Day: March 16, 2022

Application of 640769-71-7, 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. 640769-71-7, name is 2-(Pyrimidin-5-yl)benzaldehyde, molecular formula is C11H8N2O, 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.

Tetrabutylammonium fluoride (TBAF, 0.1 ml of 1M in THF) was added to a solution of 2-pyrimidin-5-yl-benzaldehyde (184 mg, 1 mmol) and trifluoromethyl trimethylsilane (TMSCF3, 0.2 ml, 1.2 mmol) in 10 ml THF at 0 C. The mixture was warmed up to room temperature and stirred for 4 hours. The mixture was then treated with 3 ml of 1 M HCl and stirred overnight. The product was extracted with ethyl acetate (3*20 ml). The organic layer was separated and dried over sodium sulfate. The organic solvent was evaporated to give 0.21 g of 2,2,2-trifluoro-1-(2-pyrimidin-5-yl-phenyl)-ethanol (yield: 84%), which was directly used in next step without purification.

According to the analysis of related databases, 640769-71-7, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Liu, Qingyun; Zambrowicz, Brian; US2009/29993; (2009); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reference of 87253-62-1, 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.87253-62-1, name is 5,7-Dimethyl-[1,2,4]triazolo[1,5-a]pyrimidine-2-carboxylic acid, molecular formula is C8H8N4O2, molecular weight is 192.18, as common compound, the synthetic route is as follows.

General procedure: In 25ml RB flask to a solution of Compound 9 (200 mg) in dry DMF (5ml), EDCI (250 mg, 1.25eq) and DMAP (130 mg,1eq) were added followed by addition of Sulfonamide (1eq). RM was stirred at RT for 4hrs. Solvent from the reaction mixture was evaporated. To the residue water was added and acidified with 6N HCl, solid precipitated out. Solid was filtered and dried. Crude solid was purified by flash chromatography eluating with 4-8% MeOH/DCM as solvent system to give pure product.

Statistics shows that 87253-62-1 is playing an increasingly important role. we look forward to future research findings about 5,7-Dimethyl-[1,2,4]triazolo[1,5-a]pyrimidine-2-carboxylic acid.

Reference:
Article; Patil, Vikas; Kale, Manoj; Raichurkar, Anandkumar; Bhaskar, Brahatheeswaran; Prahlad, Dwarakanath; Balganesh, Meenakshi; Nandan, Santosh; Shahul Hameed; Bioorganic and Medicinal Chemistry Letters; vol. 24; 9; (2014); p. 2222 – 2225;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of 103365-69-1, The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 103365-69-1, name is (S)-1-Methyl-2,6-dioxohexahydropyrimidine-4-carboxylic acid. This compound has unique chemical properties. The synthetic route is as follows.

The taltirelrin was synthesized by using a core-cell (CS) skillsthat can provide amine function in C-terminal and using CS-Rink Amide MBHA. here using a quantitative method it was measured and 0.8 mmol / g loaded resin was used. The synthesis proceeded on 0.1M scale. Synthesis was performed using the fully automated peptidesynthesizer manufactured by SONATA XT a PTI Company. The removal of Fmoc protector of resin. Fmoc protected core-shell (CS) type Rink Amide MBHA Resin(100mmol, 125g, 0.8 mmol / g, beadTechpvt. ltd.) is inserted in a fully automatic peptide synthesizer SONATA XT 3.2L reaction vessel and thendimethylformamide (DMF ) was added and then inserted into the filtered reactorand and was dilated for 30 minutes.after filtration and removal of DMF, then 20% piperidine (in DMF) was put infiltration reactor and then reacted for 10 minutes and filtered, and again 20%piperidine (in DMF) is put and for reacted for 5 minutes and filtered and Fmocremoved rink Amide MBHA resin was prepared. Filtered and the filtrate discarded and the resin remaining inreactor was washed in the following procedure and then filtered: DMF x 2 times(each 5 min), Dichloromethane x 2 times (each 5 min), DMF x 2 times (each 5min) Fmoc-Pro-OH coupling After the Fmoc-Pro-OH 3equivalents was dissolved in DMF, then matching the amino acid equivalent DIC(N, N’-Diisopropylcarbodiimide) and HOBt Cl- (1-Hydroxy-6-Chlorobenzotriazole)is inserted and for about 5 minutes it is activated and inserted in a Fmocprotector removed CS-Rink Amide MBHA resin inserted filteration reactor andthen reacted for 3 hours. After the reaction was completed the reaction solution wasfiltered and the remaining Fmoc-Pro-CS-Rink Amide MBHA resin in the filtrationreactor was washed in the following order: DMF x 2 times (each 5 min),dichloromethane x 2 times ( each 5 min), DMF x 2 times (each 5 min).The reaction termination was confirmed by the color reaction(Kaiser Test). Removal of the Fmoc protector of Fmoc-Pro-CS-Rink Amide Resin In a washed Fmoc-Pro-Rink Amide MBHA resin inserted reactor 20%piperidine (in DMF) is inserted and reacted for 20 minutes and filtered, andagain 20% piperidine (in DMF) is put and for10 minutes It was reacted and then filtered to prepare Fmoc removed H-Pro-CS-Rink Amide MBHA resin. After filtration H-Pro-CS-Rink Amide MBHA resin remaining in thereactor is then washed in following order and then filtered: DMF x 2 times(each 5 min), Dichloromethane x 2 times (each 5 min), DMF x 2 times (each 5min) Fmoc-His (Trt) -OH coupling Fmoc-His (Trt) -OH 3 equivalent after dissolved in DMF, inquantity equivalent of the amino acid DIC and HOBt-Cl is put in and for about 5minutes it is actively refluxed and, then placed in a H-Pro-Rink Amide resininserted filtration reactor and reaction was carried out for 3 hours. After the reaction was completed the reaction solution wasfiltered and the remaining Fmoc-Pro-CS-Rink Amide MBHA resin in the filtrationreactor was washed in the following order: DMF x 2 times (each 5 min),dichloromethane x 2 times ( each 5 min), DMF x 2 times (each 5 min). The reaction termination was confirmed by the color reaction(Kaiser Test). Separation of the peptides from the resin In a Well-dried 1-methyl-4,5-dihydro-orotic acid -His (Trt)-Pro-CS-Rink Amide Resin inserted filtration reactor 10 times volume of resincutting solution (95% TFA, 2.5% TIS,2.5% H2O) is carefully added and reaction was carried out for 3 hours. After completion ethanol10 times the volume of the reaction filtrate is poured and the peptide isextracted. The peptide extracted to remove ethanol is precipitated using acentrifugal separator, and then using two more times ethanol and from the TFAresidue amino acid side chain protectoron removing of residue matter it is dried to yield 36.5g title compound (90%).

According to the analysis of related databases, 103365-69-1, the application of this compound in the production field has become more and more popular.

Reference:
Patent; C-TRI Co. Ltd.; Kim, Seok In; Kim, Do Yeong; Im, Chae Yeong; Jeong, Ki Hoon; Kim, Joo Seong; Ju, So Kyeong; Kim, Wan Ju; (12 pag.)KR101574252; (2015); B1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 60025-06-1, Adding some certain compound to certain chemical reactions, such as: 60025-06-1, name is 1-(4,6-Dichloropyrimidin-5-yl)ethanone,molecular formula is C6H4Cl2N2O, 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 60025-06-1.

Intermediate 21: 4-(4-Chloro-3-methyl-pyrazolo[3,4-d]pyrimidin-1-yl)-piperidine-1-carboxylic acid isopropyl ester; Triethylamine (0.33 mL, 2.4 mmol) was added to a stirred mixture of 4-hydrazino-piperidine-1-carboxylic acid isopropyl ester hydrochloride (Intermediate 10; 188 mg, 0.8 mmol) and 1-(4,6-dichloro-pyrimidin-5-yl)-ethanone (Intermediate 17; 150 mg, 0.8 mmol) in toluene (5 mL) at room temperature under nitrogen and the resulting mixture was heated to reflux for 8 hours. The solvent was removed in vacuo and the crude reaction mixture was purified on a flash silica column (30 mm×4) eluting with 10-33% ethyl acetate/hexanes to give 4-(4-chloro-3-methyl-pyrazolo[3,4-d]pyrimidin-1-yl)-piperidine-1-carboxylic acid isopropyl ester (90 mg, 33%). 1H NMR (300 MHz, DMSO-d6) delta 1.19 (d, 6H, J=6.3 Hz), 1.86-1.99 (m, 4H), 2.63 (s, 3H), 2.94-3.10 (m, 2H), 4.04-4.15 (m, 1H), 4.74-4.82 (m, 1H), 4.91-4.98 (m, 1H), 8.77 (s, 1H).

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. 60025-06-1, 1-(4,6-Dichloropyrimidin-5-yl)ethanone, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Erickson, Shawn David; Gillespie, Paul; Guertin, Kevin Richard; Karnachi, Prabha Saba; Kim, Kyungjin; Ma, Chun; McComas, Warren William; Pietranico-Cole, Sherrie Lynn; Qi, Lida; Tilley, Jefferson Wright; Zhang, Qiang; US2009/286812; (2009); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adding a certain compound to certain chemical reactions, such as: 87026-45-7, 4-Chloro-5-methoxy-2-(methylthio)pyrimidine, 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, 87026-45-7, blongs to pyrimidines compound. Safety of 4-Chloro-5-methoxy-2-(methylthio)pyrimidine

4-Chloro-2-methanesulfonyl-5-methoxy-pyrimidine A solution of 3-chloroperoxybenzoic acid (0.4 g, 2.3 mmol) in DCM (2 ml) was added dropwise to a solution of 4-chloro-5-methoxy-2-methylsulfanyl-pyrimidine (0.15 g, 0.78 mmol) in DCM (10 ml) and the mixture was stirred at room temperature for 12 h. Water (10 ml) was added, the aqueous phase was extracted with DCM and concentrated in vacuo. The crude residue was purified by column chromatography with DCM/1% NH3 in MeOH (98:2) as the eluent to give the title compound (0.18 g, 100%).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,87026-45-7, its application will become more common.

Reference:
Patent; VIFOR (INTERNATIONAL) AG; US2012/202806; (2012); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of 55150-17-9 ,Some common heterocyclic compound, 55150-17-9, molecular formula is C6H9N3O, 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.

(2) 2,2,2-Trichloroethyl (4-ethoxyprimidin-5-yl)carbamate; To a solution of 4-ethoxypyrimidine-5-amine (1.00 g, 7.19 mmol) and pyridine (1.74 ml, 21.6 mmol) in tetrahydrofuran (20 ml) was added 2,2,2-trichloroethyl chloroformate (1.49 ml, 10.8 mmol) with ice-cooling, the mixture was stirred for 30 minutes with ice-cooling, the reaction mixture was poured into ice-water and the mixture was extracted with ethyl acetate. The extract was washed with water and dried over anhydrous magnesium sulfate and the solvent was distilled off under reduced pressure. The residue was recrystallized from a mixed solvent of ethyl acetate and hexane to obtain the desired product (1.73 g, 76.5%) as a solid. 1H-NMR (CDCl3) delta; 1.48 (3H, t, J = 7.2 Hz), 4.55 (2H, q, J = 7.2 Hz), 4.87 (2H, s), 7.15(1H, br s), 8.51 (1H, s), 9.20 (1H, br s).

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. 55150-17-9, 4-Ethoxypyrimidin-5-amine, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Takeda Pharmaceutical Company Limited; EP1813606; (2007); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 313339-35-4, 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. 313339-35-4, name is 4,6-Dichloro-2-(methylthio)pyrimidine-5-carboxylic acid, molecular formula is C6H4Cl2N2O2S, 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.

Method same In Example 1, 0.49 g (2.03 mmol) of 4,6-dichloro-2-(methylsulfanyl)pyrimidine-5-carboxylic acid was dissolved in 20 mL of methylene chloride solvent, 0.52 g (4.06 mmol) of oxalyl chloride was added, DMF, stirred for 5 h at room temperature and the solvent and excess oxalyl chloride removed in vacuo to give a yellow solid; this was dissolved in 20 mL of dichloromethane and then 0.37 g (2.03 mmol) of 5-[(methylamino)methyl]-1H-imidazole-4-ethylformate,0.35g (3.45mmol) of triethylamine, stirred at room temperature After the reaction was completed, it was poured into 30mL of saturated sodium bicarbonate solution, extracted with dichloromethane (20mLX2), combined organic phase, dried over anhydrous sodium sulfate, filtered After the solvent was distilled off under reduced pressure, 5-((4,6-dichloro-N-methyl-2-(methylsulfanyl)pyrimidine-5-carboxamido)methyl)-1H-imidazole-4-ethylformate was obtained, used directly in the next reaction.5-((4,6-dichloro-N-methyl-2-(methylsulfanyl)pyrimidine-5-carboxamido)methyl)-1H-imidazole-4-ethylformate was dissolved in 20 mL of acetonitrile , 0.98g (7. 10mmol) of anhydrous potassium carbonate was added and the mixture was stirred at room temperature until the reaction was completed. The solvent was distilled off under reduced pressure.This was dissolved in 20 mL of methylene chloride, washed with 30 mL of saturated brine and dried over anhydrous sodium sulfate. After filtration, the solvent was evaporated under reduced pressure and the residue was purified by column chromatography (CH2C12: CH3COCH3 = 60: 1) to give a white solid The yield is 27%.0.35g (1.71mmol) of 4-chloro-2-(methylsulfanyl)pyrimidine-5-carboxylic acid was dissolved in 20mL dichloromethane solvent, 0.37g (2.94mm0l) oxalyl chloride was added, 1 drop DMF, stirred at room temperature for 6h and then under reduced pressure Evaporation of solvent and excess oxalyl chloride gave a yellow solid;This was dissolved in 20 mL of dichloromethane and then 0.22 g (1.21 mmol) of 5-[(methylamino)methyl]-1H-imidazole-4-ethylformate and 0.21 g (2.05 mmol) of triethylamine were added and stirred at room temperature After the reaction, it was poured into 30 mL of saturated sodium bicarbonate solution and extracted with dichloromethane (20 mL × 2). The combined organic phase was dried over anhydrous sodium sulfate and filtered. The solvent was evaporated under reduced pressure to give 5-((4-chloro-N-methyl-2-(methylsulfanyl)pyrimidine-5-carboxamido)methyl)-1H-imidazole-4-ethylformate was used directly in the next reaction.A solution of ethyl 5-((4-chloro-N-methyl-2-(methylsulfanyl)pyrimidine-5-carboxamido)methyl)-1H-imidazole-4-ethylformate in 20 mL of acetonitrile was added 0.58 g 4.22 mmol) anhydrous potassium carbonate and stirred at room temperature until the reaction was completed. The solvent was distilled off under reduced pressure.The residue was dissolved in 20 mL of methylene chloride, washed with 30 mL of saturated brine and dried over anhydrous sodium sulfate. After filtration, the solvent was distilled off under reduced pressure and the residue was purified by column chromatography (CH2C12: CH3COCH3 = 10: 1) to give a white solid The yield is 60%.

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 313339-35-4, 4,6-Dichloro-2-(methylthio)pyrimidine-5-carboxylic acid.

Reference:
Patent; Beijing Normal University; The Chinese People’s Liberation Army Military Academy Of Medical Sciences Poison Pharmaceutical Institute; Zhang Zhanbin; Yu Gang; Li Yi; Xiao Guiying; Cao Yanqing; Su Ruibin; Zheng Zhibing; Zhou Xinbo; (12 pag.)CN107312012; (2017); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of 19808-30-1, 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.19808-30-1, name is 5-Bromopyrimidin-4(3H)-one, molecular formula is C4H3BrN2O, molecular weight is 174.9834, as common compound, the synthetic route is as follows.

Reference Example 3 5-Bromopyrimidin-4(3H)-one (578 mg) was dissolved in N,N-dimethylformamide (15 mL), and potassium carbonate (685 mg) and methyl iodide (247 muL) were added, followed by stirring at room temperature for 24 hours. Water was added to the reaction mixture, followed by extraction with chloroform. The organic layer was washed with saturated brine and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure, and the resulting residue was purified by silica gel column chromatography (hexane:ethyl acetate = 1:1) to obtain 5-bromo-3-methylpyrimidin-4(3H)-one (337 mg) as a white solid.

The chemical industry reduces the impact on the environment during synthesis 19808-30-1, I believe this compound will play a more active role in future production and life.

Reference:
Patent; Astellas Pharma Inc.; EP1947086; (2008); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthetic Route of 216309-28-3 ,Some common heterocyclic compound, 216309-28-3, molecular formula is C9H12N2Si, 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.

b) 5-Ethynyl-pyrimidine; Potassium carbonate (7.38 g, 53.4 mmol) was added in one portion to a stirred solution of 5-trimethylsilanylethynyl-pyrimidine (4.71 g, 26.7 mmol) in methanol (10 ml). The reaction mixture was stirred for 2 hours at room temperature then concentrated in vacuo. The residue was suspended in dichloromethane and the inorganic solids were removed by filtration. The filtrate was concentrated in vacuo to remove ca. 95% of the solvent to afford 5-ethynyl-pyrimidine as a brown oil in crude form. This material was used in the subsequent Sonogashira reaction without further purification.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,216309-28-3, its application will become more common.

Reference:
Patent; Hebeisen, Paul; Roever, Stephan; US2008/70931; (2008); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 122567-97-9, name is ((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate. This compound has unique chemical properties. The synthetic route is as follows. Recommanded Product: ((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate

5-methyl thymine 20-2 as a raw material, the reaction steps are as follows:(3) Synthesis of compound 21-3 (d4T):Compound 21-2 (0.288 g, 0.88 mmol) was added to the reactor,Saturated methanolic methanol solution 30mL, stirring at room temperature reaction,TLC tracks the reaction to the end. The solvent was removed by concentration,Column chromatography (MeOH: CHCl3 = 5: 100)To give the target product 21-3 (yield 75%).

With the rapid development of chemical substances, we look forward to future research findings about 122567-97-9.

Reference:
Patent; Soochow University (Suzhou); Zou Jianping; Zhang Peizhi; Li Jianan; (13 pag.)CN106496130; (2017); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia