Category: 1520-70-3

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. 1520-70-3, name is Ethanesulfonamide, A new synthetic method of this compound is introduced below., name: Ethanesulfonamide

Example 19: 5-(4-CHLOROPHENYL)-6-CYCLOHEXYL-N-(ETHYLSULFONYL)-4-(2- MORPHOLIN-4-YL-2-OXOETHYL)-4H-THIENO [3, 2-B] PYRROLE-2-CARBOXAMIDE; A solution (0.015 M) of 5- (4-CHLOROPHENYL)-6-CYCLOHEXYL-4- (2-MORPHOLIN-4- YL-2-OXOETHYL)-4H-THIENO [3, 2-B] PYRROLE-2-CARBOXYLIC acid in THF at RT was treated with CDI (1. 1 eq. ) and DMAP (1.1 eq. ). After stirring for 1H at RT, ETHANESULFONAMIDE (2 eq. ) and DBU (2 eq. ) were added. The mixture was heated to reflux for 5 h then cooled down and diluted with AcOEt. The organic phase was washed with aqueous HC1 (0.1 N) and dried. Evaporation of the solvent under reduced pressure gave a residue which was purified by RP-HPLC (Conditions : Waters X-TERRA MS C18,10 micron, 19 x 100 mm ; flow : 20 ML/MIN ; Gradient : A: H20 + 0.05percent TFA ; B : MECN + 0.05percent TFA ; 50percent A isocratic for 1 min then linear to 20percent A in 9 min) to afford the title compound (17percent) as a solid. ‘H NMR (400 MHz, DMSO-d6, 300 K) 8 1. 1-1.3 (m, 7H), 1.5-1. 8 (m, 8H), 2.44 (m, 1H), 3.4-3. 6 (m, 8H), 4.83 (s, 2H), 7.33 (d, J = 8.0 Hz, 2H), 7.61 (d, J = 8. 0 Hz, 2H), 8. 07 (s, 1H), 11.91 (bs, 1H); MS (ES+) M/Z 578, 580 (M+H) +.

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; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPA; WO2005/23819; (2005); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

1520-70-3, name is Ethanesulfonamide, belongs to amides-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. HPLC of Formula: C2H7NO2S

A solution (0.05 M) of 3-cyclohexyl-1-[2(dimethylamino)-2-oxoethyl]-2-phenyl-1H- INDOLE-6-CARBOXYLIC acid (from Example 7) in CH2C12 was treated with DMAP (1.5 EQ.) and ethane sulfonamide (1.5 eq. ). EDCI (1.5 eq. ) was added and the mixture was stirred overnight. The volatiles were evaporated under reduced pressure and the residue was purified by RP-HPLC to afford the title compound (42 percent) as a solid. 1H NMR (400 MHz, DMSO-d6, 300 K) 8 1.20-1. 43 (m, 3H), 1.28 (T, J 7. 2 Hz, 3H) 1.63-1. 80 (m, 7H), 2.50-2. 58 (m, 1H, under DMSO), 2.80 (s, 3H), 2.90 (s, 3H), 3.51 (q, J 7. 2 Hz, 2H), 4.57 (s, 2H), 7.31-7. 36 (m, 2H), 7.49-7. 56 (m, 3H), 7.66 (d, J 9. 0 Hz, 1H), 7.85 (d, J 9. 0 Hz, 1H), 8.05 (s, 1H), 10.76 (br s, 1H) ; MS (ES+) m/z 496 (M+H) +.

The synthetic route of 1520-70-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPA; WO2004/87714; (2004); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Synthetic Route of 1520-70-3,Some common heterocyclic compound, 1520-70-3, name is Ethanesulfonamide, molecular formula is C2H7NO2S, 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 stirred solution of free acid (50 mg, 0.11 mmol) from Example 226 in 1 ML of methylene chloride was added ethyl sulfonamide (18 mg, 0.17 mmol), EDAC (25 mg, 0.13 mmol), and DAMP (2.7 mg, 0.022 mmol) sequentially.The mixture was stirred at ambient temperature for 16 h.The solvent was then removed on a rotavap under reduced pressure and the residue was purified on an Alltech sep-pak, eluding with 1percent MeOH in EtOAc to give 30 mg (50percent yield) of the title compound as a light yellow solid. 1H NMR (CDCl3, 300 MHz) delta 1.18 (d, J=6.3 Hz, 6H), 1.34 (t, J=7.5 Hz, 3H), 1.61-1.74 (m, 2H), 1.84-2.04 (m, 1H), 2.13-2.35 (m, 1H), 2.60-2.75 (m, 2H), 3.44 (p, J=7.5 Hz, 2H), 3.53-3.66 (m, 1H), 3.66-3.85 (m, 2H), 4.00-4.18 (m, 1H), 6.71 (d, J=8.7 Hz, 1H), 6.88 (d, J=15.6 Hz, 1H), 7.31 (dd, J=2.4, 8.4 Hz, 1H), 7.41 (d, J=1.8, 8.4 Hz, 1H), 7.51 (d, J=1.8 Hz, 1H), 7.54 (d, J=8.4 Hz, 1H), 7.67 (d, J=15.6 Hz, 1H), 8.43 (s, 1H). MS (ESI+) (M+H)+ at m/z 546.

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

Reference:
Patent; Abbott Laboratories; US2004/116518; (2004); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

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. 1520-70-3, name is Ethanesulfonamide, A new synthetic method of this compound is introduced below., HPLC of Formula: C2H7NO2S

Example 19: 5-(4-CHLOROPHENYL)-6-CYCLOHEXYL-N-(ETHYLSULFONYL)-4-(2- MORPHOLIN-4-YL-2-OXOETHYL)-4H-THIENO [3, 2-B] PYRROLE-2-CARBOXAMIDE; A solution (0.015 M) of 5- (4-CHLOROPHENYL)-6-CYCLOHEXYL-4- (2-MORPHOLIN-4- YL-2-OXOETHYL)-4H-THIENO [3, 2-B] PYRROLE-2-CARBOXYLIC acid in THF at RT was treated with CDI (1. 1 eq. ) and DMAP (1.1 eq. ). After stirring for 1H at RT, ETHANESULFONAMIDE (2 eq. ) and DBU (2 eq. ) were added. The mixture was heated to reflux for 5 h then cooled down and diluted with AcOEt. The organic phase was washed with aqueous HC1 (0.1 N) and dried. Evaporation of the solvent under reduced pressure gave a residue which was purified by RP-HPLC (Conditions : Waters X-TERRA MS C18,10 micron, 19 x 100 mm ; flow : 20 ML/MIN ; Gradient : A: H20 + 0.05percent TFA ; B : MECN + 0.05percent TFA ; 50percent A isocratic for 1 min then linear to 20percent A in 9 min) to afford the title compound (17percent) as a solid. ‘H NMR (400 MHz, DMSO-d6, 300 K) 8 1. 1-1.3 (m, 7H), 1.5-1. 8 (m, 8H), 2.44 (m, 1H), 3.4-3. 6 (m, 8H), 4.83 (s, 2H), 7.33 (d, J = 8.0 Hz, 2H), 7.61 (d, J = 8. 0 Hz, 2H), 8. 07 (s, 1H), 11.91 (bs, 1H); MS (ES+) M/Z 578, 580 (M+H) +.

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; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPA; WO2005/23819; (2005); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

1520-70-3, name is Ethanesulfonamide, belongs to amides-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. category: amides-buliding-blocks

A solution (0.05 M) of 3-cyclohexyl-1-[2(dimethylamino)-2-oxoethyl]-2-phenyl-1H- INDOLE-6-CARBOXYLIC acid (from Example 7) in CH2C12 was treated with DMAP (1.5 EQ.) and ethane sulfonamide (1.5 eq. ). EDCI (1.5 eq. ) was added and the mixture was stirred overnight. The volatiles were evaporated under reduced pressure and the residue was purified by RP-HPLC to afford the title compound (42 percent) as a solid. 1H NMR (400 MHz, DMSO-d6, 300 K) 8 1.20-1. 43 (m, 3H), 1.28 (T, J 7. 2 Hz, 3H) 1.63-1. 80 (m, 7H), 2.50-2. 58 (m, 1H, under DMSO), 2.80 (s, 3H), 2.90 (s, 3H), 3.51 (q, J 7. 2 Hz, 2H), 4.57 (s, 2H), 7.31-7. 36 (m, 2H), 7.49-7. 56 (m, 3H), 7.66 (d, J 9. 0 Hz, 1H), 7.85 (d, J 9. 0 Hz, 1H), 8.05 (s, 1H), 10.76 (br s, 1H) ; MS (ES+) m/z 496 (M+H) +.

The synthetic route of 1520-70-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPA; WO2004/87714; (2004); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Related Products of 1520-70-3,Some common heterocyclic compound, 1520-70-3, name is Ethanesulfonamide, molecular formula is C2H7NO2S, 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 stirred solution of free acid (50 mg, 0.11 mmol) from Example 226 in 1 ML of methylene chloride was added ethyl sulfonamide (18 mg, 0.17 mmol), EDAC (25 mg, 0.13 mmol), and DAMP (2.7 mg, 0.022 mmol) sequentially.The mixture was stirred at ambient temperature for 16 h.The solvent was then removed on a rotavap under reduced pressure and the residue was purified on an Alltech sep-pak, eluding with 1percent MeOH in EtOAc to give 30 mg (50percent yield) of the title compound as a light yellow solid. 1H NMR (CDCl3, 300 MHz) delta 1.18 (d, J=6.3 Hz, 6H), 1.34 (t, J=7.5 Hz, 3H), 1.61-1.74 (m, 2H), 1.84-2.04 (m, 1H), 2.13-2.35 (m, 1H), 2.60-2.75 (m, 2H), 3.44 (p, J=7.5 Hz, 2H), 3.53-3.66 (m, 1H), 3.66-3.85 (m, 2H), 4.00-4.18 (m, 1H), 6.71 (d, J=8.7 Hz, 1H), 6.88 (d, J=15.6 Hz, 1H), 7.31 (dd, J=2.4, 8.4 Hz, 1H), 7.41 (d, J=1.8, 8.4 Hz, 1H), 7.51 (d, J=1.8 Hz, 1H), 7.54 (d, J=8.4 Hz, 1H), 7.67 (d, J=15.6 Hz, 1H), 8.43 (s, 1H). MS (ESI+) (M+H)+ at m/z 546.

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

Reference:
Patent; Abbott Laboratories; US2004/116518; (2004); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

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. 1520-70-3 name is Ethanesulfonamide, This 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. 1520-70-3

EXAMPLE 154 N-(4-fluorobenzyl)-8-hydroxy-5-[methyl(methylsulfonyl)amino]-1,6-naphthyridine-7-carboxamide To a mixture of methyl-methanesulfonamide (1.06 g, 9.65 mmol), 5-bromo-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide (1.21 g, 3.22 mmol), and Cu2O (0.46 g, 3.22 mmol) under an atmosphere of argon was added pyridine (25 mL) and the suspension was stirred at reflux for 16 hr. The reaction was allowed to cool to room temperature and the solvent evaporated in vacuo. The residue was treated with DMF (12 mL) and TFA (0.5 mL) and filtered to remove the solids. The filtrate was purified by reverse phase HPLC. (Waters PrePak 500 cartridge C18, Gradient elution with Water: Acetonitrile 95:5 to 5:95 with 0.1percent TFA at 75 mL/min over 45 mins). Lyophilization of the pure fractions afforded the title compound as an off white solid. 1H NMR (d6DMSO, 400 MHz) delta 13.80 (1H, s), 9.66 (1H, t, J=6.4 Hz), 9.19 (1H, d, J=4.2 Hz), 8.62 (1H, d, J=8.4 Hz), 7.88 (1H, dd, J=8.4 and 4.2 Hz), 7.41 (2H, dd, J=8.6 and 5.7 Hz), 7.18 (2H, t, J=8.9 Hz), 4.61 (2H, d, J=6.4 Hz) 3.38 (3H, s), 3.19 (3H, s) ppm. FAB MS calcd for C18H17FN4O4S 405 (MH+), found 405.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, Ethanesulfonamide, and friends who are interested can also refer to it.

Reference:
Patent; Anthony, Neville J.; Gomez, Robert P.; Young, Steven D.; Egbertson, Melissa; Wai, John S.; Zhuang, Linghang; Embrey, Mark; Tran, LeKhanh; Melamed, Jeffrey Y.; Langford, H. Marie; Guare, James P.; Fisher, Thorsten E.; Jolly, Samson M.; Kuo, Michelle S.; Perlow, Debra S.; Bennett, Jennifer J.; Funk, Timothy W.; US2003/55071; (2003); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics