Tag: M.W=100-200

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. 13484-56-5, name is 3-Chloro-6-methoxypyrazin-2-amine belongs to pyrazines compound, it is a common compound, a new synthetic route is introduced below. category: Pyrazines

Sodium hexamethyldisilazane (1M solution in THF; 0.76 ml) was added dropwise to amixture of 3-amino-2-chloro-5-methoxypyrazine (0.062 g), 4-chloro-7-(3-chloropropoxy)-3-cyano-6-methoxyquinoline (Bioorg. Med. Chem. Letters. 2000,10,2826; 0.096 g) and DMF(1.5 ml) that had been cooled to 0C. The mixture was stirred at 0C for 5 minutes and atambient temperature for 30 minutes. Acetic acid (0.023 ml) was added and the resultantmixture was evaporated. The residue was partitioned between methylene chloride and a10% aqueous sodium bicarbonate solution. The organic solution was dried over magnesiumsulphate and evaporated. The residue was triturated under diethyl ether and the resultant solidwas isolated. There was thus obtained the title compound as a solid (0.103 g); Mass Spectrum:M+lT434and436.

The synthetic route of 13484-56-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/108703; (2004); A1;,
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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. 5521-55-1, name is 5-Methylpyrazine-2-carboxylic acid belongs to pyrazines compound, it is a common compound, a new synthetic route is introduced below. SDS of cas: 5521-55-1

5-Methylpyrazin-2-carboxylic acid (13.81 g, 0.1 mol), tert-butanol (95 mL, 1 mol), triethylamine (27.9 mL, 0.2 mol) and diphenylphosphoryl azide (30.27 g, 0.11 mol) were mixed in 300 mL toluene, heated to reflux and reacted for 8 hours, and chromatographed on a silica gel column (petroleum ether – petroleum ether:ethyl acetate=20:1) to obtain a light yellow solid 15.2 g, at a yield of 72.7%.

The synthetic route of 5521-55-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; KBP Biosciences Co., Ltd.; ZHANG, Yan; ZHANG, Min; LO, HoYin; (52 pag.)EP2781508; (2014); A1;,
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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. 4774-14-5, name is 2,6-Dichloropyrazine, A new synthetic method of this compound is introduced below., Product Details of 4774-14-5

A solution of compound 8 4500 g, 302 mol) in conc. aq. NH3 (3.0 L) was stirred at135C overnight in a 10 L sealed pressure vessel. TLC and LC/MS showed completeconversion of the starting material. The reaction mixture was cooled to roomtemperature and filtered to afford a white solid. The solid was washed with water (200mL x 3), and then dried to afford compound 9 (312 g, 80% yield) as a solid.1HNMR (400 MHz, DMSO-d6): 7,82 (s, 1 H), 712 (s, 1 H), 6.93 (s, 2H). MS Calcd.:129 MS Found: 130 ([M+Hj).

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.

Reference:
Patent; H. LUNDBECK A/S; SVENSTRUP, Niels; WEN, Kate; WANG, Yazhou; (78 pag.)WO2017/5786; (2017); A1;,
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Related Products of 33332-29-5, 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. 33332-29-5, name is 2-Amino-5-chloropyrazine, This compound has unique chemical properties. The synthetic route is as follows.

General procedure: Method B is a modification of Method A and was performed under nitrogen atmosphere andwith extended work-up. Substituted benzoyl chloride (1.5 mmol, 1.2 equiv) was placed into the askunder nitrogen, diluted with dry DCM (5 mL) and dry pyridine (400 mg, 5 mmol, 4 equiv) was added.The mixture was mixed for 5 min under nitrogen. Then, 5-chloropyrazin-2-amine (162 mg, 1.25 mmol,1 equiv) dissolved in DCM (10 mL) was added dropwise over 10 min under nitrogen ow. The askwas closed by septum and stirred for additional 6 h. After reaction, the mixture was diluted with DCMto the final volume of 40 mL and washed with water (1 30 mL), 5% (m/m) aqueous NaHCO3 solution(1 30 mL), and brine (1 30 mL). The organic layer was dried over anhydrous Na2SO4 and adsorbedon silica (4 g) by evaporating the solvents under reduced pressure. Automated flash chromatographywas run using same conditions as described in Method A. If needed, the products were recrystallizedfrom hot EtOH (crystallization initiated by cooling and dropwise addition of cold water).

The chemical industry reduces the impact on the environment during synthesis 2-Amino-5-chloropyrazine. I believe this compound will play a more active role in future production and life.

Reference:
Article; Zitko, Jan; Mindlova, Al?b?ta; Vala?ek, Ond?ej; Jand’ourek, Ond?ej; Paterova, Pavla; Janou?ek, Ji?i; Kone?na, Klara; Dole?al, Martin; Molecules; vol. 23; 9; (2018);,
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Application of 33332-29-5, The chemical industry reduces the impact on the environment during synthesis 33332-29-5, name is 2-Amino-5-chloropyrazine, I believe this compound will play a more active role in future production and life.

To a solution of 5-chloropyrazin-2-amine (500 mg, 3.86 mmol) in DCM (5mL) was added NBS (686.92 mg, 3.86 mmol), and the brown mixture was stirred at 40 C for 1 hour. After cooling to r.t., the mixture was filtered through silica gel and eluted with EtOAc (20 mL x 3), and the filtrate was concentrated to give the crude product. The crude product was purified by flash chromatography on silica gel (EtOAc in PE = 20% to 40% to 50%) to give the product (600 mg) as a solid. *H NMR (400MHz, CDC13 ) _ = 7.98 (s, 1H), 5.05 (br s, 2H).

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, 2-Amino-5-chloropyrazine, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; PRAXIS PRECISION MEDICINES, INC.; REDDY, Kiran; MARTINEZ BOTELLA, Gabriel; GRIFFIN, Andrew, Mark; MARRON, Brian, Edward; (364 pag.)WO2018/98499; (2018); A1;,
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Synthetic Route of 56423-63-3, 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. 56423-63-3, name is 2-Bromopyrazine belongs to pyrazines compound, it is a common compound, a new synthetic route is introduced below.

EXAMPLE 92(f) Synthesis of 2-(1H-Imidazol-4-yl)-pyrazine To a solution of 4-Iodo-1-trityl-1H-imidazole (1 eq) in THF at room temperature was added ethylmagnesium bromide (1.2 eq) under dry conditions. After stirring for 90 minutes, zinc chloride (1.2 eq) was added to the reaction mixture. After stirring for another 90 minutes, tetrakis(triphenylphosphine) palladium (10%) and 5-bromopyrazine (1.3 eq) were added to the reaction mixture. Subsequent reaction conditions and work up are as described previously in Example 73, the resulting solid 2-(1H-Imidazol-4-yl)-pyrazine (37%) was collected by filtration. MH+(147)

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, 2-Bromopyrazine, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Chu, Daniel; Burger, Matthew; Lin, Xiaodong; Carroll, Georgia Law; Plattner, Jacob; Rico, Alice; US2003/125266; (2003); A1;,
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Related Products of 27398-39-6, 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. 27398-39-6, name is 3-Chloropyrazine-2-carboxylic acid belongs to pyrazines compound, it is a common compound, a new synthetic route is introduced below.

3-Chloropyrazine-2-carboxylic acid (2.97 g, 18.73 mmol, 1 eq.) was dissolved in tetrahydrofuran (75 mL). The solution was stirred in an ice bath and triethylamine (5.2 mL, 37.5 mmol, 2 eq.) was added followed by addition of methyl chloroformate (1.74 mL, 22.5 mmol, 1.2 eq.) dropwise. After 30 m, the reaction was filtered and the solid rinsed with more tetrahydrofuran (10 mL). The tetrahydyofuran solution was stirred in an ice bath and a suspension of sodium borohydride (1.4 g, 37.5 mmol, 2 eq.) in water (3 mL) was added. After 1 h, a saturated aqueous ammonium chloride solution (100 mL) was added to the reaction and the mixture was extracted with ethyl acetate (2 x 100 mL). The combined organic phases were washed with a saturated aqueous sodium chloride solution (25 mL) and dried over sodium sulfate. After filtration and evaporation, the residue was purified by silica gel chromatography (5 – 70percent ethyl acetate/hexanes) to give (3-chloropyrazin-2-yl)methanol (0.84 g, 31percent) as a faintly colored oil.

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, 3-Chloropyrazine-2-carboxylic acid, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; GLOBAL BLOOD THERAPEUTICS, INC.; LI, Zhe; HARRIS, Jason, R.; DUFU, Kobina, N.; GENG, Xin; SINHA, Uma; (101 pag.)WO2016/160755; (2016); A1;,
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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. 4858-85-9, name is 2,3-Dichloropyrazine belongs to pyrazines compound, it is a common compound, a new synthetic route is introduced below. Recommanded Product: 4858-85-9

59.6 g (0.40 mol) of 2,3-dichloropyrazine, 37.3 g (0.40 mol) of aniline, and 42.4 g (0.40 mol) of sodium carbonate are suspended in 250 ml of 1-methyl-pyrrolidone and heated at 151C during 24 hours. The black suspension is cooled down to 100C, filtered, and the solid residue further washed with ethyl acetate. The filtrate is concentrated under vacuum and the residual oil further purified by distillation (125-128C, 0.3 mbar) giving the title productas light yellow solid (yield: 58.3 g (71%)).1HNMR (300 MHz, CDCI3): = 7.05-7.22 (m, 2 H), 7.32-7.45 (m, 2 H), 7.57-7.68 (m, 2 H),7.75 (d, I H), 8.05 (d, H).

The synthetic route of 4858-85-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BASF SE; MURER, Peter; BATTAGLIARIN, Glauco; DORMANN, Korinna; METZ, Stefan; WAGENBLAST, Gerhard; BENEDITO, Flavio Luiz; WATANABE, Soichi; LENNARTZ, Christian; GESSNER, Thomas; WO2015/14835; (2015); A1;,
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These common heterocyclic compound, 33332-29-5, name is 2-Amino-5-chloropyrazine, 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. Application In Synthesis of 2-Amino-5-chloropyrazine

General procedure: Sodium nitrite (3.4 g, 50 mmol, 1.3 eq.) was added in small portionsto 98% sulfuric acid (15 mL) ice bath, and the mixture was allowed towarm up and heated to 60. When getting clear, the solution wascooled in an ice bath again. A solution of 2-amino-pyrazine (9) (4 g,39.3 mmol, 1 eq.) in 98% sulfuric acid (15 mL) was added dropwise.The reaction mixture was stirred at 40 for 1 h. After cooling to roomtemperature, it was slowly poured onto crushed ice and stirred until nonitrogen run out. The solution was adjusted to pH 6 with a 40% solutionof sodium hydroxide, resulting in lots of sodium sulfate which wasfiltered off whereafter. The filtrate was extracted with EA (50 mL×3),and the combined organics were dried (Na2SO4), filtered and concentratedin vacuo to give the product as a white precipitate (6.38 g,53%).

The synthetic route of 2-Amino-5-chloropyrazine has been constantly updated, and we look forward to future research findings.

Reference:
Article; Guo, Shuang; Xu, Mingshuo; Guo, Qi; Zhu, Fuqiang; Jiang, Xiangrui; Xie, Yuanchao; Shen, Jingshan; Bioorganic and Medicinal Chemistry; vol. 27; 5; (2019); p. 748 – 759;,
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Application of 4858-85-9, A common heterocyclic compound, 4858-85-9, name is 2,3-Dichloropyrazine, molecular formula is C4H2Cl2N2, 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.

A 12L 3 -neck round bottom flask fitted with a magnetic stirrer under nitrogen was charged with zinc dust (745 g, preactivated according to the above Preparation 1 , 11.4 mol, 2 eq.) and DMA (2 L, anhydrous). 1, 2-dibromoethane (71 mL, 0.855 mol, 0.15 eq, Aldrich) was then added over 10 min, followed by TMSC1 (108 mL, 0.855 mol, 0.15 eq, Acros) over 20 min. The reaction mixture was stirred for 25 min at RT. A solution of N-Boc-3-iodoazetidine (2) (2420 g, 8.55 mol, 1.5 eq, CNH Technologies) in DMA (5 L, anhydrous) was added via a 2L addition funnel over 2 h keeping the internal temperature below 65 C using a water bath. The suspension was stirred for 1 h at RT at which point it was degassed with nitrogen. Stirring was stopped and the suspension was allowed to stand. A 22L 3 -neck round bottom flask fitted with a mechanical stirrer was charged with 2, 3-dichloropyrazine (6) (850 g, 5.70 mol, 1.0 eq, AK Scientific), PdCl2dppf-CH2Cl2 (140 g, 171 mmol, 0.03 eq, Aldrich), Cul (67.3 g, 353 mmol, 0.062 eq, Aldrich), and DMA (5 L, anhydrous). The solution was degassed with nitrogen. The clear zinc reagent solution above the residual solid zinc was poured into the 22L flask under nitrogen. The brown solution was degassed with nitrogen and heated to 80 C for 16 h at which point LCMS indicated complete conversion of 2, 3-dichloropyrazine (6). The reaction mixture was transferred to brine (8 L) in 50L separatory funnel. Water (8 L) and EtOAc (15 L) were added and the layers were separated. The aqueous layer was extracted with EtOAc (2 x 10 L). The combined organics were washed with water (3 x 10 L) and brine (5 L), dried over sodium sulfate and evaporated. The resulting residue was purified by column chromatography (eluting with hexanes/ethyl acetate = 10: 1) to obtain 536 g of pure tert-butyl 3-(3-chloropyrazin-2- yl)azetidine-l-carboxylate (7) and 121 g of mixed fractions. The impure material was distilled under high vacuum to remove the impurity (N-Boc-azetidine) to give 81 g of pure tert-butyl 3-(3- chloropyrazin-2-yl)azetidine- 1 -carboxylate (7).Total: 617g, Yield: 40%.

The synthetic route of 4858-85-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; AMGEN INC.; ALLEN, Jennifer R.; CHEN, Jian J.; FROHN, Michael J.; HU, Essa; LIU, Qingyian; PICKRELL, Alexander J.; RUMFELT, Shannon; RZASA, Robert M.; ZHONG, Wenge; WO2011/143365; (2011); A1;,
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