Tag: M.W=300-400

Reference of 916420-27-4, 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. 916420-27-4, name is tert-Butyl 2,4-dichloro-5,6-dihydropyrido[3,4-d]pyrimidine-7(8H)-carboxylate, molecular formula is C12H15Cl2N3O2, 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.

Benzyl 1-piperazinecarboxylate (1.268 mL, 6.575 mmol) and tert-Butyl 2,4-dichloro-5,6-dihydropyrido[3 4-d]pyrimidine-7(8H)-carboxylate (2 g, 6.575 mmol) were dissolved in dimethyl acetamide (10 mL) and treated with N-ethyl-N-isopropylpropan-2-amine (3.445 mL, 19.73 mmol). The reaction mixture was stirred at 85° C. for 2 hours. The reaction mixture was cooled to room temperature, diluted with ethyl acetate, washed with water and brine, dried over MgSO 4, filtered and concentrated. The concentrate was purified by chromatography (CombiFlash , 0%-50% ethyl acetate:Hexanes as the eluent to provide the product (2.69 g, 83%). ES+APCI MS m/z 488.2, 490.2 [M+H] +.

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 916420-27-4, tert-Butyl 2,4-dichloro-5,6-dihydropyrido[3,4-d]pyrimidine-7(8H)-carboxylate.

Reference:
Patent; Mirati Therapeutics, Inc.; Array BioPharma Inc.; Blake, James F.; Burgess, Laurence E.; Chicarelli, Mark Joseph; Christensen, James Gail; Cook, Adam; Fell, Jay Bradford; Fischer, John P.; Marx, Matthew Arnold; Mejia, Macedonio J.; Savechenkov, Pavel; Vigers, Guy P.A.; Smith, Christopher Ronald; Rodriguez, Martha E.; US2019/144444; (2019); A1;,
Pyrimidine | C4H4N2 – PubChem,
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Electric Literature of 131860-97-4, 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.131860-97-4, name is (E)-Methyl 2-(2-((6-chloropyrimidin-4-yl)oxy)phenyl)-3-methoxyacrylate, molecular formula is C15H13ClN2O4, molecular weight is 320.73, as common compound, the synthetic route is as follows.

Methyl (£)-2-{2-[6-chloropyiimidin-4-yloxy]phenyl}-3-methoxyacrylate (E) (3g of 95.4% strength) was charged to the reaction tube followed by the solvent (10 ml) then 2- cyanophenol (1.2g), base (1.5 mol equivalents) and the compound being tested as a catalyst (15 mol%). The reaction mixtures were held, with stirring, at 400C for 4hrs, then at 6O0C for 2 hrs. The reaction was monitored for formation of product, throughout the hold period, by Gas Chromatography. Results are recorded as area % levels of methyl (£)-2-{2-[6- chloropyrimidin-4-yloxy]phenyl}-3-methoxyacrylate (II) and methyl (E)-2-{2-[6-(2- cyanophenoxy)pyrimidin-4-yloxy]phenyl}-3-methoxyacrylate (I) in the reaction mixture.The following systems were tested:TABLE l The results are shown in Table 2 below:TABLE 2; Further screening experiments, using DMF as a solvent, were carried out as detailed below: Methyl (£)-2-{2-[6-chlororhoyrimidin-4-yloxy]ph.enyl}-3-methoxyacrylate (H) (6.4g of 45.2% strength solution in DMF) was charged to the reaction tube followed by further DMF (6.4 g), 2-cyanophenol (1.2g), potassium carbonate (1.5 mol equivalents) and the compound being tested as a catalyst (10 mol%). The reaction mixtures were held, with stirring, at 4O0C for 4hrs, then at 6O0C for 2 hrs. The reaction was monitored for loss of starting material and formation of product, throughout the hold periods, by Gas Chromatography. Results are recorded as area % levels of methyl (E)-2-{2-[6-chloropyrimidin-4-yloxy]phenyl}-3- methoxyacrylate (II) and methyl (2s)-2-{2-[6-(2-cyanophenoxy)pyrimidin-4-yloxy]phenyl}-3- methoxyacrylate (I) in the reaction mixture.The following systems were tested:TABLE 3The results are shown in Table 4 below:

The chemical industry reduces the impact on the environment during synthesis 131860-97-4, I believe this compound will play a more active role in future production and life.

Reference:
Patent; SYNGENTA LIMITED; WO2008/43977; (2008); A1;,
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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. 147118-37-4, name is N-(4-(4-Fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide, the common compound, a new synthetic route is introduced below. Application In Synthesis of N-(4-(4-Fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide

Example 6b Using NaHMDS N-(4-(4-fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (0.5 g, 1.4 mmol) and 2-((4 ,6S)-6-((benzo[d]thiazol-2-ylsulfonyl)methyl)-2,2-dimethyl- 1 ,3-dioxan-4-yl)acetate te/f-butyl ester (0.7 g, 1.6 mmol) were added to 10 mL of dry THF. After stirring for 10 min at 20C, the reaction mixture was cooled to -70C. At this temperature 1.9 mL of NaHMDS solution (1 M in THF, total 3.8 mmol) was added in 60 min keeping the temperature between -70 and -75C. When dosing was completed, the temperature of the reaction mixture was allowed to increase to -10C. After stirring at this temperature for 1 h, the reaction was quenched with 10% aqueous NaHC03 (5 mL). The phases were separated. The aqueous layer was extracted with 2 x 20 mL of ethyl acetate. The combined organic phases were washed with 5% aqueous Na2C03 and concentrated under vacuum. H PLC analysis indicated an E to Z ratio of >99: 1 . The residue was crystallized from methanol to give 2-((4f?,6S)-6-((E)-2-(4-(4-fluorophenyl)-6- isopropyl-2-(N-methylmethylsulfonamido) pyrimidin-5-yl)vinyl)-2,2-dimethyl-1 ,3-dioxan- 4-yl)acetate, te/f-butyl ester as a solid (0.52 g, 0.9 mmol, 64% yield).

The synthetic route of 147118-37-4 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.; DE LANGE, Ben; RIEBEL, Peter, Hans; WOLBERG, Michael; HEEMSKERK, Dennis; MINK, Daniel; WO2012/98048; (2012); A1;,
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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. 146533-41-7, name is 5-(4-Bromophenyl)-4,6-dichloropyrimidine, molecular formula is C10H5BrCl2N2, 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. Product Details of 146533-41-7

To a solution of 5-(4-bromophenyl)-4,6-dichloro-pyrimidine (100 g) in dimethyl sulfoxide (700 ml), potassium(N-propylsulfamoyl)amide (145 g) was added at 25-30C under nitrogen atmosphere and stirred for 10 hrs. After reaction completion, pH of the reaction mass was adjusted to 2-3 using aqueous hydrochloric acid at 25-30C and stirred for 75 mins. The solid obtained was filtered, washed with water and suck dried under vacuum. Methanol (3500 ml) was added to the above compound and heated to reflux temperature then stirred for an hour at reflux. The reaction mass was distilled upto 450-550 mL remained in the flask. The reaction mass was cooled to 25-30C, stirred for 75 mins then further cooled to 0- 5C and stirred for 75 mins. The obtained solid was filtered, washed with methanol and dried under vacuum at 50-55C for 4 hrs to get the title compound. Yield: 110 g; Purity by HPLC: 99.10%

With the rapid development of chemical substances, we look forward to future research findings about 146533-41-7.

Reference:
Patent; LAURUS LABS PRIVATE LIMITED; JAMJANAM, Srivardhana Rao; MOTURU, Venkata Ramakrishna Murthy; INDUKURI, Venkata Sunil Kumar; KALIDINDI, Srihari Raju; CHAVA, Satyanarayana; (37 pag.)WO2017/93903; (2017); A1;,
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Application of 131860-97-4, 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 131860-97-4, name is (E)-Methyl 2-(2-((6-chloropyrimidin-4-yl)oxy)phenyl)-3-methoxyacrylate. This compound has unique chemical properties. The synthetic route is as follows.

Further screening experiments, using DMF as a solvent, were carried out as detailed below: Methyl (£)-2-{2-[6-chlororhoyrimidin-4-yloxy]ph.enyl}-3-methoxyacrylate (H) (6.4g of 45.2% strength solution in DMF) was charged to the reaction tube followed by further DMF (6.4 g), 2-cyanophenol (1.2g), potassium carbonate (1.5 mol equivalents) and the compound being tested as a catalyst (10 mol%). The reaction mixtures were held, with stirring, at 4O0C for 4hrs, then at 6O0C for 2 hrs. The reaction was monitored for loss of starting material and formation of product, throughout the hold periods, by Gas Chromatography. Results are recorded as area % levels of methyl (E)-2-{2-[6-chloropyrimidin-4-yloxy]phenyl}-3- methoxyacrylate (II) and methyl (2s)-2-{2-[6-(2-cyanophenoxy)pyrimidin-4-yloxy]phenyl}-3- methoxyacrylate (I) in the reaction mixture.The following systems were tested:TABLE 3The results are shown in Table 4 below:

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; SYNGENTA LIMITED; WO2008/43977; (2008); A1;,
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Pyrimidine – Wikipedia

Adding a certain compound to certain chemical reactions, such as: 302964-08-5, 2-((6-Chloro-2-methylpyrimidin-4-yl)amino)-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide, 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, 302964-08-5, blongs to pyrimidines compound. Recommanded Product: 302964-08-5

Example 25; Procedure for the Preparation of Dasatinib Form T1E2-1 (Hemi-Ethanolate)A mixture of compound 1 (0.45 g, 1.14 mmol), N-(2-hydroxyethyl)piperazine (0.30 g, 2.30 mmol) and N-ethyldiisopropylamine (0.30 ml, 1.75 mmol) in DMSO (5 ml) was stirred at 60-65 C. for 2 hours. EtOH (30 ml) was slowly added at this temperature followed by H2O (40 ml). The solution was slowly cooled to 0-5 C. The product was filtered off and washed with ethanol (5 ml) and dried on the filter. Yield: 0.38 g.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,302964-08-5, its application will become more common.

Reference:
Patent; SIMO, Ondrej; Filipcik, Jiri; Martaus, Alexandr; Jegorov, Alexandr; Gavenda, Ales; Aronhime, Judith; Vraspir, Pavel; Koltai, Tamas; Faustmann, Jiri; Gabriel, Roman; US2009/118297; (2009); A1;,
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Application of 1197953-49-3, 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 1197953-49-3, name is (2-((2,5-Dichloropyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide. This compound has unique chemical properties. The synthetic route is as follows.

Add compound 13 to a 25 mL single-mouth bottle with magnetic stirrer and condenser(160 mg, 0.61 mmol), compound 7 (192 mg, 0.61 mmol)And ethylene glycol monomethyl ether (4mL), stir and dissolve,Add hydrogen chloride isopropanol solution (0.91 mmol, 0.18 mL, 5 M) dropwise.The temperature was raised to 120 C under a nitrogen atmosphere and stirred to react overnight. Cool to room temperature,Add water(10 mL) and saturated sodium bicarbonate (5 mL), dichloromethane (15 mL×3)The organic phase was combined, washed with saturated brine, dried over anhydrous sodiumConcentrated, the residue was passed through a silica gel column to give a white solid200 mg, the yield was 60.7%.

According to the analysis of related databases, 1197953-49-3, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Shenzhen Tajirui Bio-pharmaceutical Co., Ltd.; Wang Yihan; Li Huanyin; (49 pag.)CN109851638; (2019); A;,
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Synthetic Route of 186046-78-6, 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 186046-78-6, name is 2-(4-(((Benzhydryloxy)carbonyl)amino)-2-oxopyrimidin-1(2H)-yl)acetic acid. This compound has unique chemical properties. The synthetic route is as follows.

Example 21 N-[2-(Benzothiazole-2-sulfonylamino)-ethyl]-N-{[4-N-(benzhydryloxycarbonyl)-cytosin-1-yl]-acetyl}-glycine ethyl ester The title compound (2.99 g, 85%) was synthesised by the reaction of N-[2-(benzothiazole-2-sulfonylamino)-ethyl]-glycine ethyl ester (1.72 g, 5 mmol) and [4-N-(benzhydryloxycarbonyl)-cytosin-1-yl]-acetic acid (1.90 g, 5 mmol) as per the procedure of Example 20. 1H NMR (500 MHz; DMSO-d6) delta 11.00 (s, 1H), 8.86 (brs, 1H), 8.27 (d, 1H), 8.18 (d, 1H), 7.89 (d, 0.6H), 7.83 (d, 0.4H), 7.68~7.61 (m, 2H), 7.45~7.26 (m, 10H), 6.94 (t, 1H), 6.79 (s, 1H), 4.81 (s, 1.2H), 4.62 (s, 0.8H), 4.35 (s, 0.8H), 4.13 (q, 0.8H), 4.06 (s, 1.2H), 4.03 (q, 1.2H), 3.59 (t, 1.2H), 3.44~3.39 (m, 2H), 3.21 (t, 0.8H), 1.19 (t, 1.2H), 1.13 (t, 1.18H).

According to the analysis of related databases, 186046-78-6, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Kim, Sung Kee; Lee, Hyunil; Lim, Jong Chan; Choi, Hoon; Jeon, Jae Hoon; Ahn, Sang Youl; Lee, Sung Hee; Yoon, Won Jun; US2003/225252; (2003); A1;,
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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 131860-97-4, name is (E)-Methyl 2-(2-((6-chloropyrimidin-4-yl)oxy)phenyl)-3-methoxyacrylate. This compound has unique chemical properties. The synthetic route is as follows. SDS of cas: 131860-97-4

Methyl (£)-2-{2-[6-chloropyiimidin-4-yloxy]phenyl}-3-methoxyacrylate (E) (3g of 95.4% strength) was charged to the reaction tube followed by the solvent (10 ml) then 2- cyanophenol (1.2g), base (1.5 mol equivalents) and the compound being tested as a catalyst (15 mol%). The reaction mixtures were held, with stirring, at 400C for 4hrs, then at 6O0C for 2 hrs. The reaction was monitored for formation of product, throughout the hold period, by Gas Chromatography. Results are recorded as area % levels of methyl (£)-2-{2-[6- chloropyrimidin-4-yloxy]phenyl}-3-methoxyacrylate (II) and methyl (E)-2-{2-[6-(2- cyanophenoxy)pyrimidin-4-yloxy]phenyl}-3-methoxyacrylate (I) in the reaction mixture.The following systems were tested:TABLE l The results are shown in Table 2 below:TABLE 2

With the rapid development of chemical substances, we look forward to future research findings about 131860-97-4.

Reference:
Patent; SYNGENTA LIMITED; WO2008/43977; (2008); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reference of 146533-41-7, 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 146533-41-7, name is 5-(4-Bromophenyl)-4,6-dichloropyrimidine. This compound has unique chemical properties. The synthetic route is as follows.

A mixture of 1 (100 g, 0.33 mol), K2CO3 (221 g, 1.6 mol), and acetonitrile (1.3 L) washeated to 50C and stirred for 20 min. The solution of 2 (43 g, 0.31 mol) in acetonitrile(200 mL) was added dropwise and maintained at 50C for 10 h. The reaction solvent wasreplaced with toluene (2 L) using a Dean-Stark apparatus. The precipitated solid was filteredand suspended in water (2 L). The pH was adjusted to 7 by using 6 N hydrochloricacid and stirred for 20 min. The resulting precipitate was filtered and dried in the oven at55C for 5 h. The crude product was recrystallized from ethyl acetate to acquire 106 g(85%) of 3 as a white solid, mp 236C-238C. IR (KBr): 3272, 2966, 1593, 1566, 1438.1H NMR (500 MHz, DMSO-d6): d 0.73-0.76 (t, JD6.9, Me); 1.30-1.36 (m, CH2), 2.52-2.56 (m, CH2), 5.68-5.71 (t, JD6.6, NH), 7.12-7.14 (d, 2 H, ArH), 7.50-7.51 (d, 2 H,ArH), 8.04 (s, 1 H, ArH). 13C NMR (125 MHz, DMSO): d 12.41, 21.63, 45.75, 120.26,120.93, 131.50, 133.38, 136.21, 155.26, 156.73, 164.76.

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 146533-41-7, 5-(4-Bromophenyl)-4,6-dichloropyrimidine.

Reference:
Article; Nami, Majid; Sovari, Sara Nasiri; Haghighatnia, Yaghoub; Dabiri, Minoo; Salehi, Peyman; Organic Preparations and Procedures International; vol. 49; 3; (2017); p. 258 – 264;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia