Category: amides-buliding-blocks

Application of 22958-64-1, 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. 22958-64-1, name is 2-(4-Sulfamoylphenyl)acetic acid belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.

[00324] To a solution of 2-amino-5-(cyclohexylmethyl)-6,6-dimethyl-4, 5,6,7- tetrahydrothieno[3,2-c]pyridine-3-carbonitrile Core-1 c_A (1.15 g, 3.8 mmol) in DMF (12 mL) was added 2-(4-sulfamoylphenyl)acetic acid (1.23 g, 5.7 mmol), DIPEA (982 mg, 7.6 mmol) and a solution of T3P in EtOAc (4.84 g, 50% w/w, 7.6 mmol). The mixture was stirred at 65 C for 1 h. The reaction mixture was diluted with water (25 mL) and extracted with EtOAc (15 mLx4). The organic layer was concentrated. The residue was purified by column chromatography on silica (PE:EtOAc=10:1 ~2:1) to afford the desired product (1.15 g, yield 60%) as light yellow solid; LC-MS Rt 1.08 min, MS m/z [M+H]+ 501.3; Method 1 ; 1H NMR (400 MHz, DMSO-cfe) d 1 1.9 (s, 1H), 7.78 (d, J = 8.4 Hz, 2H), 7.48 (d, J = 8.4 Hz, 2H), 7.33 (s, 2H), 3.96 (s, 2H), 3.49 (s, 2H), 2.46 (s, 2H), 2.24 (d, J = 6.8 Hz, 2H), 1.76 – 1.73 (m, 2H), 1.67 – 1.64 (m, 3H), 1.39 – 1.33 (m, 1H), 1.25 – 1.15 (m, 3H), 1.02 (s, 6H), 0.88 – 0.75 (m, 2H).

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, 2-(4-Sulfamoylphenyl)acetic acid, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; NOVARTIS AG; KOUNDE, Cyrille; SIM, Wei Lin Sandra; SIMON, Oliver; WANG, Gang; YEO, Hui Quan; YEUNG, Bryan KS; YOKOKAWA, Fumiaki; ZOU, Bin; (122 pag.)WO2019/244047; (2019); A1;,
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Electric Literature of 201162-53-0, These common heterocyclic compound, 201162-53-0, name is 3-Boc-3,8-Diazabicyclo[3.2.1]octane, 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.

Aldehyde Intermediate 2 (1.0 equiv) and /er/-butyl 3,8-diazabicyclo[3.2. l]octane-3- carboxylate (1.2 equiv) were combined into l,2-DCE (5 mL). To the mixture was added acetic acid (0.5 equiv). The mixture was stirred at rt for 3h. Solid NaBH(OAc)3(3.0 equiv) was then added into the reaction. The resulting mixture was stirred at rt overnight. The reaction was quenched with MeOH (10 mL) and washed with saturated NaHC03, water, and brine. The crude mixture was purified on a silica gel column to afford /er/-butyl 8-((2-ethyl-4′-(l,l,l,3,3,3-hexafluoro-2- hydroxypropan-2-yl)-[l,r-biphenyl]-4-yl)methyl)-3,8-diazabicyclo[3.2. l]octane-3-carboxylate (yield 55%) as a white solid.

The synthetic route of 201162-53-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ESCALIER BIOSCIENCES B.V.; MOHAN, Raju; NUSS, John; HARRIS, Jason; YUAN, Shendong; (144 pag.)WO2019/177996; (2019); A1;,
Amide – Wikipedia,
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These common heterocyclic compound, 5338-44-3, name is Ethyl 4-acetamidobenzoate, 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. Computed Properties of C11H13NO3

General procedure: To a solution of amidoxime 1 (2 mmol) and ester 2 (3 mmol) inDMSO (2 mL) 120 mg (3 mmol) powdered NaOH was rapidlyadded.The reaction mixture was stirred at room temperature for therequired time (TLC or precipitation of the product). The reactionmixture was diluted with cold water (30e50 mL). The resultingprecipitate was ltered off, washed with water (30 mL) and dried inair at 50 C.

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

Reference:
Article; Baykov, Sergey; Sharonova, Tatyana; Shetnev, Anton; Rozhkov, Sergey; Kalinin, Stanislav; Smirnov, Alexey V.; Tetrahedron; vol. 73; 7; (2017); p. 945 – 951;,
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Application of 103361-99-5, These common heterocyclic compound, 103361-99-5, name is 7-Fluoro-2H-benzo[b][1,4]oxazin-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.

Step A 6-Iodo-7-fluoro-2H-1,4-benzoxazin-3(4H)-one 7-Fluoro-2H-1,4-benzoxazin-3(4H)-one (15.8 g) was mixed with iodine monochloride (15.6 g) in acetic acid (150 ml) and heated to reflux for 36 h. The cooled mixture was treated with saturated aqueous sodium bisulfite until the color was dissipated. The solid was filtered and washed well with water. The solid was air dried and dried further by dissolution in dimethylformamide (100 ml) and evaporated to dryness under reduced pressure to give the desired product (26.3 g) contaminated with some starting material. (The reaction can be taken to completion by addition of more iodine monochloride and refluxing for 24 h longer.) The crude product was used in Step B.

The synthetic route of 103361-99-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; E. I. Du Pont de Nemours and Company; US5670455; (1997); A;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Synthetic Route of 121492-06-6, 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 121492-06-6 as follows.

General procedure: To a solution of acid 7(a-p) (1 equiv) and amine (1.5 equiv) in dichloromethane were added HoBt (1.5 equiv) and EDCI(1.5 equiv). The reaction mixture was stirred at room temperature overnight, then washed with 5% aqueous HCl, 5% aqueous sodium bicarbonate, water, and brine, and dried. Purification by chromatography afforded 8-9(a-c).

According to the analysis of related databases, 121492-06-6, the application of this compound in the production field has become more and more popular.

Reference:
Article; Yang, Ying-Rui; Wei, Jin-Lian; Mo, Xiao-Fei; Yuan, Zhen-Wei; Wang, Jia-Lin; Zhang, Chao; Xie, Yi-Yue; You, Qi-Dong; Sun, Hao-Peng; Bioorganic and Medicinal Chemistry Letters; vol. 26; 11; (2016); p. 2713 – 2718;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

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. name: R-5-(2-Aminopropyl)-2-methoxybenzenesulfonamide

EXAMPLE 34 R-(-)-5-[2-[2-(5-Fluoro-2-methoxyphenoxy)-ethylamino]propyl]-2-methoxybenzenesulfonamide hydrochloride A suspension of 1.00 g of R-(-)-5-(2-aminopropyl)-2-methoxybenzenesulfonamide [[alpha]D25 -13.8 (C=1,MeOH), m.p.156.5-160.5 C. (H2 O) ] 11.00 g of 2-(2-bromoethoxy)-4-fluoroanisole and 0.20 g of potassium iodide in 40 ml of N,N-dimethylformamide was heated for 10 hours at 85 C. After cooling, the reaction mixture was poured into water, made alkaline with 10% sodium hydroxide aqueous solution and extracted with ethyl acetate. The extract was washed with water, dried and evaporated. The residue was chromatographed on silica gel using chloroform-methanol (9:1) as an eluant to give 0.81 g of the free base as colorless crystals which were recrystallized from methanol as colorless needles, m.p.144-145 C. Analysis for C19 H25 FN2 O5 S: Calculated %: C, 55.33; H, 6.11; N, 6.79. Found %: C, 55.20; H, 5.93; N, 6.54.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 112101-81-2, its application will become more common.

Reference:
Patent; Hokuriku Pharmaceutical Co., Ltd.; US4971990; (1990); A;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Related Products of 120157-97-3, 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. 120157-97-3, name is N-Boc-2-(4-Bromophenyl)ethylamine belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.

[2- (4-Bromo-phenyl)-ethyl]-carbamic acid tert-butyl ester (1. 5g, 4.99 mmol) was dissolved in toluene (0.2 M) in a 100 mL round-bottom flask. To this was added LiCl (10.6 mg, 0.25 mmol, 0. 05eq) and the resulting solution was flushed under nitrogen for 2-3 minutes. PdCl2 (PPh3) 2 (175.4 mg, 0. 25mmol, 0. 05eq) was added to the reaction mixture and the solution was again flushed under nitrogen for 2-3 minutes. 2-Tributylstannanyl-pyridine, from Frontier (1. 84g, 4.99mmol, leq) was added last and the reaction mixture was heated to 110C overnight. The solvent was removed under vacuum. The crude material was purified on column chromatography (silica gel), and eluted with EtOAc-Hexanes 15: 85 to afford [2- (4-Pyridin-2-yl-phenyl)-ethyl]-carbamic acid tert-butyl ester in good yield.

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-Boc-2-(4-Bromophenyl)ethylamine, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; ELAN PHARMACEUTICALS, INC.; WO2003/93245; (2003); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Synthetic Route of 125414-41-7, The chemical industry reduces the impact on the environment during synthesis 125414-41-7, name is tert-Butyl (1,3-dihydroxypropan-2-yl)carbamate, I believe this compound will play a more active role in future production and life.

2.97 g of lipoic acid (LA), 3.31 g of 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC¡¤HCl) was added to a 100 mL round bottom flask.Add 40 mL CH2Cl2 to dissolve and activate for 30 min.1.25 g of Boc-serinol dissolved in 20 mL of CH 2 Cl 2 and 2.21 g of 4-(dimethylamino)pyridine (DMAP) were added to the above mixture.Reaction for 12 h. After the reaction is completed, it is filtered.The filtrate was thoroughly washed with an excess of 0.1 mol/L hydrochloric acid.Discard the water phase after standing. Dry the oil phase with sodium sulfate and purify by column chromatography (eluent: CHCl3/CH3OH=20/1, v/v) to give a pale yellowOily liquid di-Boc-LA-Ser (3.19 g, yield 86%).Take 1g di-Boc-LA-Ser in 10mL CH2Cl2,After cooling to 0 C, 0.41 g of trifluoroacetic acid (TFA) was slowly added dropwise and reacted for 2 h.The mixture was concentrated in vacuo to give a crude di-L-Ser.

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, tert-Butyl (1,3-dihydroxypropan-2-yl)carbamate, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Southeast University; Li Xinsong; Ling Longbing; He Wei; (21 pag.)CN109224082; (2019); A;,
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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. 6292-59-7, name is 4-(tert-Butyl)benzenesulfonamide, This compound has unique chemical properties. The synthetic route is as follows., Product Details of 6292-59-7

General procedure: A Schlenk tube with a magnetic stir bar was charged with [RhCp*Cl2]2 (7.8 mg, 12.5 mumol), AgSbF6 (17.2 mg, 50 mumol), PhI(OAc)2 (120.4 mg, 0.375 mmol), NaOAc (6.2mg, 75 mumol), 8-methylquinoline derivative 1 (0.50 mmol), amide 2 (0.25 mmol), and DCM (1.0 mL) under an N2 atmosphere. The resulting mixture was stirred at room temperature for 48 h and then diluted with 3 mL of dichloromethane. The solution was filtered through a celite pad and washed with 10-20 mL of dichloromethane. The filtrate was concentrated and the residue was purified by column chromatography on silica gel to provide the desired product.

According to the analysis of related databases, 6292-59-7, the application of this compound in the production field has become more and more popular.

Reference:
Article; Huang, Xiaolei; You, Jingsong; Chemistry Letters; vol. 44; 12; (2015); p. 1685 – 1687;,
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. 33045-52-2, name is Methyl 2-methoxy-5-sulfamoylbenzoate, This compound has unique chemical properties. The synthetic route is as follows., Quality Control of Methyl 2-methoxy-5-sulfamoylbenzoate

(4) Add 245 g (1.0 mol) of methyl 2-methoxy-5-sulfamoylbenzoate prepared in step (3) and 2772 g of 5% sodium hydroxide solution by weight to the reactor, Stir the reaction for 20 h, and the reaction temperature does not exceed 40 . After the reaction, adjust the pH to 1 with 5% by weight of dilute hydrochloric acid and filter. The resulting filter cake is washed with water, dried, and recrystallized from methanol to produce 209.06 g of 2-methoxy-5-sulfamoylbenzoic acid, yield 90.5%.

According to the analysis of related databases, 33045-52-2, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Suzhou Chenghe Pharmaceutical And Chemical Co., Ltd.; Chen Xiaoqiang; Fang Huan; (7 pag.)CN111100042; (2020); A;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics