Category: 4430-75-5

Application of 4430-75-5,Some common heterocyclic compound, 4430-75-5, name is Octahydro-2H-pyrido[1,2-a]pyrazine, molecular formula is C8H16N2, 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.

To 3-({[4-(trifluoromethyl)phenyl]amino}sulfonyl)benzoic acid (4.35 g, 12.6 mmol) and 2-(3H-[l,2,3]triazolo[4,5-delta]pyridin-3-yl)-l,l,3,3-tetramethylisouronium hexafluorophosphate(V) (5.27g, 13.9 mmol) in JV,iV-dimethylacetamide (30 mL) and 2- methyltetrahydrofuran (90 mL) was added l,4-diazabicyclo[4.4.0]decane (2.47 g, 17.6 mmol). The reaction was stirred at ambient temperature for 2.5 hours, and then it was diluted with 2-methyltetrahydrofuran (57 mL). The organic solution was washed with 6% NaHCOs/6% NaCl (35 niL), and the aqueous layer was extracted with 2- methyltetrahydrofuran (50 mL). The organic layer was washed with 6% NaHCOs/6% NaCl (50 mL) and 1 : 1 saturated NaCl/water (6chi50 mL), and then it was concentrated. The residue was concentrated from ethanol (2×50 mL) to give the title compound

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route Octahydro-2H-pyrido[1,2-a]pyrazine, its application will become more common.

Reference:
Patent; ABBOTT LABORATORIES; ZHANG, Qingwei; STEWART, Andrew, O.; XIA, Zhiren; WO2010/83264; (2010); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Reference of 4430-75-5,Some common heterocyclic compound, 4430-75-5, name is Octahydro-2H-pyrido[1,2-a]pyrazine, molecular formula is C8H16N2, 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.

Step 12a:; A solution of acid 49 (50 mg, 0.125 mmol) in CH2C12 (2 mL) was treated with oxalyl chloride (100 muL, 1.16 mmol). After 20 min, the reaction mixture was concentrated in vacuo, diluted with CH2CI2 (1 mL) and treated with Et3N (130 muL, 1.20 mmol) followed by (+/-)-1,4-diazabicyclo[4.4.0]decane (140 mg, 1.0 mmol). After 18 h, the reaction mixture was diluted with saturated aqueous NH4CI and extracted with CH2CI2 (2x). The combined organic layers were washed with saturated aqueous NaHC03, dried over MgS04 and concentrated in vacuo. Preparative TLC (0.5:4.5:95 NH40H/MeOH/CH2CI2), afforded Example 40 (42.0 mg, 65%) as a yellow oil. Example 40: LCMS (ES): time 3.45 min, m/z 520.3 (M+H+).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route Octahydro-2H-pyrido[1,2-a]pyrazine, its application will become more common.

Reference:
Patent; SCHERING CORPORATION; WO2005/97768; (2005); A2;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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. 4430-75-5, name is Octahydro-2H-pyrido[1,2-a]pyrazine belongs to pyrazines compound, it is a common compound, a new synthetic route is introduced below. SDS of cas: 4430-75-5

1-fluoro-2-nitrobenzene (1.2 g, 8.56 mmol),Octahydro-1H-pyrido[1,2-a]pyrazine (1.0 g, 7.13 mmol), N,N-diisopropylethylamine (1.9 mL, 10.7 mmol) was added to N,N-dimethyl In formamide (20 mL),The reaction was heated to 90 C under nitrogen for 4 hours.After completion of the reaction, the mixture was cooled to room temperature, and the reaction mixture was diluted with water (80 mL)The organic phases were combined and washed successively with water (50 mL) and brine (50 mL).Dry over anhydrous sodium sulfate, and distill off the solvent under reduced pressure.The resulting crude product was purified by silica gel column chromatography (petroleum ether: ethyl acetate (V: V) = 5: 1) to give further title compound (yellow oil, 1.74g, 93.4%).

The synthetic route of 4430-75-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Jin Chuanfei; Du Changfeng; Zhang Yingjun; (29 pag.)CN108409729; (2018); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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. 4430-75-5, name is Octahydro-2H-pyrido[1,2-a]pyrazine belongs to pyrazines compound, it is a common compound, a new synthetic route is introduced below. category: Pyrazines

To a solution of octahydropyrido[1,2-a]pyrazine (50 mg, 0.38 mmol) and NEt3 (83 muL, 0.59 mmol) in DCM (15 mL) at 0 C. was added a suspension of 2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-1,3a-diazabenzo[e]azulene-9-sulfonyl chloride from Example 121 (93 mg, 0.12 mmol) in DCM (5 mL) and the resulting mixture warmed to RT after 10 min then stirred for 1 h. The reaction mixture was diluted with DCM, washed with a saturated aqueous NaHCO3 solution then dried (Na2SO4) and concentrated in vacuo. The resulting residue was purified by column chromatography (Si-PCC, gradient 0-8% MeOH in EtOAc) then freeze-dried from MeCN/H2O affording 132 (36 mg, 62%) as a white solid. LCMS: RT 2.90 min [M+H]+ 498.3. 1H NMR (DMSO, 400 MHz): delta 8.78 (1H, d, J=2.41 Hz), 8.01 (1H, s), 7.94 (1H, s), 7.63 (1H, dd, J=8.63, 2.42 Hz), 7.28 (1H, d, J=8.62 Hz), 5.73-5.72 (1H, m), 4.63-4.59 (4H, m), 3.53 (1H, d, J=11.02 Hz), 3.43 (1H, d, J=9.07 Hz), 2.70-2.68 (2H, m), 2.33-2.32 (1H, m), 2.19-2.11 (1H, m), 1.93-1.92 (3H, m), 1.62 (1H, d, J=12.59 Hz), 1.57-1.52 (2H, m), 1.49 (6H, t, J=6.30 Hz), 1.38-1.16 (2H, m), 1.01-0.87 (1H, m)

The synthetic route of 4430-75-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Genentech, Inc.; US2012/245144; (2012); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

4430-75-5, name is Octahydro-2H-pyrido[1,2-a]pyrazine, belongs to pyrazines compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. name: Octahydro-2H-pyrido[1,2-a]pyrazine

EXAMPLE 84 5-(3,4-Dimethoxybenzylamino)-2-(2-furyl)-8-(1,3,4,6,7,8,9,9a-octahydropyrido[1,2-a]pyrazin-2-ylmethyl)[1,2,4]triazolo[1,5-c]pyrimidine (Compound 84) The subject compound (92%) was obtained as a pale brown oily matter from 5-(3,4-dimethoxybenzylamino)-8-formyl-2-(2-furyl)[1,2,4]triazolo[1,5-c]pyrimidine and 1,3,4,6,7,8,9,9a-octahydropyrido[1,2-a]pyrazine in a manner similar to that in Example 1. 1H NMR (CDCl3, delta, ppm): 1.24-1.26 (m, 2H), 1.48-1.51 (m, 2H), 1.70-1.73 (m, 2H), 2.06-2.09 (m, 4H), 2.35-2.39 (m, 1H), 2.78-2.96 (m, 4H), 3.83 (s, 2H), 3.89 (s, 3H), 3.89 (s, 3H), 4.76 (d, J=5.6 Hz, 2H), 6.40 (t, J=5.6 Hz, 1H), 6.56 (dd, J=1.8, 3.6 Hz, 1H), 6.85 (d, J=8.1 Hz, 1H), 6.95 (s, 1H), 6.97 (d, J=8.1 Hz, 1H), 7.21 (d, J=3.5 Hz, 1H), 7.59 (d, J=1.8 Hz, 1H), 7.92 (s, 1H)

The synthetic route of 4430-75-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Uesaka, Noriaki; Imma, Hironori; Kashima, Hajime; Kurokawa, Masako; Nonaka, Hiromi; Kanda, Tomoyuki; Kuwana, Yoshihisa; Toki, Shinichiro; Shimada, Junichi; US2004/110826; (2004); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Related Products of 4430-75-5, These common heterocyclic compound, 4430-75-5, name is Octahydro-2H-pyrido[1,2-a]pyrazine, 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.

Step A Ethyl 3-(octahydro-2H-pyrido[1,2-a]pyrazin-2-yl)propionate A solution of 7 g of octahydro-2H-pyrido[1,2-a]pyrazine and 15 ml of ethyl acrylate in 100 ml of acetonitrile is refluxed for 24 hours and then concentrated to dryness in vacuo to yield the expected product.

The synthetic route of 4430-75-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Goldstein, Solo; Poissonnet, Guillaume; Parmentier, Jean-Gilles; Lestage, Pierre; Lockhart, Brian; US2003/195216; (2003); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Application of 4430-75-5,Some common heterocyclic compound, 4430-75-5, name is Octahydro-2H-pyrido[1,2-a]pyrazine, molecular formula is C8H16N2, 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.

DIPEA (71 mg, 00.1 mL, 0.55 mmol) was added to a stirred solution of (R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyridine-3-carboxylic acid (75 mg, 0.22 mmol) in DMF (1.5 mL) followed by addition of EDCl (63 mg, 0.33 mmol) and HOBt (32 mg, 0.24 mmol). After 10 minutes of stirring the reaction mixture, octahydro-1H-pyrido[1,2-a]pyrazine (46 mg, 0.33 mmol) was added and the resulting mixture was stirred for 16 h at 20-35 C. The reaction mixture was diluted with cold water and extracted with ethyl acetate. The ethyl acetate layer was washed with water and brine solution. The ethyl acetate portion was dried over anhydrous sodium sulfate and concentrated under reduced pressure to afford the crude compound, which was refluxed in hexane, filtered, and the filtrate was concentrated under reduced pressure to afford 45 mg of the title compound as a yellow solid. MS (ESI): m/z 466.3 (M+H).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route Octahydro-2H-pyrido[1,2-a]pyrazine, its application will become more common.

Reference:
Patent; DR. REDDY’S LABORATORIES LTD.; Sasmal, Pradip Kumar; Ahmed, Shahadat; Prabhu, Ganesh; Tehim, Ashok; Paradkar, Vidyadhar; Dattatreya, Marahanakuli Prasanna; Mavinahalli, Nanjegowda Jagadeesh; US2015/5280; (2015); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Synthetic Route of 4430-75-5, A common heterocyclic compound, 4430-75-5, name is Octahydro-2H-pyrido[1,2-a]pyrazine, molecular formula is C8H16N2, 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.

Step A Ethyl 3-(octahydro-2H-pyrido[1,2-a]pyrazin-2-yl)propanoate A solution of 3.5 g of octahydro-2H-pyrido[1,2-a]pyrazine and 8 ml of ethyl acrylate in 50 ml of acetonitrile is refluxed for 24 hours. The solvent is removed in vacuo to yield the expected product.

The synthetic route of 4430-75-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Goldstein, Solo; Poissonnet, Guillaume; Parmentier, Jean-Gilles; Lestage, Pierre; Lockhart, Brian; US2003/195216; (2003); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Reference of 4430-75-5, The chemical industry reduces the impact on the environment during synthesis 4430-75-5, name is Octahydro-2H-pyrido[1,2-a]pyrazine, I believe this compound will play a more active role in future production and life.

Step A 2-(Octahydro-2H-pyrido[1,2-a]pyrazin-2-yl)acetonitrile 8 g of octahydro-2H-pyrido[1,2-a]pyrazine and 12 ml of acrylonitrile are refluxed for 48 hours in 150 ml of acetonitrile. The solvent is then removed in vacuo to yield 11 g of a pale yellow 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, Octahydro-2H-pyrido[1,2-a]pyrazine, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Goldstein, Solo; Poissonnet, Guillaume; Parmentier, Jean-Gilles; Lestage, Pierre; Lockhart, Brian; US2003/195216; (2003); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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 4430-75-5 as follows. Product Details of 4430-75-5

8. Synthesis of 2-(1-(triisopropylsityl)-1H-indol-6-yl)-octahydro-1H-pyrido[1,2-a]pyrazine Into a 100 mL 3-necked round-bottom flask purged and maintained with an inert atmosphere of nitrogen was placed 6-bromo-1-(triisopropylsilyl)-1H-indole (2 g, 5.40 mmol). To this was added octahydro-1H-pyrido[1,2-a]pyrazine (2.1 g, 14.25 mmol). Addition of t-BuONa (2 g, 20.83 mmol) was next. This was followed by the addition of (t-Bu)3P (200 mg, 0.99 mmol). This was followed by the addition of Pd(OAc)2 (50 mg, 0.22 mmol). To the mixture was added xylene (30 mL). The resulting solution was allowed to react, with stirring, for 2 hours while the temperature was maintained at 110 C. in a bath of oil. The reaction progress was monitored by TLC (CH2Cl2MeOH=10:1). The resulting mixture was washed 1 time with 30 mL of H2O. The resulting solution was extracted three times with 100 mL of ethyl acetate and the organic layers combined. The resulting mixture was washed 1 time with 10 mL of NaCl(sat.). The mixture was dried over Na2SO4 and concentrated by evaporation under vacuum using a rotary evaporator. This resulted in 2.15 g (80%) of 2-(1-(triisopropylsilyl)-1H-indol-6-yl)-octahydro-1H-pyrido[1,2-a]pyrazine as red oil.

According to the analysis of related databases, 4430-75-5, the application of this compound in the production field has become more and more popular.

Reference:
Patent; MEMORY PHARMACEUTICALS CORPORATION; US2008/200471; (2008); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem