Tag: M.W=200-300

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. 535170-20-8, name is tert-Butyl (3-amino-2,6-difluorophenyl)carbamate, This compound has unique chemical properties. The synthetic route is as follows., Safety of tert-Butyl (3-amino-2,6-difluorophenyl)carbamate

The tert-butyl-3-amino-2,6-difluorophenylcarbamate (100 mg, 0.41 mmol) prepared at Step 3 was added and dissolved into dichloromethane solvent. 2- propane sulfonyl chloride (50 uL, 0.45 mmol) and pyridine (36 uL, 0.045mmol) were added into the reaction solution and stirred at 50C for 2 hours. After the reaction, the reactant was washed with 1N aqueous hydrochloric acid solution and salt water. After extraction with dichloromethane, the organic layer was dried with sulfuric anhydride magnesium and vacuum concentrated, and then refined by means of column chromatography, so that 94 mg of the target compound, tert-butyl-2,6-difluoro-3-(1-methylethylsulfonamido)phenylcarbamate (percentage yield: 65%), was obtained.1H NMR(400MHz, CDCl3): delta 7.43(td, J = 8.8, 5.6 Hz, 1H), 6.97(bs, 1H), 6.90(td, J = 8.8, 1.6 Hz, 1H) 6.33(bs, 1H), 3.25(m, 1H), 1.49(s, 9H), 1.39(d, J = 6.8 Hz, 6H).

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 535170-20-8.

Reference:
Patent; Youai Co., Ltd.; SHIM, Eun Kyong; KIM, Nam Doo; SHIM, Tae Bo; KIM, Seung Yong; EP2647637; (2013); A2;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Reference of 68524-30-1,Some common heterocyclic compound, 68524-30-1, name is 2-[(Diphenylmethyl)thio]acetamide, molecular formula is C15H15NOS, 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.

HTP Assay of CHMO Polypeptides: (0203) Primary screening used to guide optimization was carried out in a 200 muL volume in 96-well plate high-throughput (HTP) assay protocol using cell lysates. The general HTP assay conditions were: 1-100 g/L substrate (i.e., compound (1a) or (1b)), 10-200 muL of clear cell lysate containing the engineered CHMO polypeptide, 0.05-1.0 g/L NADP cofactor, 1 g/L ketoreductase (KRED) polypeptide for cofactor recycling, 0.025-0.100 M phosphate or TEA buffer solution containing 3.5%-10% (v/v) IPA (and optionally, 1.5% acetone or 10% PEG200) co-solvent, pH 8-9, 25 C. reaction temperature and 20 h reaction time (with 200 rpm shaking). The HTP assay conditions were changed slightly over the different rounds of the directed evolution of the CHMO variant polypeptide disclosed in order to detect those variants most improved in enzyme properties. Table 4 shows the HTP assay conditions used to perform primary screening of those variant polypeptides whose improved properties were confirmed by SFP assay as summarized in Tables 2A and 2B. Rounds 1-6 assays used the amide substrate of compound (1a) and Rounds 7-16 assays used the acid substrate of compound (1b). HTP Assay Results: (0220) Representative results in the primary screening using the HTP assay for both the amide substrate (compound (10) and the acid substrate (compound (2a)) are shown below in Tables 7 and 8.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-[(Diphenylmethyl)thio]acetamide, its application will become more common.

Reference:
Patent; CODEXIS, INC.; Ang, Ee Lui; Alvizo, Oscar; Behrouzian, Behnaz; Clay, Michael; Collier, Steven; Eberhard, Ellen; Fu, Fan Jaslyn; Song, Shiwei; Smith, Derek; Widegren, Magnus; Wilson, Robert; Xu, Junye; Zhu, Jun; (200 pag.)US9267159; (2016); B2;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Adding a certain compound to certain chemical reactions, such as: 143557-91-9, name is tert-Butyl 3-endo-3-hydroxy-8-azabicyclo[3.2.1]octane-8-carboxylate, 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 143557-91-9, category: amides-buliding-blocks

To a stirred solution of Intermediate 63 (0.68 g, 2.98 mmol) in dry DMF (10 mL) wasadded NaH (60 % dispersion in mineral oil,120 mg, 3.00 mmol). After the mixturewas stirred for 15 mm Intermediate 26 (0.5 g, 2.29 mmol) was added as one portion. The resulting mixture was stirred at RT for 48 h. The reaction mixture was poured onto brine and extracted into EtOAc. The organic layer was washed with brine, separated, dried over MgSO4, filtered and concentrated under reducedpressure to give brown oil. The crude material was purified by Biotage Isolera chromatography (silica gel, eluting with heptane-EtOAc, 1:0 to 0:1) to afford 531 mg (54% yield) of the title compound as an off-white powder.1H NMR (250 MHz, Chloroform-d): 6 [ppm] 7.71 (t, J = 1.4 Hz, 2H), 7.68 – 7.63 (m, 1H), 7.53 (d, J = 1.2 Hz, 1H), 7.13 (dd, J = 2.4, 1.3 Hz, 1H), 4.75 (tt, J = 10.6, 5.9Hz, 1H), 4.34 (5, 2H), 2.53 (d, J = 1.1 Hz, 3H), 2.20- 2.00 (m, 4H), 1.93 – 1.65 (m,4H), 1.49 (5, 9H).LCMS (Analytical Method A) Rt = 1 .46 mm, MS (ESIpos): m/z = 426.05 (M+H)+.

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; EVOTEC AG; DAVENPORT, Adam James; BRAEUER, Nico; FISCHER, Oliver Martin; ROTGERI, Andrea; ROTTMANN, Antje; NEAGOE, Ioana; NAGEL, Jens; GODINHO-COELHO, Anne-Marie; (703 pag.)WO2016/91776; (2016); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

These common heterocyclic compound, 138-41-0, name is Carzenide, 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. Safety of Carzenide

Compound 3-7 (300 mg, 1.33 mmol), p-sulfonamide benzoic acid (294 mg, 1.46 mmol, 1.1 eq.), HOBt (539 mg, 3.99 mmol, 3 eq.) and EDCI (765 mg, 3.99 mmol, 3 eq.) in 50 mL Single mouth bottle,DMF and TEA (0.74 mL, 5.32 mmol, 4 eq.) were added.Stir at room temperature overnight. TLC tracking monitoring. Rotate the DMF,Add EA and water for extraction, wash with saturated brine, dry, spin dry, and pass through column (DCM:acetone = 3:1). A white solid of 450 mg was obtained in a yield of 83%.

The synthetic route of Carzenide has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Guangzhou Hengnuokang Pharmaceutical Technology Co., Ltd.; Zhang Jiancun; Lin Cai; Zou Qingan; (45 pag.)CN108456208; (2018); A;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

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;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

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;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

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;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

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;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

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;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

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;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics