Category: amides-buliding-blocks

Related Products of 53844-02-3, 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. 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.

General procedure: To a solution of 1 (15.0mmol) in CH3CN (60mL) were added K2CO3 (3.10g, 22.5mmol) and N-Cbz-2-bromoethylamine (3.87g, 15.0mmol) under stirring. It was then kept at 80C, and monitored by TLC (Hexane/EtOAc=2/1, v/v). Next, K2CO3 was removed by filtration. The filtrate was concentrated to give a light brown oil. The oil was dissolved in ethyl acetate (150mL) and the solution was washed with water (2¡Á50mL). The organic phase was dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford the crude product. The residue was concentrated and purified by silica gel column chromatography (Hexane/EtOAc=4/1, v/v) to give a white solid

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

Reference:
Article; Ao, Chunyan; Men, Jian; Wang, Yang; Shao, Tao; Huang, Yuanyuan; Huo, Junji; Gao, Guowei; Tetrahedron Asymmetry; vol. 27; 13; (2016); p. 589 – 595;,
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Related Products of 6292-59-7, 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. 6292-59-7, name is 4-(tert-Butyl)benzenesulfonamide belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.

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 molpercent) 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

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, 4-(tert-Butyl)benzenesulfonamide, other downstream synthetic routes, hurry up and to see.

Reference:
Article; Reddy, Thurpu Raghavender; Battina, Suresh Kumar; Kashyap, Sudhir; Journal of Carbohydrate Chemistry; vol. 34; 3; (2015); p. 133 – 144;,
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Reference of 72505-21-6, These common heterocyclic compound, 72505-21-6, name is 4-(Trifluoromethyl)thiobenzamide, 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.

Intermediate Example P; EMI70.1Ethyl 4- (1-methylethyl)-2- [4- (trifluoromethyl) phenyl]-1, 3-thiazole-5-carboxylate(XI-5a) Ethyl isobutyrylacetate(XI-3a) (3.006 g, 19.0mmol) was dissolved in chloroform (20 mL). Sulfuryl chloride (1.70 mL, 21.2mmol) was added and the solution was stirred at RT for 18 hours, then was concentrated. The residue was dissolved in ethanol (50 mL).4- (Trifluoromethyl) benzenethioamide (4.234 g, 20.6mmol) was added and the solution was heated to reflux for 24 hours. The mixture was cooled to RT and filtered. The solid was washed with cold ethanol and dried to provide the title product (2.68 g, 32%) as a pale yellowsolid.’H NMR (400 MHz,CDCI3)6 8.09 (d, J= 8.1 Hz, 2H), 7.69 (d, J= 8.1 Hz, 2H), 4.35 (q, J= 7.1 Hz, 2H), 3.99 (qu, J= 6.8 Hz,1H), 1.39 (t, J= 7.1 Hz,3H), 1.35 (d, J= 6.8 Hz, 6H).

Statistics shows that 4-(Trifluoromethyl)thiobenzamide is playing an increasingly important role. we look forward to future research findings about 72505-21-6.

Reference:
Patent; SMITHKLINE BEECHAM CORPORATION; WO2005/51890; (2005); A1;,
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Synthetic Route of 749927-69-3, The chemical industry reduces the impact on the environment during synthesis 749927-69-3, name is 4-Bromo-2-fluoro-N-methylbenzamide, I believe this compound will play a more active role in future production and life.

N-methyl-2-fluoro-4-bromo-benzamide 1a (23.21 g, 100 mmol) was added to a three-necked flask.Cyclobutyrate hydrochloride 2 (15.16 100 mmol) and N,N-dimethylacetamide (116 mL),Copper iodide (1.90 g, 10 mmol) and cesium carbonate (71.68 g, 220 mmol) were added under a nitrogen atmosphere, and the mixture was stirred and heated to 90 to 95 C overnight.At the end of the reaction, water (232 mL) and isopropyl acetate (232 mL) were added, and the mixture was stirred and the aqueous phase was collected, and the pH was adjusted to 3 to 4 with 4N hydrochloric acid.Precipitating a large amount of solids,Filtration dried to give compound 3 (17.88 g, 79%).

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, 4-Bromo-2-fluoro-N-methylbenzamide, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Hangzhou Kechao Biological Technology Co., Ltd.; Zheng Xuchun; Zhang Yiping; (10 pag.)CN108383749; (2018); A;,
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Application of 40724-47-8, 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 40724-47-8 as follows.

[0216] In a microwave tube was placed ethyl 2-(5-fluoro-3-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl)- 1H-indol- 1 -yl)thiazole-4-carboxylate (114 mg, 0.15 mmol, ?55percent purity), 4-(bromomethyl)benzenesulfonamide (49.9 mg, 0.200 mmol), and Pd(Ph3P)4 (17.33 mg,0.0 15 mmol). The tube was sealed and air was removed and re-filled with N2 (2-3 times). A mixture of toluene (0.75 ml, ratio: 2.500)/EtOH (0.3 ml, ratio: 1.000) was added, and then 2 N Na2CO3(aq) (0.3 mL, 0.6 mmol, 4 equiv) was added. The mixture was stirred at 80 ¡ãC (preheated) for 2 h. The organic layer was separated, and the aqueous layer was extracted with EtOAc (2 mL x 3). The combined organic layer was dried (Na2504) and filtered. After removal of the solvent, the product was purified by silica gel chromatography using 20-50percent EtOAc/hexane as the eluent to give ethyl 2-(5-fluoro-3-(4-sulfamoylbenzyl)-1H-indol-1- yl)thiazole-4-carboxylate (47 mg, 0.102 mmol, 68.2percent yield) as a white solid.

According to the analysis of related databases, 40724-47-8, the application of this compound in the production field has become more and more popular.

Reference:
Patent; THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES; VANDERBILT UNIVERSITY; MALONEY, David J.; JADHAV, Ajit; BANTUKALLU, Ganesha Rai; BRIMACOMBE, Kyle Ryan; MOTT, Bryan T.; YANG, Shyh Ming; URBAN, Daniel Jason; HU, Xin; SIMEONOV, Anton; KOUZNETSOVA, Jennifer L.; WATERSON, Alex Gregory; SULIKOWSKI, Gary Allen; KIM, Kwangho; CHRISTOV, Plamen; JANA, Somnath; (387 pag.)WO2016/109559; (2016); A2;,
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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. 5202-85-7, name is 2-Amino-5-chlorobenzamide belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below. HPLC of Formula: C7H7ClN2O

General procedure: To an oven-dried 20 cm3 test tube with a ground-in stopperequipped with a stir bar were added anthranilamide (1.0 mmol), benzyl alcohol (1.0 mmol), KOH (2.0 mmol),and 4 cm3 toluene. The test tube was put in an oil bath potpreheated at 90 C and the mixture was stirred for 20 h at90 C. After cooling to room temperature, the reactionmixture was added about 5 g silica gel and directly condensedon a rotator under vacuum. The resulting residualwas transferred to a silica gel chromatography column andeluted with a solution of petroleum ether and ethyl acetate[4/1 (v/v)] to give a white solid 2-phenyl-4(3H)-quinazolinone.For some products (3f, 3g, 3n, and 3t) onlysparingly soluble in ethyl acetate, the reaction mixtureswere condensed in vacuo on a rotary evaporator. Theresiduals were washed three times with water and oncewith ethyl acetate, and then dried in an infrared oven togive the desired products pure enough for NMR analysis.

The synthetic route of 5202-85-7 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Qiu, Dezhi; Wang, Yanyan; Lu, Dongming; Zhou, Lihong; Zeng, Qingle; Monatshefte fur Chemie; vol. 146; 8; (2015); p. 1343 – 1347;,
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Synthetic Route of 162576-01-4, 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. 162576-01-4, name is Benzyl (2-aminoethyl)(methyl)carbamate hydrochloride, This compound has unique chemical properties. The synthetic route is as follows.

Boc-Arg (Pbf) -OH (16.0 g, ca. 30.4 mmol) in DMF (150 mL)Compound CA solution of hydrochloride (8.2 g, 33.4 mmol) and DIEA (16.9 mL, 97.2 mmol) was cooled in an ice bath followed by a solution of HATU (13.8 g, 36.4 mmol) dropwise In 20 minutes. The temperature of the reaction mixture was raised to ambient temperature and stirring was continued for an additional hour. The reaction mixture was diluted with EtOAc (1 L) and extracted with water (3 ¡Á 200 mL) and brine (200 mL). The organic layer was dried over MgSO 4 and evaporated to give compound D (24.4 g, yield exceeding the quantitative value) as a yellowish oil.

The chemical industry reduces the impact on the environment during synthesis Benzyl (2-aminoethyl)(methyl)carbamate hydrochloride. I believe this compound will play a more active role in future production and life.

Reference:
Patent; SIGNATURE THERAPEUTICS INCORPORATED; JENKINS, THOMAS E; Husfeld, Craig O; Seroogy, Julie D; Wray, Jonathan W; (162 pag.)JP2016/41698; (2016); A;,
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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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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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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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