Month: April 2021

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. 496-12-8, name is Isoindoline, A new synthetic method of this compound is introduced below., Product Details of 496-12-8

General procedure: Isoindoline (0.5 g, 4.2 mmol, 1.0 equiv) was dissolved in dry pyridine (10 ml). Methane sulfonyl chloride (0.65 g, 5.9 mmol, 1.4 equiv) was added dropwise and the reaction mixture was stirred overnight at rt. Monitoring by HPLC and LCMS indicated that the reaction was completed. The solvent was evaporated under reduced pressure. A solution of HCl 1N (50 mL) and EtOAc (50 mL) were added. The organic layer was separated and the aqueous phase was extracted twice with EtOAc (2×50 mL). The combined organic phase was dried over Na2SO4 and the solvent was evaporated under reduced pressure to yield the pure product: 325 mg, 39 % yield.

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.

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. 6326-79-0, name is 6-Bromoisatin, A new synthetic method of this compound is introduced below., category: indolines-derivatives

Step 1: Synthesis of Intermediate 1-5.1To RiO (25.0 g, 111 mmol) in acetonitrile (750 mL) is added Mel (15 mL, 241 mmol) and K2C03(60.0 g, 434 mmol) and the reaction mixture is stirred at 60 C for 2 h. The reaction mixture isfiltered and concentrated. Water and ethyl acetate are added to the residue. The organic layer isextracted twice with water, is dried over MgSO4 and concentrated. Yield 56%, m/z 240/242[M+H]+, rt 0.48 mi LC-MS Method X001 004.

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.

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. 1074-82-4, name is Potassium 1,3-dioxoisoindolin-2-ide belongs to indolines-derivatives compound, it is a common compound, a new synthetic route is introduced below. Product Details of 1074-82-4

To a stirred solution of 1,6-dibromohexane (12.3 mL, 81.0 mmol) in DMF (10 mL), was added potassium phthalate (5.0 g, 27.0 mmol) portion-wise over 30 min at room temperature. After complete addition, the reaction mixture was stirred at 90 C for 18 h, then quenched with water (300 mL) and extracted with diethyl ether (150 mL x 2). The combined organic extracts were washed with water (100 mL x 2), followed by brine (50 mL x 2) and dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure. The resultant residue was purified by silica gel column chromatography (60-120 mesh) using 5-10% EtOAc / hexanes to afford 3-i as an off- white solid (6.3 g, 76% yield). LCMS: 310.95 (M+1).

The synthetic route of 1074-82-4 has been constantly updated, and we look forward to future research findings.

Reference of 675109-26-9, 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. 675109-26-9, name is 6-Bromoisoindolin-1-one belongs to indolines-derivatives compound, it is a common compound, a new synthetic route is introduced below.

Preparation 314: Mixture of 6-bromo-2-(2-methoxyethyl)isoindolin-1-one and 6-bromo- 2,3-bis(2-methoxyethyl)isoindolin-1 -one (2064) (2065) Sodium hydride (60% wt in mineral oil) (0.1 13 g, 2.83 mmol) was added to a stirred solution of 6-bromoisoindolin-1-one (0.5 g, 2.358 mmol) and 1-bromo-2-methoxyethane (0.277 ml, 2.83 mmol) in DMF (12 mL) under nitrogen at 0 C. The resulting orange solution was allowed to warm slowly to room temperature and stirred for 3 days. The reaction was quenched with water (15 mL) and extracted with EtOAc (3 x 15 mL). The organic extracts were combined and washed with brine (50 mL), dried (MgS04), filtered, and concentrated in vacuo to afford a yellow oil. The crude product was purified by chromatography (S1O2, 24 g GRACE column, 0-100% EtOAc in isohexane) to afford a mixture of 6-bromo-2-(2-methoxyethyl)isoindolin-1-one (549 mg, 62.9%) and 6-bromo-2,3-bis(2-methoxyethyl)isoindolin-1-one as a yellow oil (~3: 1 ratio by LCMS and NMR analyses). Further purification by chromatography (S1O2, 24 g GRACE column, 0-10% MeOH in DCM) did not improve ratio of products, which was used without further purification in the next step. LCMS: [M+H]+ = 270 and 328.

The synthetic route of 6-Bromoisoindolin-1-one has been constantly updated, and we look forward to future research findings.

Electric Literature of 18711-13-2, These common heterocyclic compound, 18711-13-2, name is 4,7-Dichloroindoline-2,3-dione, 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.

4,7-Dichloro-3-(2-(4-cyclopropylphenyl)-2-oxoethyl)-3-hydroxyindolin-2-one EXAMPLE 7): To 4,7-dichloroindoline-2,3-dione (A) (300 mg, 1.39 mmol) in 15 niL of methanol were added l-(4-cyclopropylphenyl)ethanone (B) (0.9 g, 5.5 mmol) and 10 drops of diethylamine (2). The reaction was stirred at 50C for 24 hours. The solvent was removed and the residue was purified with flash chromatography (0-5% Methanol/CH2C12) to get an off white solid. 4,7-Dichloro-3-(2-(4-cyclopropylphenyl)-2-oxoethyl)-3-hydroxyindolin-2- one (EXAMPLE 7): off-white solid; 1H NMR (DMSO-d6, 400 MHz) delta 0.76 (m, 2H), 1.06 (m, 2H), 2.0(m, 1H), 3.65 (d, 1H, J=16 Hz), 4.35 (d, 1H, J=16Hz), 6.43(s, 1H), 6.89(d, 1H, J=8Hz), 7.19 (d, 2H, J=8Hz), 7.30 (d, 1H, J=8Hz), 7.79 (d, 2H, J=8Hz), 10.97 (s, 1H).

Statistics shows that 4,7-Dichloroindoline-2,3-dione is playing an increasingly important role. we look forward to future research findings about 18711-13-2.

Application of 239463-85-5, 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. 239463-85-5, name is (R)-3-(5-(2-Aminopropyl)-7-cyanoindolin-1-yl)propyl benzoate (2R,3R)-2,3-dihydroxysuccinate belongs to indolines-derivatives compound, it is a common compound, a new synthetic route is introduced below.

General procedure: Fifty grams of 5-[(2R)-2-aminopropyl]-1-[3-(bezoyloxy)propyl]-2,3-dihydro-1H-indol-7-carbonitrile (2R,3R)-2,3-dihydroxybutanedioate (tartrate salt of the compound of formula (III), 26.9 g of K2CO3, 39.8 g of 2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl methanosulfonate and 250 mL of acetonitrile are introduced in a 500 mL reactor with mechanical stirring. It is heated to reflux for 24 h. After this time has elapsed, it is cooled at 20 C. and AcOEt (400 mL) and water (250 mL) are added. It is stirred for 30 min, and the phases are separated. The organic phase is dried with anhydrous sodium sulfate, filtered and concentrated to dryness, obtaining 70.9 g of 3-{7-cyano-5-[(2R)-2-({2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl}amino)propyl]-2,3-dihydro-1H-indol-1-yl}propyl benzoate (free base). Eighteen grams of 3-{7-cyano-5-[(2R)-2-({2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl}amino)propyl]-2,3-dihydro-1H-indol-1-yl}propyl benzoate are weighed and dissolved in 90 mL of 96% EtOH. Fifteen milliliters are distributed in different balloons. A different acid (for example, 0.60 g of maleic acid) dissolved in 15 mL of 96% EtOH is added to each balloon. It is left under stirring at room temperature for two hours, and then cooled at 0-5 C., maintaining stirring. In the case of maleic acid, the maleate precipitates after 30 minutes. If a salt is formed, it is filtered, washed with 96 C. EtOH and vacuum dried. Table 2 shows the result obtained with different acids.

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, (R)-3-(5-(2-Aminopropyl)-7-cyanoindolin-1-yl)propyl benzoate (2R,3R)-2,3-dihydroxysuccinate, other downstream synthetic routes, hurry up and to see.

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. 22190-33-6, name is 5-Bromoindoline, This compound has unique chemical properties. The synthetic route is as follows., category: indolines-derivatives

To a stirred solution of 5- bromo-indoline (3.0 g , 15mmol) in acetonitrile (100 ml), was added DMAP (0.185 g , 1.522 mmol) and di-ieri-butyl dicarbonate (3.98 g, 18.3 mmol) and the reaction was stirred at RT for 16 h. The reaction mixture was concentrated on reduced pressure to obtain a residue which was diluted with diethyl ether and washed with water and brine solution (2X). The combined ether layer was dried over anhydrous Na2S04 and concentrated under reduced pressure to afford the crude product as an off-white solid, which was used in the next step without further purification (3.0 g).

According to the analysis of related databases, 22190-33-6, the application of this compound in the production field has become more and more popular.

Synthetic Route of 59-48-3,Some common heterocyclic compound, 59-48-3, name is Indolin-2-one, molecular formula is C8H7NO, 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.

PREPARATION 17 5-Acetyl-2-oxindole To 95 ml. of carbon disulfide was added 27 g. (0.202 mole) of aluminum chloride, followed by the dropwise addition of a solution of 3 ml. (0.042 mole) of acetyl chloride in 5 ml. of carbon disulfide, with stirring. Stirring was continued for 5 minutes and then 4.4 g. (0.033 mole) of 2-oxindole was added. The resulting mixture was heated under reflux for 4 hours and cooled. The carbon disulfide was removed by decantation and the residue was triturated under water and recovered by filtration. After drying, 3.2 g. of the title compound was obtained, m.p. 225-227 C.

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

Reference of 446292-07-5,Some common heterocyclic compound, 446292-07-5, name is (R)-2-(2-Hydroxy-3-((4-(3-oxomorpholino)phenyl)amino)propyl)isoindoline-1,3-dione, molecular formula is C21H21N3O5, 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.

In a four neck round bottom flask, charged dichloromethane (3400ml), 2-((2R)-2-Hydroxy-3- {[4-(3-oxo-4-morpholinyl)phenyl]amino}propyl)-lH-isoindole-l,3(2H)-dione (340 g) and Nu,Nu’ -dicarbonyldiimidazole (209.13 g) at 25 to 30C. The obtained reaction mass then stirred for 8hr. at 25 to 30C. Reaction mass is concentrated under reduced pressure to obtain residue. Added tetrahydrofuran (1700 ml) to residue. The obtained mixture is heated to 40 to 45C for 30 minutes followed by cooling to room temperature. Finally obtained solid is filtered off and washed by tetrahydrofuran(170 ml) Yield =93.55%

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route (R)-2-(2-Hydroxy-3-((4-(3-oxomorpholino)phenyl)amino)propyl)isoindoline-1,3-dione, its application will become more common.

Adding a certain compound to certain chemical reactions, such as: 897957-06-1, name is 6-Bromo-1-methylindolin-2-one, belongs to indolines-derivatives compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 897957-06-1, HPLC of Formula: C9H8BrNO

vi) (S)-tert-Butyl 2-((S)-l-amino-3-(4-(l-methyl-2-oxoindolin-6-yl)phenyl)-l-oxopropan- 2-ylcarbamoyl)piperidine-l-carboxylate(S)-tert-Butyl 2-((S)- 1 -amino- 1 -oxo-3-(4-(4,4,5 ,5-tetramethyl- 1 ,3 ,2-dioxaborolan-2- yl)phenyl)propan-2-ylcarbamoyl)piperidine-l-carboxylate (Example 1, step (iv), 200 mg) was dissolved in acetonitrile (15 mL) and treated with aqueous 2M potassium carbonate (0.6 mL), 1,1 delta(di-fert-butylphosphino)ferrocene palladium dichloride (24 mg) and 6-bromo-l- methylindolin-2-one (Example 1 , step (v), 90 mg) with stirring under nitrogen. The reaction was heated to 800C for 4h. The reaction mixture was diluted with dichloromethane (30 rnL) and dried with magnesium sulfate before being passed through an isolute HM-N cartridge, washed through with dichloromethane. The organic extracts were concentrated in vacuo and purified by flash silica chromatography eluting with ethyl acetate to give the sub-titled compound (200 mg).m/e (APCI+) 421 [M+2H-BOC]+

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it.