127107-23-7 | pyrazoles-derivatives

Sep-21 News Continuously updated synthesis method about 127107-23-7

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

Electric Literature of 127107-23-7, 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. 127107-23-7, name is 1-Methyl-1H-pyrazol-4-amine hydrochloride, This compound has unique chemical properties. The synthetic route is as follows.

Step 4) fert-butyl 5-((5-chloro-2-((l-methyl-lH-pyrazol-4-yl)amino)pyrimidin-4-yl)amino)-5- (cvanomethyl)hexahydrocvclopentarc1pyrrole-2(lH)-carboxylate [0464] To a suspension of tert-butyl 5-(cyanomethyl)-5-((2,5-dichloropyrimidin-4-yl)amino) hexahydrocyclopenta[c]pyrrole-2(lH)-carboxylate (631.5 mg, 1.53 mmol) and 1-methyl-lH- pyrazol-4-amine hydrochloride (213.2 mg, 1.60 mmol) in -BuOH (10 mL) was added Et3N (322.1 mg, 3.18 mmol). The reaction mixture was stirred at 150 C in a sealed tube overnight and concentrated in vacuo. The residue was purified by silica gel column chromatography (MeOH/DCM (v/v) = 1/50) to give the title compound as a yellow solid (283.0 mg, yield 39.1%). LC-MS (ESI, pos. ion) m/z: 473.3 [M+H]+.

Reference:
Patent; SUNSHINE LAKE PHARMA CO., LTD.; CALITOR SCIENCES, LLC; XI, Ning; LI, Minxiong; LI, Xiaobo; CHEN, Wuhong; ZHANG, Tao; HU, Haiyang; DAI, Weilong; WU, Yanjun; (192 pag.)WO2017/44434; (2017); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

17-Sep-2021 News Research on new synthetic routes about 127107-23-7

In a pressure tube, l-methylpyrazol-4-amine HCI (21 mg, 0.16 mmol), (S,2S)-2-(6-((2- bromo pyridin-4-yl)methoxy)-4-methoxybenzo[cf|thiazol-2-ylamino) cyclohexanol (60 mg, 0.13 mmol), RuPhos Pd G4 (11 mg, 0.013 mmol), RuPhos (6 mg, 0.013 mmol) and Cs2C03 (127 mg, 0.39 mmol) were dissolved in 1,4-dioxane (2 mL). The tube was sealed and purged with N2. The reaction mixture was stirred at 85C for 3h. LCMS monitored the reaction. The mixture was filtered and purified by mass-triggered preparative HPLC (Mobile phase: A = 10M NH4HCO3/H2O, B = MeCN; Gradient: B = 30-60%; 10.0 min; Column: C18) to give (15′,25)-2-(4-methoxy-6-((2-(l-methyl-lH-pyrazol-4-ylamino)pyridin-4-yl) (1492) methoxy)benzo[cf|thiazol-2-ylamino)cyclohexanol (5 mg, 9%) as a white solid. MS (ES+) C24H28N603S requires: 480, found: 481 [M+H]+. NMR (500MHz, DMSO) delta 8.81 (s, 1H), 8.07 (d, J = 5.3 Hz, 1H), 7.91 (s, 1H), 7.61 (d, J = 7.5 Hz, 1H), 7.37 (s, 1H), 6.91 (d, J = 2.3 Hz, 1H), 6.70 (s, 1H), 6.65 (d, J= 5.3 Hz, 1H), 6.54 (d, J = 2.2 Hz, 1H), 5.02 (s, 2H), 4.77 (d, J = 5.0 Hz, 1H), 3.83 (s, 3H), 3.79 (s, 3H), 3.51 (s, 1H), 2.02 (s, 1H), 1.87 (d, J = 11.2 Hz, 1H), 1.63 (t, J= 10.8 Hz, 2H), 1.23 (s, 5H).

Reference:
Patent; TESARO, INC.; JONES, Philip; CZAKO, Barbara; BURKE, Jason P.; CROSS, Jason; LEONARD, Paul Graham; TREMBLAY, Martin; MANDAL, Pijus; (232 pag.)WO2018/119387; (2018); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

September 16, 2021 News Some tips on 127107-23-7

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.

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. 127107-23-7, name is 1-Methyl-1H-pyrazol-4-amine hydrochloride, A new synthetic method of this compound is introduced below., Computed Properties of C4H8ClN3

The 2,5-dichloro-N-(6-methoxyhexahydrofuro[3,2-b]furan-3-yl)pyrimidin-4-amine (430mg, 1.4046 mmol), diisopropylethylamine (546.7 mg, 4.23 mmol) and 1-methylpyrazol-4-amine hydrochloride (283.3 mg,2.12 mmol) was dissolved in n-BuOH (10 mL), the temperature of the reaction solution was raised to 150 C, sealed tube reaction for 23 hours, and then concentrated under reduced pressure.The residue was purified by silica gel column chromatography (DCM / MeOH (v / v) = 50/1) to afford the title compound as a white solid which was recrystallized from acetone to give the title compound as a white solid (220 mg, 42.6% ).

Reference:
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Jiatuo Sciences Corporation; Xi Ning; Li Minxiong; Li Xiaobo; Dai Weilong; Wang Tingjin; (74 pag.)CN104926824; (2017); B;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

9/9/2021 News Some tips on 127107-23-7

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.

Adding a certain compound to certain chemical reactions, such as: 127107-23-7, name is 1-Methyl-1H-pyrazol-4-amine hydrochloride, 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 127107-23-7, Product Details of 127107-23-7

. Into a 2000-mL 3-necked round-bottom flask, were placed a solution of intermediate 24.3 (56 g, 152.22 mmol, 1.00 equiv) in n-butanol (1000 mL) and 1- methyl-1H-pyrazol-4-amine hydrochloride (40.89 g, 306.11 mmol, 2.01 equiv). The reaction was stirred overnight at 110 C in an oil bath. Upon completion, the reaction was cooled to room temperature solids were collected by filtration and the resulting solution was diluted with 500 mL of H20. The pH value of the solution was adjusted to 10 with sodium hydroxide (1 mol/L). The resulting solids were collected by filtration and dried in an oven under reduced pressure to furnish 61.9 g (95%) of compound 1-24 as an off-white solid. LCMS: (ES, m/z):429 [M+H] ?HNMR: (400MHz, CD3OD): ?5 7.877(1H, s), 7.568(1H, s), 4.044(1H, s), 3.887(3H, s), 3.751- 3.740(4H, d), 2.692-.2638(7H, m), 2.343(1H, s), 2.264(2H, s), 2.099(2H, s), 1.514-1.392(4H, m).

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; NIMBUS IRIS, INC.; ROMERO, Donna L.; MASSE, Craig E.; ROBINSON, Shaughnessy; GREENWOOD, Jeremy Robert; HARRIMAN, Geraldine; WO2015/48281; (2015); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Simple exploration of 127107-23-7

According to the analysis of related databases, 127107-23-7, the application of this compound in the production field has become more and more popular.

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 127107-23-7 as follows. Quality Control of 1-Methyl-1H-pyrazol-4-amine hydrochloride

6-((2,5-dichloropyrimidin-4-yl)(methyl)amino)hexahydrofuro[3,2-b]furan-3-ol (342.2mg, 1.12 mmol) and 1-methyl-1H-pyrazol-4-amine hydrochloride (185.0 mg,1.38 mmol) was suspended in n-BuOH (5 mL) and DIPEA (358.8 mg, 2.78 mmol) was added. The resulting reaction was warmed to 150 C and the sealed tube was allowed to react overnight. The reaction mixture was concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (DCM / MeOH (v / v) = 40/1) to give the title compound as a beige solid (156 mg, 38.0%).

According to the analysis of related databases, 127107-23-7, the application of this compound in the production field has become more and more popular.

Introduction of a new synthetic route about 127107-23-7

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 1-Methyl-1H-pyrazol-4-amine hydrochloride, its application will become more common.

Related Products of 127107-23-7,Some common heterocyclic compound, 127107-23-7, name is 1-Methyl-1H-pyrazol-4-amine hydrochloride, molecular formula is C4H8ClN3, 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: To 8a (0.25 g, 0.95 mmol) and 1-methyl-1H-pyrazol-4-amine hydrochloridesalt (0.14 g, 1.1 mmol) in n-butanol (5 mL) was added trifluoroaceticacid (0.27 g, 2.4 mmol), and the mixture was stirredovernight at 120 C. The mixture was then concentrated, neutralizedwith ammonia in methanol, and purified by column chromatography(dichloromethane: methanol=60:1) to yield 0.26 g (86.7%) of 9a as apale-yellow solid. MS (ESI) m/z 326 [M+H]+.

Reference:
Article; Yu, Ru-Nan; Chen, Cheng-Juan; Shu, Lei; Yin, Yuan; Wang, Zhi-Jian; Zhang, Tian-Tai; Zhang, Da-Yong; Bioorganic and Medicinal Chemistry; vol. 27; 8; (2019); p. 1646 – 1657;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Extracurricular laboratory: Synthetic route of 127107-23-7

HATU (0.329 g, 0.867 mmol), DBU (0.152 g, 1.000 mmol) and 1- methyl-lH-pyrazol-4-amine hydrochloride (0.0745 mL, 0.800 mmol) were added to 6- bromoquinazolin-4(3H)-one (0.150 g, 0.667 mmol) in MeCN (3.5 mL). The solution was aged for 25 hours at ambient temperature before it was diluted with EtOAc and washed with brine-water. The concentrated organics were purified via silica gel chromatography eluting with 2% MeOH-EtOAc to yield 6-bromo-3-(l-methyl-lH-pyrazol-4-yl)quinazolin-4(3H)-one (0.018 g, 0.059 mmol, 18% yield).

Reference:
Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; GRINA, Jonas; HANSEN, Joshua D.; LAIRD, Ellen; MATHIEU, Simon; MORENO, David; REN, Li; RUDOLPH, Joachim; WENGLOWSKY, Steven Mark; WO2012/118492; (2012); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Simple exploration of 1-Methyl-1H-pyrazol-4-amine hydrochloride

The synthetic route of 127107-23-7 has been constantly updated, and we look forward to future research findings.

127107-23-7, name is 1-Methyl-1H-pyrazol-4-amine hydrochloride, 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. HPLC of Formula: C4H8ClN3

6-((2-chloropyrimidin-4-yl)(methyl)amino)hexahydrofuro[3,2-b]furan-3-ol (358.0 mg, 1.32 mmol) and 1-methyl-1H-pyrazole-4-amine hydrochloride were dissolved in n-BuOH (5 mL), and DIPEA (434.6 mg, 3.36 mmol). The resulting reaction was warmed to 150 C and the tube was allowed to react overnight. The reaction mixture was concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (DCM / MeOH (v / v) = 10/1) to give the title compound as a beige solid (300 mg, 68.4%).

The synthetic route of 127107-23-7 has been constantly updated, and we look forward to future research findings.

The important role of 1-Methyl-1H-pyrazol-4-amine hydrochloride

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 1-Methyl-1H-pyrazol-4-amine hydrochloride, and friends who are interested can also refer to it.

To a 25 mL round-bottom flask containing a solution of intermediate 20.1 (110 mg, 0.27 mmol, 1.00 equiv) in n-Butanol (6 mL) was added 1-methyl- 1H-pyrazol-4-amine hydrochloride (103.2 mg, 0.77 mmol, 2.85 equiv) at room temperature under nitrogen. The reaction was stirred overnight at 110 C in an oil bath. After cooling, the resulting mixture was concentrated under vacuum and resulting crude was purified using flash column chromatography to furnish 120 mg (95%) of compound 1-21 as a yellow solid. LCMS (ES, m/z): 467 [M+H] ?H NMR (400MHz, CDC13): 5 9.02 (1H, s), 7.81 (1H, s), 7.46 (1H, s),7.43 (1H, brs), 4.05-3.93 (1H, m), 3.79 (3H, s), 2.98 (2H, q), 2.53-2.50 (4H, m), 2.39-2.28 (1H, m), 2.05-1.94 (2H, m), 1.85 (2H, d), 1.58-1.30 (8H, m), 1.31 (3H, t), 0.23 (4H,s).

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 1-Methyl-1H-pyrazol-4-amine hydrochloride, and friends who are interested can also refer to it.

Some tips on 127107-23-7

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 127107-23-7, its application will become more common.

Some common heterocyclic compound, 127107-23-7, name is 1-Methyl-1H-pyrazol-4-amine hydrochloride, molecular formula is C4H8ClN3, 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. category: pyrazoles-derivatives

Into a 25 mL round-bottom flask, were placed intermediate 44.3 (300 mg, 0.74 mmol, 1.00 equiv), 1-methyl-1H-pyrazol-4-amine hydrochloride (119 mg, 0.89 mmol, 1.20 equiv), hydrogen chloride in dioxane (0.5 mL) and n-BuOH (5 mL). The reaction was stirred for 12 h at 110 C. Upon completion of the reaction resulting mixture was concentrated under vacuum. The solution was adjusted to pH 9-10 with sodium hydroxide (2M) and resulting solids were collected by filtration. The crude product was purified by recrystallization from methanol to furnish 208.8 mg (61%) of compound 1-45 as a yellow solid. LCMS (ES, mlz): 465.4[M+H] ?H NMR (300MHz, CD3OD): 7.86 (1H, s), 7.54 (1H, s), 6.75-7.11 (1H, t), 4.05 (1H, s), 3.85 (3H, s), 3.78 (4H, t), 2.60 (4H, s), 2.08-2.32 (5H, m), 1.29-1.47 (4H, m).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 127107-23-7, its application will become more common.