Month: March 2021

96799-02-9, name is 5-(Furan-2-yl)-1H-pyrazol-3-amine, belongs to pyrazoles-derivatives 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 5-(Furan-2-yl)-1H-pyrazol-3-amine

General procedure: The general method was described for the synthesis of D1. Compound C1 (150 mg, 0.393 mmol) was dissolved in ethanol (2 mL),followed by addition of 5-phenyl-1H-pyrazol-3-amine (62.63 mg, 0.393 mmol) and triethylamine (119.43 mg, 1.18 mmol). The mixture was stirred at room temperature for 5 h. The resultant mixture was purified by column chromatography to give D1.

The synthetic route of 96799-02-9 has been constantly updated, and we look forward to future research findings.

Synthetic Route of 176969-34-9, 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. 176969-34-9, name is 3-(Difluoromethyl)-1-methyl-1H-pyrazole-4-carboxylic acid, This compound has unique chemical properties. The synthetic route is as follows.

3-(Difluoromethyl)-1-methyl-pyrazole-4-carboxylic acid (75 mg, 0.43 mmol) and (S)- 6-(4-(1,1,1-trifluoropropan-2-yl)-4H-1,2,4-triazol-3-yl)pyridin-2-amine (110 mg, 0.43 mmol) were dissolved in Et3N (0.60 mL, 4.3 mmol). Propylphosphonic anhydride ( 50 wt% in EtOAc, 0.44 mL) was then added and the reaction was heated at 80 C for 3 h. After this time, he reaction was cooled to rt and quenched by addition of MeOH (2 mL). The resulting solid was filtered and dried under vacuum to give the title compound (150 mg, 85%) as a white solid. 1H NMR (400 MHz, MeOD) d ppm 9.01 (s, 1H), 8.30 – 8.38 (m, 1H), 8.18 – 8.26 (m, 1H), 7.92 – 8.05 (m, 2H), 7.05 – 7.41 (m, 2H), 4.02 (s, 3H), 1.85 – 1.94 (m, 3H). MS (ESI): 416.0 [M + H]+.

The chemical industry reduces the impact on the environment during synthesis 3-(Difluoromethyl)-1-methyl-1H-pyrazole-4-carboxylic acid. I believe this compound will play a more active role in future production and life.

Electric Literature of 288-13-1, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 288-13-1 name is 1H-Pyrazole, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

2a (5.Og, 73.5mmol) was added in portions to H2SO4 (35mL) while keeping the temperature below 400C, then 70% HNO3 (5.06mL, 80.6mmol) was added dropwise while maintaining the temperature below 55 0C. The mixture was then heated at 550C for 5h and cooled to 00C. The mixture was neutralized with 50% NaOH and the resulting slurry was diluted with ethyl acetate. The resulting precipitate was removed by filtration. The filtrate was separated and the organic phase was washed with water and brine, dried over MgSO4 and concentrated in vacuum. The residue was crystallized for ethanol to afford 2b (7.1g, 85.5%)

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 1H-Pyrazole, and friends who are interested can also refer to it.

Adding a certain compound to certain chemical reactions, such as: 120068-79-3, name is 5-Amino-1-(2,6-dichloro-4-(trifluoromethyl)phenyl)-1H-pyrazole-3-carbonitrile, belongs to pyrazoles-derivatives 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 120068-79-3, Safety of 5-Amino-1-(2,6-dichloro-4-(trifluoromethyl)phenyl)-1H-pyrazole-3-carbonitrile

General procedure: Phenylpyrazole (0.2 mmol), arylboronic acid (0.4 mmol), NIS (0.2 mmol), [Pd] (10 mol%), NaHCO3 (0.4 mmol) and C2H5OH:H2O (3:1, 10 mL), were added to a Schlenk tube. Then the tube was charged with N2 and the reaction mixture was stirred at 80 C for 18 h. After the completion of the reaction, as monitored by TLC, the mixture was cooled and filtrated. The filtrate was extracted with ethyl acetate and washed with brine. Then the combined organic extracts were dried over Na2SO4, concentrated under vacuum and the resulting residue was purified by silica gel column chromatography to afford the desired products.

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These common heterocyclic compound, 5932-20-7, name is 3-Bromo-4-methyl-1H-pyrazole, 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 5932-20-7

To a solution of 58 (120 mg, 0.74 mmol) in dimethylformamide (DMF) (1 mL) was added NaH (40 mg, 1.6 mmol). The mixture was stirred for 0.5 h at room temperature and 2- bromo-l,3-thiazole (125 mg, 0.74 mmol) was added. The reaction mixture was stirred for 1 h at room temperature. The reaction temperature was raised to 90C and stirred overnight. The reaction was quenched with MeOH and solvent was removed in vacuo. The residue was treated with water and EtOAc. The organic layer was separated and aqueous was extracted with EtOAc. The combined organic phase was dried over a2S04, filtered, and concentrated to give crude product. The crude product was purified on ISCO columns. Fractions containing pure product were combined and evaporated to give 59 (67 mg, 37%) as a yellow solid.

The synthetic route of 3-Bromo-4-methyl-1H-pyrazole has been constantly updated, and we look forward to future research findings.

Adding a certain compound to certain chemical reactions, such as: 155600-99-0, name is 3,5-Dibromo-1-methyl-4-nitro-1H-pyrazole, belongs to pyrazoles-derivatives 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 155600-99-0, Quality Control of 3,5-Dibromo-1-methyl-4-nitro-1H-pyrazole

Nucleophilic aromatic substitution of the compound 2 with benzylamine in DMSO produces benzyl-(5-bromo-2-methyl-4-nitro-2H-pyrazol-3-yl)-amine 3.

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.

Electric Literature of 10199-68-5, A common heterocyclic compound, 10199-68-5, name is 4-Phenyl-1H-pyrazole, molecular formula is C9H8N2, 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.

4-phenyl-lH-pyrazole (775 mg, 5.38 mmol, 1.0 eq), l-iodo-3-methoxybenzene (1510 mg, 768 mu, 6.45 mmol, 1.2 eq), Cul (21 mg, 0.11 mmol, 0.02 eq) and 2C03 (1561 mg, 11.30 mmol, 2.1 eq) were added to a dry pressure tube equipped with a magnetic stir bar. Then trans- 1,2-cyclohexanediamine (123 mg, 1.08 mmol, 0.20 eq) and dioxane (12 mL) were added. The mixture was bubbled with nitrogen for 30 minutes and then the tube was sealed. The mixture was stirred in an oil bath at a temperature of 110 C for three days and then cooled to ambient temperature. The solvent was removed under reduced pressure and the residue was purified through column chromatography on silica gel using hexane and ethyl acetate (10: 1 -5 : 1 -3 : 1) as eluent to obtain the desired product, l-(3-methoxyphenyl)-4-phenyl-lH-pyrazole 8, as a colorless liquid (1.13 g in 84% yield). H NMR (DMSO-Je, 400 MHz): delta 3.84 (s, 3H), 6.87-6.90 (m, 1H), 7.25 (t, J = 12 Hz, 1H), 7.38-7.48 (m, 5H), 7.71 (d, J= 7.2 Hz, 2H), 8.20 (s, 1H), 9.01 (s, 1H).

The synthetic route of 10199-68-5 has been constantly updated, and we look forward to future research findings.

Some common heterocyclic compound, 35344-95-7, name is 1H-Pyrazole-4-carbaldehyde, molecular formula is C4H4N2O, 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 35344-95-7

into a 100-mL round-bottom flask, was placed a solution of tert-butyl N-[3-(methanesulfonyloxy)cyclobutyl]carbamate (2.65 g, 9.99 mmol, 1.00 eq.), 1H-pyrazole-4-carbaldehyde (1.152 g, 11.99 mmol, 1.20 eq.) and Cs2CO3 (6.52 g, 20.01 mmol, 2.00 eq.) inDMF (20 mL). The resulting solution was stirred for 4 h at room temperature. The reaction was then quenched by the addition of 100 mL of water. The resulting solution was extracted with 3×100 mL of ethyl acetate and the organic layers combined. The resulting mixture was washed with 100 mL of brine. The mixture was dried over anhydrous sodium sulfate andconcentrated under vacuum. The crude product was purified by Flash-Prep-HPLC with the following conditions (CombiFlash-1): Column, C18 silica gel; mobile phase, MeCN/H20=60:40 increasing to MeCN/H20=70:30 within 3 mm; Detector, UV 254 nm. The crude product was purified by Prep-SFC with the following conditions (prep SFC 350-2):Column: Phenomenex Lux 5u Cellulose-4 250*50mm; mobile Phase A: C02:70, Mobile PhaseB: MeQH-HPLC:30; Flow rate: 150 mL/min; 254 nm; RT1:4.53; RT2:5.36. This resulted in 712 mg (54%) of tert-butyl N-[cis-3 -(4-formyl- 1 H-pyrazol- 1 -yl)cyclobutyl]carbamate as a white solid.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 35344-95-7, its application will become more common.

Reference of 2075-46-9, 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. 2075-46-9, name is 4-Nitro-1H-pyrazole, This compound has unique chemical properties. The synthetic route is as follows.

EXAMPLE 119 This example illustrates the preparation of Compound 108 namely, 3-pyridinecarboxylic acid, 5-[(4-amino-1H-pyrazol-1-yl)carbonyl]-2-methoxy-4-(2-methylpropyl)-6-(trifluoromethyl)-, methyl ester. A solution of 4-nitropyrazole (22.62 g, 200 mmol) in THF (100 mL) was cooled to 0 C., then sodium bis(trimethylsilyl)amide (204.3 mmol) in THF solution was added dropwise. A solution of Compound 84 (70.75 g, 200 mmol) in THF (100 mL) was then added dropwise at 0 C., then the pot was stirred at 25 C. for 30 minutes. The reaction mixture was then poured into 5% hydrochloric acid and extracted with dichloromethane. The organic layer was dried with MgSO4 and the solvent removed by rotary evaporation. The residue was purified by silica gel chromatography (5% ethyl acetate: hexane) to give 70.14 g (82%) of the pyrazole amide (Compound 101).

The chemical industry reduces the impact on the environment during synthesis 4-Nitro-1H-pyrazole. I believe this compound will play a more active role in future production and life.

Adding a certain compound to certain chemical reactions, such as: 5334-40-7, name is 4-Nitro-1H-pyrazole-3-carboxylic acid, belongs to pyrazoles-derivatives 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 5334-40-7, Formula: C4H3N3O4

To a solution of 4-nitro-1H-pyrazole-3-carboxylic acid (1.00 g, 6.37 mmol) in DMF (20 mL) were added K2C03 (1.93 g, 14.01 mmol) and iodomethane (1.99 g, 14.01 mmol), and the mixture was stirred at rt overnight under nitrogen. Water (50 mL) was added and the mixture was extracted with EtOAc (3 x 60 mL). The combined organic layers were washed with brine (25 mL), dried over anhydrous Na2SO4 and concentrated. The residue was purified by silica gel chromatography eluting with petroleum ether EtOAc (8: ito 1:2) to afford methyl 1- methyl-4-nitro- 1H-pyrazole-3-carboxylate.

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