.)CN106478522; (2017); A;,
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Some common heterocyclic compound, 121-30-2, name is 4-Amino-6-chlorobenzene-1,3-disulfonamide, molecular formula is C6H8ClN3O4S2, 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: 121-30-2

A suspension of 1000 g (3.5 mol) of 4-Amino-6-chloro-l,3-benzenedisulfonamide Q and 78.9 g (2.63 mol) paraformaldehyde in 1264 ml of methanol was heated to reflux and a solution of 55.56 ml of concentrated sulphuric acid in 180.54 ml of methanol was added to the refluxing reaction mixture. After refluxing for one hour additional 23.34 g (0.78 mol) paraformaldehyde was added. The reaction mass was further refluxed for one hour and one more lot of 13.88 g (0.46 mol) paraformaldehyde was 5 added. The combined reaction mixture was refluxed for six hours followed by cooling to 20-300C. It was further stirred at this temperature for one hour and filtered; the solid mass was washed successively with methanol and water to get 980 g off white crude wet product.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 121-30-2, its application will become more common.

Reference:
Patent; UNICHEM LABORATORIES LIMITED; WO2007/26376; (2007); A2;,
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. 147962-41-2, name is N-Propylsulfamide, This compound has unique chemical properties. The synthetic route is as follows., category: amides-buliding-blocks

A.ii. N-(5-(4-bromophenyl)-6-chloropyrimidin-4-yl)propane-1-sulfamide:tBuOK (16.0 g; 0.14 mol; 1 eq.) was added to the above prepared cold (5C) solution of Intermediate A.i in DMSO. The resulting suspension was heated to 20C and stirred for 30 mi 5-(4-bromophenyl)-4,6-dichloropyrimidine (10.7 g; 0.035 mol; 0.25 eq.) was added portionwise and the mixture was heated to 50C for 1 h. Water was added. The pH of the solution was adjusted to 4-5 using 33% aq. HC1. The suspension was cooled to 0C and stirred for 30 mm. It was filtered off, rinsed with a solution of water and MeOH and dried under reduced pressure to yield the title compound as a white solid (12.6 g, 89% yield with respect to S -(4-bromophenyl)-4,6-dichloropyrimidine).

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 147962-41-2.

Reference:
Patent; ACTELION PHARMACEUTICALS LTD; ABELE, Stefan; FUNEL, Jacques-Alexis; SCHINDELHOLZ, Ivan; WO2014/155304; (2014); 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. 5466-88-6, name is 2H-1,4-Benzoxazin-3(4H)-one, A new synthetic method of this compound is introduced below., SDS of cas: 5466-88-6

General procedure: Phosphoric acid (3.15 g, 0.032 mol) and TFAA (21.8 mL, 0.104 mol) were added to the mixture of 4H-Benzo [1,4]oxazin-3-one (4 g, 0.026 mol) and substituted phenylacetic acid (1.1eq), at 0 C. After completion of addition, the mixture was allowed to warm to room temperature and stirred for 1 h. The reaction mixture was cooled to 0 C and adjusted the pH to 7 by adding the saturated NaHCO3 solution. The precipitated solid was filtered, washed with water and dried to give the desired product.

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; Rajitha, Chittipaka; Dubey; Sunku, Venkataiah; Javier Piedrafita; Veeramaneni, Venugopal Rao; Pal, Manojit; European Journal of Medicinal Chemistry; vol. 46; 10; (2011); p. 4887 – 4896;,
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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. 112257-19-9, name is tert-Butyl methyl(2-(methylamino)ethyl)carbamate belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below. Computed Properties of C9H20N2O2

The N- (4- fluoro-2-methoxy-5-nitrophenyl) -4- (1-methyl -1H- indol-3-yl) -5- (trifluoromethyl) pyrimidin – 2-Amine (922mg, 1.0eq), single-Boc protected -N, N’- dimethylethylenediamine (500mg), diisopropylethylamineAmine (2ml), trifluoroethanol were added to a microwave tube 20ml, 100 microwave reaction 2h, the solvent evaporated under reduced pressure,Flash column chromatography to obtain 2 – ((5-methoxy-4- (4- (1-methyl -1H- indol-3-yl) -5- (trifluoromethyl) pyrimidin-2-yl-amineYl) -2-nitrophenyl) (methyl) amino) ethyl (methyl) carbamic acid tert-butyl ester (1.13g, 90percent yield).

The synthetic route of 112257-19-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Qilu Pharmaceutical Co., Ltd.; Zhang, Long; Zhao, Shuyong; Chen, Chuanwen; Zhou, Haojie; Yang, Yingying; Chen, Dong; Zheng, Qingmei; Li, Yuhao; Zheng, Shansong; (57 pag.)CN105461695; (2016); A;,
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Synthetic Route of 154350-29-5, 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. 154350-29-5, name is Cyclopropanesulfonamide, This compound has unique chemical properties. The synthetic route is as follows.

Stage lc:oI IBocHN-SI Io[0182] Cyclopropanesulfonamide (5.0 g, 41.26 mmol, 1.0 eq.), triethylamine (8.62 g, 61.90 mmol, 1.5 eq.) and dichloromethane (50 mL) were charged in a 100 mL round bottom flask. Di-te/t-butyldicarbonate (10.8 g, 49.52 mmol, 1.2 eq.) and N,N- dimethylaminopyridine (252 mg, 2.06 mmol, 0.05 eq.) were added portion wise and the reaction mixture stirred at ambient temperature for 48 hours. The solvent was removed in vacuo and the residue diluted with water (20 mL). The aqueous phase was acidified to pH = 1 with 1M hydrochloric acid, and extracted with ethyl acetate (3 x 100 mL). The organic extracts were combined, washed with water (100 mL) and brine (100 mL), dried over magnesium sulfate, filtered and the solvent removed in vacuo to give 9.1 g (99percent yield) of the title compound as a white solid. 1H NMR (500 MHz, CDC13) delta ppm 7.14 (br. s., 1 H) 2.90 (tt, 7=8.09, 4.73 Hz, 1 H) 1.50 – 1.54 (m, 9 H) 1.35 – 1.40 (m, 2 H) 1.09 – 1.15 (m, 2 H). LC-MS: purity 100percent (UV), tR 1.62 min m/z [M+Na]+ 243.95 (MET/CR/1278).

The chemical industry reduces the impact on the environment during synthesis Cyclopropanesulfonamide. I believe this compound will play a more active role in future production and life.

Reference:
Patent; INTERMUNE, INC.; BUCKMAN, Brad; NICHOLAS, John, B.; SEREBRYANY, Vladimir; SEIWERT, Scott, D.; WO2012/37259; (2012); A1;,
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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. 108468-00-4, name is 1-(N-Boc-aminomethyl)-4-(aminomethyl)benzene, This compound has unique chemical properties. The synthetic route is as follows., Quality Control of 1-(N-Boc-aminomethyl)-4-(aminomethyl)benzene

2,4-dichloro-3-nitroquinoline (150 mg, 0.617 mmol) was dispersed in anhydrous DCM (10 mL) and stirred at room temperature for 5 min before a solution of l-(N-Boc-aminomethyl)-4-(aminomethyl)benzene (146 mg, 0.617 mmol) in DCM (lOmL) with EbN (90pL) was added in dropwise. This mixture was then stirred at 20 C for 3 h, then added asolution of l-(N-Boc-aminomethyl)-4-(aminomethyl)benzene (90 mg) with EbN (90 uL) and was allowed to stir at 20 C for 24 h, where LCMS saw full conversion of the dichloro-nitro-quinoline. The reaction mixture was diluted with DCM to 25 mL and was washed with brine, which was extracted with 2x 50 mL DCM. The combined organic phases were dried with Na2S04, filtered, and concentrated before the crude product was purified by flash column chromatography on silica (hexane/ethyl acetate 3:2). Product containing fractions with single spot by TLC were pooled and concentrated to an orange oil that was further concentrated to an orange solid at 0.2 mbar. Yielded 246.9 mg (90%). Rf = 0.57 (hexane/ethyl acetate 1 : 1 (v/v)). UPLCMS of product (LC2, C’ is): Retention time = 4.58 min. Calculated mass of C22H23CIN4O4 = 442.14; Observed [M+Na:M+Na+2]? as m/z = 465.1/467.2 in a 3: 1 ratio. NMR (400 MHz, DMSO-d6) d 8.53 (d, J= 8.5 Hz, 1H), 8.48 (t, J= 6.3 Hz, 1H), 7.88- 7.81 (m, 2H), 7.67 (ddd, J= 8.4, 5.3, 2.9 Hz, 1H), 7.36 (t, J= 6.2 Hz, 1H), 7.21 (d, J= 8.3 Hz, 2H), 7.17 (d, J= 8.4 Hz, 2H), 4.41 (d, J= 6.1 Hz, 2H), 4.09 (d, J= 6.2 Hz, 2H), 1.38 (s, 9H).13C NMR (101 MHz, DMSO) d 155.8, 145.3, 144.4, 141.1, 139.5, 136.1, 132.3, 128.6, 127.0, 126.9, 126.7, 126.5, 123.1, 119.7, 77.8, 46.6, 43.0, 28.2.

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 108468-00-4.

Reference:
Patent; TORQUE THERAPEUTICS, INC.; ANDRESEN, Thomas Lars; HENRIKSEN, Jonas Rosager; KRAEMER, Martin Kisha; (217 pag.)WO2020/23680; (2020); 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. 136927-63-4, name is Pyrrolo[1,2-a]pyrazin-1(2H)-one, A new synthetic method of this compound is introduced below., Quality Control of Pyrrolo[1,2-a]pyrazin-1(2H)-one

PREPARATION 20 1-chloropyrrolo[1,2-a]pyrazine (A compound of formula (BB)) To pyrrolo[1,2-a]pyrazin-1(2H)-one (0.35 g, 2.61 mmol) was added phosphorous oxychloride (4.0 g, 26.1 mmol). The reaction mixture was agitated for approximately 16 hours. The reaction mixture was then made alkaline by the addition of sodium bicarbonate. The reaction mixture was then extracted with hexane, washed with a saturated sodium bicarbonate solution, dried over MgSO4 and evaporated. The product was purified by recrystallization in hexane and cooled with a mixture of dry ice and acetone to give the title compound, 1-chloropyrrolo[1,2-a]pyrazine (71%), m.p. 56-57 C.

The synthetic route of 136927-63-4 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Syntex (U.S.A.) Inc.; US5041442; (1991); A;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Related Products of 5349-24-6, These common heterocyclic compound, 5349-24-6, name is N-Butyl-2-chloroacetamide, 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: Compound 1,2,4-triazol-3-thiol (4) (0.01 mol) was dissolved in aqueous potassium hydroxide solution (0.61g in 100 ml distilled water) with stirring till a clear yellow color solution was obtained. It was filtered to remove any suspended impurities. Then various N-substituted-alpha-chloroacetanilides (0.01 mol) compound were dissolved in ethanol and added with shaking at 55C stirred for 4.5 h. Then the reaction mixture was left overnight and the next day, the separated solid was filtered and washed twice with cold distilled water to remove KCl, dried and recrystallized from dilute glacial acetic acid. In case of aliphatic N-substituted-alpha-chloroacetanilides, the amide was added at room temperature.

The synthetic route of 5349-24-6 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Rajoriya, Vaibhav; Kashaw, Varsha; Kashaw, Sushil K.; Letters in drug design and discovery; vol. 15; 5; (2018); p. 451 – 462;,
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These common heterocyclic compound, 1882-71-9, name is 2-Amino-5-methoxybenzamide, 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 1882-71-9

General procedure: A 12mL vial was charged with MCM-41-2P-Pd(OAc)2 (2molpercent), 2-aminobenzamide (1mmol), aryl iodide (1mmol) (if solid) and a stirring bar. Then, DMF (2mL), aryl iodide (1mmol) (if liquid) and DBU (2mmol) were injected by syringe under an argon atmosphere. The vial was placed in an alloy plate, which was transferred into a 300mL Parr Instruments 4560 series autoclave under an argon atmosphere. After flushing the autoclave three times with CO, a pressure of 10bar CO was fixed at ambient temperature. The autoclave was heated for 20hat 120¡ãC. After completion of the reaction, the autoclave was cooled to room temperature and the pressure was released carefully. The reaction mixture was diluted with ethyl acetate (10mL) and filtered. The palladium catalyst was washed with distilled water (2¡Á5mL) and acetone (2¡Á5mL), and reused in the next run. The filtrate was concentrated in vacuo and the pure product was isolated by either washed with water, ethyl acetate and finally hexane or recrystallization from MeOH.

The synthetic route of 2-Amino-5-methoxybenzamide has been constantly updated, and we look forward to future research findings.

Reference:
Article; You, Shengyong; Huang, Bin; Yan, Tao; Cai, Mingzhong; Journal of Organometallic Chemistry; vol. 875; (2018); p. 35 – 45;,
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