Day: September 8, 2021

Electric Literature of 2972-52-3, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.2972-52-3, name is 2,4-Dichloro-5-pyrimidinecarbonyl chloride, molecular formula is C5HCl3N2O, molecular weight is 211.43, as common compound, the synthetic route is as follows.

2,4-dichIoro-2,4-(morpho A solution of 2,4-dichloropyrimidine-5-carbonyl chloride (422mg, 2,0 mmoi) in dichloromethane (10 mL) was added 4-(morpholinosulfonyl)aniline (508 nig. 2.1 mmoi) and DIEA (387 mg, 3.0 mmoi) at 0 C. The resulting mixture was stirred at 0 C for 1 h, Then, water was added. The resulting mixture was extracted with EtOAc (3x). The combined organic layers were dried (NaSO4), filtered and concentrated. The residue was purified on ISCO to give the title compound as a white solid (701.2 mg, 84%). 1H NMR (400 MHz, DMSO-d6) delta 1 1.98 – 1 1.90 (m5 I B), 8.29 (d, J = 6.4 Hz, IH), 7.89 (d, J = 8.8 Hz, 2H), 7.69 (d, J= 8.8 Hz, 2H), 3.65 – 3.56 (m, 4H), 2.87 – 2.78 (m, 4H); MS m/z 418,30 [M+H]+

Statistics shows that 2972-52-3 is playing an increasingly important role. we look forward to future research findings about 2,4-Dichloro-5-pyrimidinecarbonyl chloride.

Reference:
Patent; THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL; WANG, Xiaodong; ZHANG, Weihe; KIREEV, Dmitri; LIU, Jing; MCIVER, Andrew Louis; WO2014/85225; (2014); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application of 1448307-66-1, 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. 1448307-66-1, name is 1-(2-Chloropyrimidin-4-yl)-3-methyl-1H-pyrazole-4-carbaldehyde, molecular formula is C9H7ClN4O, The 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.

A stirred suspension of commercially available l-(2-chloro-4-pyrimidinyl)-3-methyl- lH-pyrazole-4-carbaldehyde (222 mg, 1.0 mmol) and 3-azetidinol hydrochloride (219 mg, 2.0 mmol) in dichloromethane (10 mL) was treated with triethylamine (700 muTau, 5.0 mmol) followed by portionwise addition of Na(OAc)3BH (636 mg, 3.0 mmol). The resulting mixture was stirred at room temperature overnight. Next morning, LCMS indicated clean conversion to product. The reaction mixture was transferred to a separately funnel, diluted with dichloromethane, washed with saturated aqueous NaHC03 solution. The organic layer was dried over anhydrous MgS04, filtered and concentrated in vacuo. The crude product was obtained as a white foam (185 mg, 0.66 mmol, 66%) and used directly in the next step. LC/MS – HPLC (254 nm) – Rt 1.04 min. MS (ESI) m/z 280.5 [M+ + H+]. Purity = 95 % by UV (254 nm).

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 1448307-66-1, 1-(2-Chloropyrimidin-4-yl)-3-methyl-1H-pyrazole-4-carbaldehyde.

Reference:
Patent; SIGNALRX PHARMACEUTICALS, INC.; MORALES, Guillermo, A.; GARLICH, Joseph, R.; DURDEN, Donald, L.; (155 pag.)WO2018/226739; (2018); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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. 1005-37-4, name is 6-Chloro-N4-methylpyrimidine-2,4-diamine. A new synthetic method of this compound is introduced below., Computed Properties of C5H7ClN4

General procedure: General Procedure 5: To a mixture of a suitable chloropyrimidine derivative (1 equiv.) in DMF/water (9: 1) is added the appropriate boronic acid (or boronic ester) derivative (1.1 equiv.), Na2C03 (2 equiv.) and Pd(PPh3)4 (0.1 equiv.). The mixture is heated at 120 C overnight or in the microwave until the reaction is complete as shown by LCMS. The crude mixture is then purified by preparative HPLC to afford the desired product.

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, 1005-37-4, 6-Chloro-N4-methylpyrimidine-2,4-diamine.

Reference:
Patent; THOMAS HELLEDAYS STIFTELSE FOeR MEDICINSK FORSKNING; SCOBIE, Martin; WALLNER, Olov; KOOLMEISTER, Tobias; VALLIN, Karl Sven Axel; HENRIKSSON, Carl Martin; HOMAN, Evert; HELLEDAY, Thomas; JACQUES, Sylvain; DESROSES, Matthieu; JACQUES-CORDONNIER, Marie-Caroline; FISKESUND, Roland Julius Yu; (359 pag.)WO2015/187089; (2015); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adding a certain compound to certain chemical reactions, such as: 1820-81-1, 5-Chlorouracil, 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, 1820-81-1, blongs to pyrimidines compound. category: pyrimidines

Method 19 2,4,5-Trichloropyrimidine 5-Chlorouracil (10.0 g, 68.5 mmol) was dissolved in phosphorus oxychloride (60 ml) and phosphorus pentachloride (16.0 g, 77 mmol) was added. The reaction mixture was then stirred at reflux (110 C.) for 16 hrs then allowed to cool to 20 C. The reaction mixture was then poured slowly and carefully into water (200 ml) at 25 C. with vigorous stirring. Then stirred well for 90 minutes before addition of EtOAc (250 ml). Organic layer separated off and aqueous layer re-extracted into EtOAc (250 ml). The organic layers were then combined and washed with sodium bicarbonate (200 ml aqueous solution), brine (200 ml) and then evaporated to a yellow liquid. The crude material was purified by column chromatography eluding with dichloromethane to afford the product as a yellow liquid (6.37 g, 51%). NMR (CDCl3): 8.62 (s, 1H); MS (M+): 182, 184,186.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,1820-81-1, its application will become more common.

Reference:
Patent; Pease, Elizabeth Janet; Breault, Gloria Anne; Morris, Jeffrey James; US2003/149064; (2003); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthetic Route of 131860-97-4, 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. 131860-97-4, name is (E)-Methyl 2-(2-((6-chloropyrimidin-4-yl)oxy)phenyl)-3-methoxyacrylate, molecular formula is C15H13ClN2O4, The 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.

Example 1: In a 500 mL flask equipped with a magnetic stirrer, (E)-methyl 2-(2- ((6-chloropyrimidin-4-yl)oxy)phenyl)-3-methoxyacrylate (100 g, 97 % pure, 302 mmol), 2-hydroxybenzonitrile (41 g, 341 mmol) and potassium carbonate (25.08 g, 181 mmol) were added. Water (50 mL) and /V-methyl- piperidine (2.86 g, 28.8 mmol) were added at ambient temperature, then the mixture was placed on an oil bath at ambient temperature and heating begun. The mixture was heated to 120 C over 20 min and stirring begins once the external temperature is approx. 80 C. Some gas evolution was noted. The mixture was stirred at 100 C for 5 h, under a mild reflux. The mixture was then cooled to 80 C and diluted with ethyl acetate (200 mL) and then with water (100 mL). The two phases were stirred and separated. The upper organic portion was evaporated to dryness under vacuum at 40 C. The crude residue was dissolved in methanol (200 mL) at reflux, then water (30 mL) was added slowly at that temperature. The solution was allowed to cool freely with agitation to ambient temperature over lh and the solution was seeded with 0.4 g pure azoxystrobin at 40 C. The resulting slurry was further cooled to 0 C over 20 min, and held there for a further 20 min, then the solids were recovered by suction filtration and washed with 50 mL cold methanokwater 4: 1. The filter cake was dried under vacuum at ambient temperature overnight, affording the product azoxystrobin (114.68 g, 97% pure, 91.2 % yield) as a free flowing pale brown powder.

According to the analysis of related databases, 131860-97-4, the application of this compound in the production field has become more and more popular.

Reference:
Patent; CHEMINOVA A/S; LINDSAY, Karl Bernhard; WO2014/190997; (2014); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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. 49845-33-2, name is 2,4-Dichloro-5-nitropyrimidine, the common compound, a new synthetic route is introduced below. SDS of cas: 49845-33-2

[00510] To a solution of 2,4-dichloro-5-nitropyrimidine (582 mg, 3 mmol) in THF (5 mL) wasadded DIEA (775 mg, 6 mmol) and tert-butyl3-aminophenylcarbamate (625 mg, 3 mmol, in 2mL THF) at -78 °C underN2 atmosphere. After stirring at -78 °C for 30 min, the reaction waswarmed up tor. t. and stirred overnight. The reaction was quenched with water (10 mL) andextracted with IPA/DCM (15:85) (5 mL X 3). The combined organic layer was washed withbrine, and dried over Na2S04. The solvents were removed under vacuum and the residue waspurified by flash chromatography (silica gel, 0 to 5percent ethyl acetate in PE/DCM (Ill) with 0.5percentTEA) to provide tert-butyl 3-(2-chloro-5-nitropyrimidin-4-ylamino )phenylcarbamate (1)(1.087g, 99percent) as an orange solid. LC-MS (ESI) m/z (M/M+2) 366.2/368.2.

The synthetic route of 49845-33-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; PHARMACYCLICS, INC.; CHEN, Wei; YAN, Shunqi; LOURY, David, J.; FRYE, Leah, Lynn; GREENWOOD, Jeremy, Robert; SHELLEY, Mee, Yoo; WANG, Longcheng; WO2014/130693; (2014); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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. 62802-42-0, name is 2-Chloro-5-fluoropyrimidine, molecular formula is C4H2ClFN2, The 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. category: pyrimidines

To a solution of 2- chloro-5-fluoropyrimidine (10.0 g, 75.46 mmol, Sigma Aldrich) in DMF (100 mL) was added tributyl(vinyl)tin (31.1 g, 98.09 mmol) at RT. The reaction mixture was purged with N2for 5 min and Pd(PPh3)4(2.62 g, 2.26 mmol) was added. The reaction mixture was further degassed with N2for 5 min and stirred at 100 C for 24 h. After completion of the reaction (monitored by TLC), the reaction mixture was cooled to RTand quenched with water (100 mL). The aqueous layer was extracted with diethyl ether (2 x 100 mL) and the combined organic layers were washed with brine (100 mL), dried over anhydrous Na2SO4, and concentrated in vacuo to obtain the initial product which was purified by silica gel chromatography (eluent: 6% EtOAc in hexanes) to provide 400.1 (8.0 g, 85% yield) as an oil.1H NMR (400 MHz, CDCl3) delta 8.58- 8.49 (m, 2H), 6.86 (dd, J = 17.4, 10.6 Hz, 1H), 6.53 (d, J = 17.3 Hz, 1H), 5.70 (d, J = 10.6 Hz, 1H). LCMS-ESI (pos.) m/z: = 125.1.

With the rapid development of chemical substances, we look forward to future research findings about 62802-42-0.

Reference:
Patent; AMGEN INC.; CHEN, Ning; CHEN, Xiaoqi; CHEN, Yinhong; CHENG, Alan C.; CONNORS, Richard V.; DEIGNAN, Jeffrey; DRANSFIELD, Paul John; DU, Xiaohui; FU, Zice; HARVEY, James S.; HEATH, Julie Anne; HEUMANN, Lars V.; HORNE, Daniel B.; HOUZE, Jonathan; KALLER, Matthew R.; KAYSER, Frank; KHAKOO, Aarif Yusuf; KOPECKY, David J.; LAI, Su-Jen; MA, Zhihua; MEDINA, Julio C.; MIHALIC, Jeffrey T.; NISHIMURA, Nobuko; OLSON, Steven H.; PATTAROPONG, Vatee; SWAMINATH, Gayathri; WANG, Xiaodong; WANSKA, Malgorzata; YANG, Kevin; YEH, Wen-Chen; (700 pag.)WO2018/97945; (2018); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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. 287714-35-6, name is Methyl 2-chloropyrimidine-5-carboxylate. A new synthetic method of this compound is introduced below., Formula: C6H5ClN2O2

A solution of methyl 2-chloropyrimidine-5-carboxylate (200 mg, 1.16 mmol) in dichloromethane (4.00 mL) was added to a stirred solution of 1-methyl-1,4-diazepane (0.144 mL, 1.16 mmol) and N-ethyl-N-propan-2-ylpropan-2-amine (0.902 mL, 5.22 mmol) in dichloromethane (4.00 mL) at 25 C. The resulting solution was stirred at ambient temperature for 18 h. The reaction mixture was evaporated to dryness and redissolved in MeOH (20 mL) and the crude product was purified by ion exchange chromatography, using an SCX column. The desired product was eluted from the column using 7M NH3/MeOH and evaporated to dryness to afford methyl 2-(4-methyl-1,4-diazepan-1-yl)pyrimidine-5-carboxylate (274 mg, 94%) as a white solid. This was used directly with no further purification. 1H NMR (399.9 MHz, DMSO-d6) delta 1.86-1.89 (2H, m), 2.26 (3H, s), 2.49-2.54 (2H, m, partially obscured by DMSO peak), 2.62-2.64 (2H, m), 3.81 (3H, s), 3.80-3.84 (2H, m), 3.89-3.91 (2H, m), 8.79 (2H, d). MS: m/z 251 (MH+)

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, 287714-35-6, Methyl 2-chloropyrimidine-5-carboxylate.

Reference:
Patent; ASTRAZENECA AB; US2008/153812; (2008); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of 130049-82-0, 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 130049-82-0 as follows.

To a methanol (500 mL) solution, nitrogen was purged for 30 minutes to remove the nascent oxygen. 6-Fluoro-3-piperidin-4-yl-benzo[d]isoxazole Hydrochloride (50 g), 9-Hydroxy-3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido (1,2-a) pyrimidine-4-one (52 g) and triethylamine (55) were added and stirred at reflux for 30-32 hours. The reaction mixture was cooled to 25-35 C, and filtered off to yield paliperidone base. Yield: 75 g.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,130049-82-0, its application will become more common.

Reference:
Patent; ORCHID CHEMICALS & PHARMACEUTICALS LIMITED; US2010/298566; (2010); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 89392-03-0, 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. 89392-03-0, name is Phenyl (4,6-dimethoxypyrimidin-2-yl)carbamate, molecular formula is C13H13N3O4, The 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.

5-Amino-2-dimethylaminocarbonyl-N-[(4,6-dimethoxypyrimidin-2-yl)-aminocarbonyl]benzenesulfonamide 0.6 ml of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) is added with stirring at 0 C. to a suspension of 1.0 g of 5-amino-2-dimethylaminocarbonylbenzene-sulfonamide and 1.1 g of 4,6-dimethoxy-2-(phenoxycarbonylamino)-pyrimidine in 10 ml of acetonitrile. The mixture is stirred again until complete reaction has taken place. Following the distillative removal of the volatile components, the residue is taken up in a little water and washed with diethyl ether. The aqueous phase is subsequently acidified with concentrated hydrochloric acid (pH=2-3). The deposited solid is washed with diisopropyl ether and then dried, to give 1.4 g of a solid which comprises the two compounds 5-amino-2-dimethylaminocarbonyl-N-[(4,6-dimethoxypyrimidin-2-yl)-aminocarbonyl]-benzenesulfonamide and 5-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonylamino]-2-dimethylaminocarbonyl-N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]benzenesulfonamide in a ratio of about 2:1.

According to the analysis of related databases, 89392-03-0, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Hoechst Schering AgrEvo GmbH; US6500952; (2002); B1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia