Downstream synthetic route of 1265231-91-1

As the paragraph descriping shows that 1265231-91-1 is playing an increasingly important role.

1265231-91-1, 3-(Dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1265231-91-1, Step 1: Synthesis of [5-amino-1-(2-methyl-1H-benzimidazol-5-yl)-1H-pyrazol-4-yl]-(1-benzenesulfonyl-1H-indol-2-yl)-methanone (1001) (2-Methyl-1H-benzimidazol-5-yl)-hydrazine dihydrochloride (830 mg) was added to an ethanol solution (15 ml) of crude 2-(1-benzenesulfonyl-1H-indole-2-carbonyl)-3-dimethylamino acrylonitrile (1.17 g). The reaction mixture was heated with stirring under reflux for four hours. After cooling to room temperature, the mixture was allowed to stand at room temperature. The precipitated solid was collected by filtration, and washed with ethanol to give [5-amino-1-(2-methyl-1H-benzimidazol-5-yl)-1H-pyrazol-4-yl]-(1-benzenesulfonyl-1H-indol-2-yl)-methanone was obtained as a yellow solid (1.5 g, with a two-step yield of 91%). 1H-NMR (DMSO-D6) delta: 8.15-8.13 (2H, m), 8.02 (1H, dd, J = 8.4, 0.8 Hz), 7.97 (1H, d, J = 2.0 Hz), 7.92 (1H, d, J = 8.8 Hz), 7.87 (1H, s), 7.76-7.62 (5H, m), 7.49-7.45 (1H, m), 7.36-7.26 (4H, m), 2.82 (3H, m) ESI (LC-MS positive mode) m/z 497 [(M+H)+]

As the paragraph descriping shows that 1265231-91-1 is playing an increasingly important role.

Reference:
Patent; Chugai Seiyaku Kabushiki Kaisha; F.Hoffmann-La Roche AG; EP2471786; (2012); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

New learning discoveries about 1265231-91-1

1265231-91-1, As the paragraph descriping shows that 1265231-91-1 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1265231-91-1,3-(Dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile,as a common compound, the synthetic route is as follows.

Methyl 5-hydrazinyl-1H-benzo[d]imidazole-2-carboxylatedihydrochloride 2e (300mg, 1.07mmol) and 3-(dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile If (408mg, 1.07mmol) were suspended in 30mL of absolute ethanol and the reaction solution was refluxed for 6 hours. The solution was subjected to suction filtration, the filter cake was washed with 5mL of ethanol, and the filtrate was concentrated under reduced pressure. The residue was further separated and purified by silica gel column chromatography (developing agent: system B) to obtain methyl 5-(5-amino-4-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)-1H-pyrazol-1-yl)-1H-benzo[d]imidazol -2-carboxylate 2g (143mg, yellow solid), yield: 24%. MS m / z (ESI): 540.7 [M + 1]

1265231-91-1, As the paragraph descriping shows that 1265231-91-1 is playing an increasingly important role.

Reference:
Patent; Zhejiang Hisun Pharmaceutical Co., Ltd; CHEN, Lei; GUAN, Dongliang; BAI, Hua; YAN, Xing; MIAO, Shuai; ZHU, Songsong; (54 pag.)EP3339305; (2018); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Analyzing the synthesis route of 1265231-91-1

1265231-91-1, The synthetic route of 1265231-91-1 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1265231-91-1,3-(Dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile,as a common compound, the synthetic route is as follows.

2-(1-Fluorocyclopropyl)-5-hydrazinyl-1H-benzo[d]imidazole dihydrochloride 10d (706mg, 2.5 3mmol) and (E)-3-(dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile 1f (959mg, 2.53mmol, prepared according to the published patent application ) were suspended in 13mL of absolute ethanol, the reaction solution was refluxed for 4 hours. The reaction solution was cooled down to room temperature, solid precipitated. The solution was subjected to suction filtration, the filter cake was washed with ethanol (15mL*3) then was subjected to infrared drying to obtain (5-amino-1-(2-(1-fluoropropyl)-1H-benzo[d]imidazol-5-yl)-1H-pyrazol-4-yl)(1-(phenylsulfonyl)-1H-indol-2-yl)methanone 10e (493mg, black solid), yield: 36%. MS m / z (ESI): 540.8 [M + 1]

1265231-91-1, The synthetic route of 1265231-91-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Zhejiang Hisun Pharmaceutical Co., Ltd; CHEN, Lei; GUAN, Dongliang; BAI, Hua; YAN, Xing; MIAO, Shuai; ZHU, Songsong; (54 pag.)EP3339305; (2018); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Simple exploration of 1265231-91-1

1265231-91-1 3-(Dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile 68005411, aindole-building-block compound, is more and more widely used in various fields.

1265231-91-1, 3-(Dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,1265231-91-1

2-Cyclopropyl-5-hydrazinyl-1H-benzo[d]imidazole 1e (540mg, 2.06mmol) and 3-(dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile 1f (581mg, 1.53mmol, prepared according to the published patent application ) were suspended in 30 mL of absolute ethanol, the reaction solution was refluxed for 6 hours. The reaction solution was cooled down to room temperature, solid precipitated. The solution was subjected to suction filtration, the filter cake was washed with 5mL of ethanol and then subjected to infrared drying to obtain (5-amino-1-(2-cyclopropyl-1H-benzo[d]imidazol-5-yl)-1H-pyrazol-4-yl)(1-(phenylsulfonyl)-1H-i ndol-2-yl)methanone 1g (675mg, tan solid), yield 67%. MS m / z (ESI): 522.8 [M + 1]

1265231-91-1 3-(Dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile 68005411, aindole-building-block compound, is more and more widely used in various fields.

Reference:
Patent; Zhejiang Hisun Pharmaceutical Co., Ltd; CHEN, Lei; GUAN, Dongliang; BAI, Hua; YAN, Xing; MIAO, Shuai; ZHU, Songsong; (54 pag.)EP3339305; (2018); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Brief introduction of 1265231-91-1

1265231-91-1, The synthetic route of 1265231-91-1 has been constantly updated, and we look forward to future research findings.

1265231-91-1, 3-(Dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

N-(5-Hydrazinyl-1H-benzo[d]imidazol-2-yl)acetamidedihydrochloride 3d (500mg, 1.8mmol) and 3-(dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile 1f (477mg, 1.26mmol) were suspended in 20mL of absoluteethanol, the reaction solution was refluxed for 4 hours. The solution was subjected to suction filtration, the filtercake was washed with 5mL of ethanol then the filtrate was concentrated under reduced pressure. The residue wasfurther separated and purified by silica gel column chromatography (developing agent: system B) to obtainN-(5-(5-amino-4-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)-1H-pyrazol-1-yl)-1H-benzo[d]imida zol-2-yl) acetamide 3e(134mg, brown solid), yield: 13.8%.MS m / z (ESI): 539.8 [M + 1]

1265231-91-1, The synthetic route of 1265231-91-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Zhejiang Hisun Pharmaceutical Co., Ltd; CHEN, Lei; GUAN, Dongliang; BAI, Hua; YAN, Xing; MIAO, Shuai; ZHU, Songsong; (54 pag.)EP3339305; (2018); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Some tips on 1265231-91-1

1265231-91-1, 1265231-91-1 3-(Dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile 68005411, aindole-building-block compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1265231-91-1,3-(Dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile,as a common compound, the synthetic route is as follows.

5-Hydrazinyl-1H-benzo[d][1,2,3]triazole 5b (583mg, 1.98mmol) and 3-(dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile 1f (550mg, 1.45mmol) were suspended in 30mL of absolute ethanol, the reaction solution was heated to reflux for 4 hours. The reaction solution was diluted with 100mL of ethyl acetate, washed with saturated sodium bicarbonate solution (20mL) and then saturated sodium chloride solution (20mL), dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure to obtain (5-amino-1-(1H-benzo[d][1,2,3]triazol-5-yl)-1H-pyrazol-4-yl)(1-(phenylsulfonyl)-1H-indol-2-yl) methanone 5c (555mg, brown solid), yield: 89%. MS m / z (ESI): 483.8 [M + 1]

1265231-91-1, 1265231-91-1 3-(Dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile 68005411, aindole-building-block compound, is more and more widely used in various fields.

Reference:
Patent; Zhejiang Hisun Pharmaceutical Co., Ltd; CHEN, Lei; GUAN, Dongliang; BAI, Hua; YAN, Xing; MIAO, Shuai; ZHU, Songsong; (54 pag.)EP3339305; (2018); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles