Category: 40155-47-3

These common heterocyclic compound, 40155-47-3, name is 3-Methoxypyrazine-2-carboxylic acid, 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. Product Details of 40155-47-3

[0423] A solution of 3-amino-4-(4-(2,4-difluorophenoxy)piperidin-l-yl)benzonitrile (50 mg, 0.152 mmol), 3~niethoxypyrazme-2-carboxyiie acid (46.8 mg, 0.304 mmol), HATU (115 mg, 0.304 mmol) and DIPEA (106 mu,, 0.607 mmol) in DMF (759 muEpsilon) was stirred on a hot plate at 80C overnight. The reaction mixture was filtered through a Millipore filter, diluted with DMF and MeOH, and purified by HPLC (Shimadzu) eluting with a gradient of ACN in water (basic mode) to give the title compound as a light brown solid (68.7 mg, 97%). .H NMR (400 MHz, CDCb) delta ppm 2.07 – 2.18 (m, 2 H), 2.19 – 2.28 (m, 2 H), 2.91 (ddd, J=l 1.68, 8.02, 3.28 Hz, 2 H), 3.26 (ddd,./ 1 1.62. 7.58, 3.54 Hz, 2 H), 4.18 (s, 3 H), 4.37 – 4.45 (m, 1H), 6.78 ·· 6.86 (m, 1H), 6.90 (ddd,.7=11, 12, 8.34, 3.03 Hz, 1H), 7.03 (td,.7=9.09, 5,56 Hz, 1H), 7.23 (d,.7=8,34 Hz, 1H), 7.41 (dd, J=8.34, 2.02 Hz, 1H), 8.26 (d, J=2.27 Hz, 1H), 8.41 (d, J=2.53 Hz, 1H), 8.93 (d,./ 1.77 Hz, 1H), 10.62 (s, 1H); ESI-MS m/z [M+H}+ 466.2.

The synthetic route of 3-Methoxypyrazine-2-carboxylic acid has been constantly updated, and we look forward to future research findings.

Reference:
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; GREEN, Jason; HOPKINS, Maria; JONES, Benjamin; KIRYANOV, Andre A.; KUEHLER, Jon; MONENSCHEIN, Holger; MURPHY, Sean; NIXEY, Thomas; SUN, Huikai; (300 pag.)WO2018/183145; (2018); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

These common heterocyclic compound, 40155-47-3, name is 3-Methoxypyrazine-2-carboxylic acid, 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. Computed Properties of C6H6N2O3

[0423] A solution of 3-amino-4-(4-(2,4-difluorophenoxy)piperidin-l-yl)benzonitrile (50 mg, 0.152 mmol), 3~niethoxypyrazme-2-carboxyiie acid (46.8 mg, 0.304 mmol), HATU (115 mg, 0.304 mmol) and DIPEA (106 mu,, 0.607 mmol) in DMF (759 muEpsilon) was stirred on a hot plate at 80C overnight. The reaction mixture was filtered through a Millipore filter, diluted with DMF and MeOH, and purified by HPLC (Shimadzu) eluting with a gradient of ACN in water (basic mode) to give the title compound as a light brown solid (68.7 mg, 97%). .H NMR (400 MHz, CDCb) delta ppm 2.07 – 2.18 (m, 2 H), 2.19 – 2.28 (m, 2 H), 2.91 (ddd, J=l 1.68, 8.02, 3.28 Hz, 2 H), 3.26 (ddd,./ 1 1.62. 7.58, 3.54 Hz, 2 H), 4.18 (s, 3 H), 4.37 – 4.45 (m, 1H), 6.78 ¡¤¡¤ 6.86 (m, 1H), 6.90 (ddd,.7=11, 12, 8.34, 3.03 Hz, 1H), 7.03 (td,.7=9.09, 5,56 Hz, 1H), 7.23 (d,.7=8,34 Hz, 1H), 7.41 (dd, J=8.34, 2.02 Hz, 1H), 8.26 (d, J=2.27 Hz, 1H), 8.41 (d, J=2.53 Hz, 1H), 8.93 (d,./ 1.77 Hz, 1H), 10.62 (s, 1H); ESI-MS m/z [M+H}+ 466.2.

The synthetic route of 3-Methoxypyrazine-2-carboxylic acid has been constantly updated, and we look forward to future research findings.

Reference:
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; GREEN, Jason; HOPKINS, Maria; JONES, Benjamin; KIRYANOV, Andre A.; KUEHLER, Jon; MONENSCHEIN, Holger; MURPHY, Sean; NIXEY, Thomas; SUN, Huikai; (300 pag.)WO2018/183145; (2018); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

These common heterocyclic compound, 40155-47-3, name is 3-Methoxypyrazine-2-carboxylic acid, 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. Recommanded Product: 40155-47-3

4-(31) N-(3-((4aS,5S,7aS)-2-amino-5-(fluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4,5-difluorophenyl)-5-methoxypyrazine-2-carboxamide (also called 4-(17)) Methoxypyrazine-2-carboxylic acid (159 mg), PyBOP (898 mg), and diisopropylethylamine (754 mul) were added to a mixture of tert-butyl ((4aS,5S,7aS)-7a-(5-amino-2,3-difluorophenyl)-5-(fluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-2-yl)carbamate, obtained in Preparation Example 4-(30), (359 mg) in DCM (14 ml) at RT. The mixture was stirred for 3 h at the same temperature. The resultant mixture was purified directly by silica gel column chromatography (gradient from 15% to 70% EtOAc in heptane).

The synthetic route of 3-Methoxypyrazine-2-carboxylic acid has been constantly updated, and we look forward to future research findings.

Reference of 40155-47-3,Some common heterocyclic compound, 40155-47-3, name is 3-Methoxypyrazine-2-carboxylic acid, molecular formula is C6H6N2O3, 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 a solution of amine salt E1.1 (0.868g, 3.39 mmol) and carboxylic acid 1a (0.475g, 3.08 mmol) in DCE (50 mL) at room temperature was sequentially added bromotripyrrolidinophosphonium hexafluorophosphate (1.80 g, 3.85 mmol), and DIEA (1.59g, 112.33 mmol). The reaction was then stirred at room temperature for 72 hours. Then CH2CI2 (100 mL) and water (100 mL) were added to the reaction, layers separated, and the organic phase washed with water (2 x 100 mL), dried over Na2S04, and concentrated in vacuoto afford a residue. The residue was purified by column chromatography using silica gel, eluting with 100% EtOAc, to afford the desired compound as an off white solid (0.690g, 69% yield). LC-MS: mass calc’d. for C17H15CI2N5O2 [M+H]+ 356.1 , found 356.0; tR= 0.688 min.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 3-Methoxypyrazine-2-carboxylic acid, its application will become more common.