Category: 147118-40-9

Reference of 147118-40-9 ,Some common heterocyclic compound, 147118-40-9, molecular formula is C23H30FN3O6S, 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.

Example 12(E)-7-[4-(4-Fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5- yl](3i?,55)-3,5-dihydroxyhept-6-enoic acid, hemi-calcium salt I; Tetrahydrofuran (35 ml) is added to weighed methyl ester II (6 g). 40percent solution of LiOH (10 ml) is added to the solution over 5 minutes, and the heterogenous mixture is stirred vigorously for 3 hours and then poured into a separatory funnel containing demineralized water (150 ml) and hexane (50 ml). After complete separation, ethyl acetate (40 ml) is poured into the aqueous phase and calcium acetate (2 g) is added. After 10 minutes of vigorous stirring, the phases are separated, and the aqueous phase is reextracted with ethyl acetate (20 ml). The ethyl acetate extract is washed with demineralized water (2 x 5 ml), dried, and evaporated, and the evaporation residue is dissolved in acetone and sprayed into the stream of an inert gas. 4.5 g (74 percent) of amorphous rosuvastatin is obtained. HPLC: 99.1 percent.

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. 147118-40-9, Rosuvastatin methyl ester, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; ZENTIVA, a.s.; WO2007/121; (2007); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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. 147118-40-9, name is Rosuvastatin methyl ester. This compound has unique chemical properties. The synthetic route is as follows. Application In Synthesis of Rosuvastatin methyl ester

The synthetic route is shown in flow diagram 4:The detailed preparing process is as follows:150mL acetonitrile and 18g (3R,5S,6E)-7-[4-(4-flurophenyl)-6-(1-methyl ethyl)-2-[methyl (methyl sulfonyl) amino]-5-pyrimidyl]-3,5-dihydroxy-6-methyl heptenoate were added to a 500mL reaction flask.Once the product was fully dissolved, 40mL purified water was added and the mixture was heated to 40°C.Subsequently, 42mL 1N sodium hydroxide solution was added at constant speed, wherein the addition process took around 15 minutes, and then the mixture was reacted at 40°C for 2.5 hours.The obtained solution was vacuum distilled to remove acetonitrile at 45°C, 30mL water was then added, and the mixture was cooled to 30°C with ice water.The mixture was washed three times with ethyl ether (50mL each time), wherein it was stirring for 15 minutes during each washing, the obtained mixture was allowed to stand for layering, and the water phase was collected.Then 3g activated carbon was added, the mixture was heated to 40°C and stirred for 60 minutes, the obtained mixture was filtered, the filter cake was washed with 10mL purified water, the filtrate and washing solution were combined and cooled to 20°C, and then 90mL ethyl ether was added.The pH value was adjusted to 5 with 0.5N hydrochloric acid, the mixture was stirred for 15 minutes and allowed to stand for layering for 15 minutes.The water phase was extracted twice with ethyl ether (60mL each time), wherein it was stirring for 15 minutes during each extraction, and then was allowed to stand for layering.The organic phases were combined and washed twice with saturated sodium chloride solution (60mL each time) and then allowed to stand for layering.The water phase was removed, while 6g anhydrous sodium sulfate was added to the organic phase and stirred for 35 minutes.The obtained mixture was filtered to remove anhydrous sodium sulfate, the filtrate was vacuum distilled to remove ethyl ether at 30°C, then 50g DMF and 2.5g K2CO3 were added.The mixture was vacuum distilled for 1.5 hours at 30°C to remove ethyl ether.As a result, 69.6g DMF solution containing (3R,5S,6E)-7-[4-(4-flurophenyl)-6-(1-methyl ethyl)-2-[methyl (methyl sulfonyl) amino]-5-pyrimidyl]-3,5-dihydroxy-6-heptonic acid was obtained.

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, 147118-40-9, Rosuvastatin methyl ester.

Reference:
Patent; Changzhou Pharmaceutical Factory; EP2298745; (2011); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reference of 147118-40-9, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.147118-40-9, name is Rosuvastatin methyl ester, molecular formula is C23H30FN3O6S, molecular weight is 495.56, as common compound, the synthetic route is as follows.

The fraction obtained in preparative HPLC is evaporated under reduced pressure (ca 200 mbar) to 50 ml and coled in freezer (ca -20°C) for 3 days. The suspension is filtered. The obtained crystals are dried under vacuum at 40 °C for 5 hours yielding 0,57 g of dry product, containing ca 11 percent of enantiomer; The fraction obtained in preparative HPLC is evaporated under reduced pressure (ca 200 mbar) to 50 ml and coled in freezer (ca -20°C) for 3 days. The suspension is filtered. The obtained crystals are dried under vacuum at 40 °C for 5 hours yielding 0,57 g of dry product, containing ca 11 percent of enantiomer; The filtrate of previous step is evaporated under reduced pressure and dried under vacuum at 40 °C for 5 hours yielding 0,43 g of dry product, containing less than 0,1percent of 3S, 5R enantiomer. The product is enantimerically pure MER having 99,9 percent enantiomeric purity, , as shown on Fig.4

The chemical industry reduces the impact on the environment during synthesis 147118-40-9, I believe this compound will play a more active role in future production and life.

Reference:
Patent; LEK Pharmaceuticals d.d.; EP2022784; (2009); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthetic Route of 147118-40-9 ,Some common heterocyclic compound, 147118-40-9, molecular formula is C23H30FN3O6S, 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.

Previous to give 62 g (0.125 mol) of crystalline product was added 860 ml of ethanol, 140 ml 1N-NaOH was stirred at 25 degrees for 1 hour. At 35-40 ° ethanol was removed by vacuum distillation, by 1 l methyl t-butyl ether and extracted twice. With an appropriate amount of the aqueous layer was filtered through Celite and activated carbon, with a small amount of water dissolved calcium acetate was added to the filtrate, stirred for 2 hours at 25 °, filtered washed with water, and dried to give 52.9 g (84.5percent theoretical yield) rosuvastatin statin calcium.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,147118-40-9, its application will become more common.

Reference:
Patent; Anhui Menovo Pharmaceuticals Co., Ltd; Fan, qijiao; Wang, bangfeng; Shi, jianxiang; (9 pag.)CN105461636; (2016); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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. 147118-40-9, name is Rosuvastatin methyl ester. A new synthetic method of this compound is introduced below., Recommanded Product: 147118-40-9

Example 663.0 g (6.0 mmol) of crystalline Form II rosuvastatin methylester are dissolved in 12 cm3 of methanol at 25 °C and while stirring, 5.9 cm3 of 1.0 M aqueous TBA solution are added at the same temperature. Thereafter five times in two-hour periods further 1.2 cm3 of 1.0 M aqueous TBA solution are added to the reaction mixture. The mixture is stirred for further 24 hours, evaporated and by adding 3 x40 cm3 eof ethylacetate, the residual water is removed by repeating azeotropic distillation three times. Into the residue thus obtained 34 cm of ethylacetate and 10 cm3 of distilled water are added. Subsequently 3.7 cm3 of 2.2 M aqueous ZnSO4 solution are added into the biphasic mixture in ten minutes at a temperature between 20 and 25 °C. After one hour stirring, the layers are separated, the organic layer is washed with 2x 10 cm of 2.2 M aqueous ZnSO4 solution and 10 cm of distilled water. The organic layer is evaporated and the remaining water is removed by repeated azeotropic distillation using ethylacetate. The suspension is cooled, filtered, washed with 3 cm of ethylacetate and dried in vacuo. Thus 2.50 g (81 percent) of crude product are obtained, which are stirred in the solutio of 1.2 mg of sodium hydroxide in 12 cm of distilled water in an argon atmosphere for 36 hours at a temperature between 0 and 5 °C. The mixture is filtered, washed with alkaline water having the same composition as described above and dried in vacuo protected from light. Thus 2.25 g (90 percent) of title product are obtained.

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, 147118-40-9, Rosuvastatin methyl ester.

Reference:
Patent; EGIS GYOGYSZERGYAR NYILVANOSAN M?KOeD? RESZVENYTARSASAG; KOVANYINE LAX, Gyoergyi; SIMIG, Gyula; VOLK, Balazs; BARTHA, Ferenc Lorant; KRASZNAI, Gyoergy; RUZSICS, Gyoergy; SIPOS, Eva; NAGY, Kalman; MOROVJAN, Gyoergy; BARKOCZY, Jozsef; KESZTHELYI, Adrienn; IMRE, Janos; BAGYINSZKI, Gabor; WO2012/73055; (2012); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 147118-40-9, 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. 147118-40-9, name is Rosuvastatin methyl ester, molecular formula is C23H30FN3O6S, The 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.

Example-5Preparation of Rosuvastatin Sodium Methyl 7-[4-(4-flourophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)- pyrimidin-5-yl]-(3R,5S)-dihydroxy -(E)–heptenate (100 g ) was added to ethyl alcohol (900 ml). To this aqueous sodium hydroxide (8.0 g sodium hydroxide dissolved in 500 ml of water) was added at a temperature of 0-5 °C. The reaction mixture was heated to room temperature and maintained for 1-2 hours. After completion of the reaction, the reaction mass was concentrated and ethyl alcohol was added and the reaction mass was distilled off azeotropically. To the obtained residue diisopropyl ether was added and stirred for lhour and filtered. The filtered solid was dried to yield Rosuvastatin sodium.

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 147118-40-9, Rosuvastatin methyl ester.

Reference:
Patent; MATRIX LABORATORIES LIMITED; WO2009/128091; (2009); A2;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application of 147118-40-9, Adding some certain compound to certain chemical reactions, such as: 147118-40-9, name is Rosuvastatin methyl ester,molecular formula is C23H30FN3O6S, 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 147118-40-9.

EXAMPLE 2; PREPARATION OF N,N’-DIBENZYLETHYLENEDIAMINEROSUVASTATIN SALT; Rosuvastatin methyl ester was (1 g) was dissolved in ethanol (15 ml) at 25-300C and cooled to 0-50C and treated with aqueous sodium hydroxide (0.1 N, 20 ml) at 0-50C. The temperature of the reaction mass was raised to 25-300C and stirred for 1 hr. Ethanol was evaporated from the reaction mass under reduced pressure at 40-450C and the resulting aqueous layer was diluted further with 15 ml of DM water. This aqueous layer containing rosuvastatin was washed with 30percent v/v ethyl acetate/toluene (50 ml) at 25-300C and treated with aqueous solution of N,N’- dibenzylethylenediamine diacetate (0.9 g in 5 ml). The resulting suspension was stirred for 1 hr for complete precipitation and the precipitated product was filtered, slurry washed with ethyl acetate (20 ml) and dried under vacuum at 40-450C. Dry wt. 0.68 g; Chromatographic purity (HPLC): 99.28percent, Anti isomer: 0.59percent.; EXAMPLE 3PREPARATION OF N,N’-DIBENZYLETHYLENEDIAMINEROSUVASTATINA solution of rosuvastatin methyl ester (5 g) in ethanol (70 ml) was treated with aqueous sodium hydroxide (0.1N, 88 ml) at 0-50C and the temperature of the reaction was raised to 300C and stirred for 1 h. Ethanol from the reaction mass was evaporated at 40-450C. This aqueous layer was washed with 30 v/v ethyl acetate/toluene (3 x 25 ml) and treated with an aqueous solution of N,N’-dibenzylethylenediamine diacetate(1.8 g in 10 ml water). The resulting mass was further stirred for a period of 2 h, filtered, slurry washed with ethyl acetate (30 ml) and dried under vacuum at 40-450C. Dry Wt. 3.3 g, Chromatographic purity: 99.48 percent, Anti isomer: 0.47percent.

According to the analysis of related databases, 147118-40-9, the application of this compound in the production field has become more and more popular.

Reference:
Patent; AUROBINDO PHARMA LIMITED; WO2008/38132; (2008); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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. 147118-40-9, name is Rosuvastatin methyl ester, molecular formula is C23H30FN3O6S, The 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. Application In Synthesis of Rosuvastatin methyl ester

In a round bottom flask 2000 ml Tetrahydrofuran (THF) was added under the nitrogen atmosphere and cooled to -90¡ãC then 1Og sodium borohydride was added followed by 230ml diethylmethoxyborane (1 M solution in THF) in 90-120mins. In this reaction mass, mixture of lOOg of Methyl -7-[4-(4-fiourophenyl)-6-isopropyl-2-(N-methyl-N- methylsulfonylaniino)-pyrimidin-5-yl]-(3R)-3-hydroxy-5-oxo-(E)-6-heptenate5 700 ml THF and 700 ml methanol was added for a duration of 90-120min then stirred for 2 hrs at -90 to -80¡ãC. After the completion of reaction, 124 ml acetic acid was added and stirred for 30-60 min at same temperature. Above reaction mass was diluted with 1500ml ethyl acetate and washed with brine solution. To the organic layer, 500 ml DM water was added and pH was adjusted to neutral by ~ 500 ml 6 percent sodium bicarbonate solution. Both the layers were separated Sc the organic layer was dried over sodium sulphate. The organic layer was concentrated at 40-450C. Above concentrated mass was diluted with 900ml ethyl alcohol and then cooled to 0¡ãC. Sodium hydroxide solution was added in 60- 90 min. The reaction mass was stirred for 30 min at room temperature and the pH was adjusted to 11.5-12.0 by using ~ 4 percent sodium hydroxide solution. In this reaction mass, 1Og activated carbon was added and stirred for 20 min. The reaction mass was filtered and washed with ethanol/DM water mixture. The reaction mass was concentrated up to thick residue at 40-45¡ãC. To this concentrated mass, 500 ml DM water was added followed by 1000ml ethyl acetate and the pH was adjusted to 3.5- 4.0 with 1:4 aqueous hydrochloric acid. Both the layers were separated and the organic layer was washed with brine solution.The organic layer was dried over sodium sulphate and concentrated till dryness at 40-45¡ãC. To the above concentrated mass, 1000 ml acetonitrile was added stirred at room temperature for half an hour. Slowly 20.5 g (S)-2-amino-3, 3 -dimethyl butane was added and stirred for almost 2 hrs. The solid was filtered and washed with acetonitrile and diisopropyl ether. Finally the solid was dried for 6-9 hrs at 40-45¡ãC.Above obtained (S)-2-amino-3, 3 -dimethyl butane salt of rosuvastatin was suspended in 1000 ml isopropanol followed by 100 ml methanol. This reaction mass was heated for half an hour at 60-80¡ãC then stirred for 3-4 hrs at 5-1O0C. The solid was filtered washed with isopropanol and diisopropyl ether. 95 gms of (S)-2-amino-3, 3 -dimethyl butane salt of rosuvastatin was obtained.

With the rapid development of chemical substances, we look forward to future research findings about 147118-40-9.

Reference:
Patent; MATRIX LABORATORIES LTD; SETHI, Madhuresh, Kumar; MAHAJAN, Sanjay; MARA, Bhairaiah; AYYARAN, Laxmi, Karthikeyan; DATTA, Debashish; WO2010/35284; (2010); A2;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adding a certain compound to certain chemical reactions, such as: 147118-40-9, Rosuvastatin methyl ester, 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, Recommanded Product: Rosuvastatin methyl ester, blongs to pyrimidines compound. Recommanded Product: Rosuvastatin methyl ester

Add 150 ml of acetonitrile to the 500 ml reaction flask and add 18.0 g of RSM. After completely dissolving, 40 ml of purified water was added and heated to 35 ¡ã C to 40 ¡ã C. 42 ml of 1N sodium hydroxide solution was added dropwise to control the dropping rate Keep the temperature between 35 ~ 40 , the entire drop process takes about 10 ~ 15min, continue to react and then need 2 to 2.5 hours.The reaction was completed at 40 ¡ã C to 50 ¡ã C under reduced pressure to remove the acetonitrile organic solvent and then 30 ml of purified water was added to open the jacketed cooling water to lower the temperature of the contents to 25 ¡ã C to 30 ¡ã C and washed with ether 3 times, each with ether 50 ml, each stirring 10 ~ 15min, static liquid separation, collecting water layer.Then add 3 g of activated carbon in the water layer, heating to maintain the temperature 35 ~ 40 , stirring 50 ~ 60min, filter, filter with 10 ml of purified water filter cake, combined filtrate and lotion, the filtrate was vacuum distillation RSA 19.0 g

At the same time, in my other blogs, there are other synthetic methods of this type of compound,147118-40-9, Rosuvastatin methyl ester, and friends who are interested can also refer to it.

Reference:
Patent; Nanjing Ouxin Pharmaceutical Technology Co., LTD; Chen, Ben Shun; Zhou, Zhang Yue; Chen, Kai; Qi, Chen Chen; (14 pag.)CN104230817; (2016); B;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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. 147118-40-9, name is Rosuvastatin methyl ester. A new synthetic method of this compound is introduced below., 147118-40-9

Example 4130.0 g (0.061 mol) of crystalline Form II rosuvastatin methylester are suspended in 150 cm3 of water with stirring at 25 ¡ãC. Into the suspension thus obtained, 61 cm of 1.0 M aqueous TBA solution are added. Thereafter in two hours periods, each time 12.2 cm3 of 1.0 M aqueous TBA solution added to the reaction mixture four times. After 16 hours reaction time, a further 12.2 cm3 portion of 1.0 M aqueous TBA solution are added and the reaction mixture is stirred for a further 24 hours. The product is filtered, washed with cold ethylacetate and dried. Thus 28.5 g (84 percent) of white product having purity (HPLC) of 99.98 percent are obtained.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,147118-40-9, Rosuvastatin methyl ester, and friends who are interested can also refer to it.

Reference:
Patent; EGIS GYOGYSZERGYAR NYILVANOSAN M?KOeD? RESZVENYTARSASAG; KOVANYINE LAX, Gyoergyi; SIMIG, Gyula; VOLK, Balazs; BARTHA, Ferenc Lorant; KRASZNAI, Gyoergy; RUZSICS, Gyoergy; SIPOS, Eva; NAGY, Kalman; MOROVJAN, Gyoergy; BARKOCZY, Jozsef; KESZTHELYI, Adrienn; IMRE, Janos; BAGYINSZKI, Gabor; WO2012/73055; (2012); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia