Category: 4058-91-7

Synthetic Route of 4058-91-7, These common heterocyclic compound, 4058-91-7, name is 5-Amino-1-methyl-1H-pyrazole-4-carboxylic acid, 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.

0.47g first After completion of the reaction, first substitution reaction 3h; after completion 0 C of the dropwise addition, 10 ml cooling, circulating water, and vacuum distillation, to obtain a yellow viscous solid, namely second intermediate (1 – methyl -5 – amino – 111H-pyraz -4 -benzoyl chloride); after completion of the dropwise addition reaction, is carried out under stirring.

Statistics shows that 5-Amino-1-methyl-1H-pyrazole-4-carboxylic acid is playing an increasingly important role. we look forward to future research findings about 4058-91-7.

Reference:
Patent; Nankai University; Li Huabin; Li Luyang; Gu Jian; Kuang Xinyi; Xia Zhe; Zhang Shangzhong; Guo Lihui; Chen Rui; (16 pag.)CN110066282; (2019); A;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Reference of 4058-91-7,Some common heterocyclic compound, 4058-91-7, name is 5-Amino-1-methyl-1H-pyrazole-4-carboxylic acid, molecular formula is C5H7N3O2, 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.

To a stirred solution of Step 3 intermediate (800 mg, 5.666 mmol) in dry DMF (8 ml), 2-bromo- l-(2-chlorophenyl)ethanone (1.32 g, 5.666 mmol) was added followed by potassium fluoride (500 mg, 8.499 mmol) at room temperature and the resultant reaction mixture was stirred overnight. The mixture was quenched with water (75 mL) and ethyl acetate (30 mL). The layers were separated and the aqueous layer was extracted with ethyl acetate (3 x 100 mL). The combined organic layers were washed with water (2 x 100 mL) and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure and the residue obtained was purified by flash silica gel column chromatography to afford 912 mg of the desired product as a solid. lH NMR (300 MHz, DMSO-d6): delta 3.54 (s, 3H), 5.31 (s, 2H), 6.31 (s, 2H), 7.43-7.53 (m, 1H), 7.55 (d, = 4.8 Hz, 1H), 7.77 (d, = 7.5 Hz, 2H), 7.95 (s, 1H).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 5-Amino-1-methyl-1H-pyrazole-4-carboxylic acid, its application will become more common.

Reference:
Patent; GLENMARK PHARMACEUTICALS S.A.; KUMAR, Sukeerthi; CHAUDHARI, Sachin Sundarlal; GHARAT, Laxmikant Atmaram; KHAIRATKAR-JOSHI, Neelima; SHAH, Daisy Manish; MUKHOPADHYAY, Indranil; (327 pag.)WO2018/203298; (2018); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

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. 4058-91-7, name is 5-Amino-1-methyl-1H-pyrazole-4-carboxylic acid belongs to pyrazoles-derivatives compound, it is a common compound, a new synthetic route is introduced below. HPLC of Formula: C5H7N3O2

As shown in Scheme 1, 3-substituted phenyl-5-methylisoxazole-4-carboxylic acid (0.02mol) was added to distillated SOCl2 (50 mL) and reacted at 80 C for 5 h to obtainintermediate 2. Then, intermediate 2 (0.02 mol) was added dropwise to a stirred solution of5-amino-1-methyl-1H-pyrazole-4-carboxylic acid (0.02 mol) in anhydrous tetrahydrofuran (THF,100 mL) and trimethylamine, the reaction mixture was stirred at room temperature for 2.0 h.The reaction mixture was poured into cold 5.0% dilute HCl solution (200 mL). The solid obtainedwas filtered, washed several times with water, dried to give the crude product which was furtherrecrystallized and dried to give intermediate 3. A mixture of intermediate 3 (0.02 mol) and aceticanhydride (0.2 mol) was heated under reflux for 4.0 h. The solvent was removed under reducedpressure. The residue was washed with water. The separated solid was collected by filtration,washed with water, dried, and recrystallized and dried to give intermediate 4. To a solution ofintermediate 4 (10 mmol) in THF (50 mL), 6 mL of 80% hydrazine hydrate was added slowly atroom temperature. Then, the mixture was further reacted at room temperature for 2 h. The solventwas removed under reduced pressure, and the residue was washed with water and anhydrousethanol to give the crude product, then recrystallized by ethanol and dried under vacuum to give thekey intermediate 3-(2-chlorophenyl)-N-(4-(hydrazinecarbonyl)-1-methyl-1H-pyrazol-5-yl)-5-methylisoxazole-4-carboxamide 5.

The synthetic route of 4058-91-7 has been constantly updated, and we look forward to future research findings.

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. 4058-91-7, name is 5-Amino-1-methyl-1H-pyrazole-4-carboxylic acid, A new synthetic method of this compound is introduced below., Quality Control of 5-Amino-1-methyl-1H-pyrazole-4-carboxylic acid

56 To a solution of 5-AMINO-L-METHYL-LH-PYRAZOLE-4- carboxylic acid (7.1 g), N- (2-AMINOETHYL) tritylamine (15.1 g) and triethylamine (10.1 g) in chloroform (200 ml) was added N- (3-DIMETHYLAMINOPROPYL)-N – ethylcarbodiimide hydrochloride (9.6 g), and the mixture was stirred at room temperature for 16 hours. The reaction mixture was washed successively with 10% aqueous citric acid solution, brine and saturated aqueous sodium hydrogencarbonate solution. The organic layer was dried over anhydrous sodium sulfate, filtered and concentrated in vacuo. The residue was triturated with ethyl acetate and dried in vacuo to give 5-AMINO-1- METHYL-N- [2- (TRITYLAMINO) ETHYL]-LH-PYRAZOLE-4- carboxamide (11.4 g) as a solid. 1H-NMR (CDCl3) 8 2.35-2. 38 (2H, m), 3.45-3. 49 (2H, M), 3.63 (3H, s), 5.15 (1H, br), 5.91 (1H, br), 7.17-7. 49 (16H, m)

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.