Tag: M.W:300-400

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 875444-08-9, molcular formula is C12H9F6NO2, introducing its new discovery. , 875444-08-9

SYNTHESIS OF INTERMEDIATES FOR PREPARING ANACETRAPIB AND DERIVATIVES THEREOF

The present invention relates to the field of organic chemistry, more specifically to the synthesis of intermediate compounds which can be used in the synthesis of pharmaceutically active agents such as anacetrapib or derivatives thereof.

Because enzymes can increase reaction rates by enormous factors and tend to be very specific, 875444-08-9, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 875444-08-9

Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H2765NO – PubChem

 

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 875444-08-9, molcular formula is C12H9F6NO2, introducing its new discovery. , 875444-08-9

CETP INHIBITORS

Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B or R2 is a phenyl group which has an ortho amine or aminomethyl substituent which is further substituted, and the other of B or R2 is also a cyclic group.

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, 875444-08-9, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 875444-08-9

Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H2758NO – PubChem

 

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 1676-86-4, Name is (S)-Benzyl (4-(2,5-dioxooxazolidin-4-yl)butyl)carbamate. In a document type is Article, introducing its new discovery., 1676-86-4

A head-to-head comparison of poly(sarcosine) and poly(ethylene glycol) in peptidic, amphiphilic block copolymers

In this work we compare chemical and solution properties, like critical aggregate concentrations (CAC) and hydrodynamic radii of aggregates based on either poly(ethylene glycol) or poly(sarcosine) block copolymers in aqueous solution. The amine functionalized, hydrophilic polymers poly(sarcosine) (degree of polymerization, Xn = 100 and 200) and PEG (Xn = 121 and 242) of comparable hydrodynamic volume were used to initiate the ring opening polymerization of alpha-amino acid-N-carboxyanhydrides based on epsilon-benzyl-l-glutamate (Glu(OBn)) or epsilon-carboxybenzyl-l-lysine (Lys(Z)). The second, hydrophobic block was kept at a degree of polymerization of 25 and 50 to enable a direct comparison of solution properties of block copolymers. In both cases block length could be precisely adjusted and all synthesized block copolymers have narrow molecular weight distributions and dispersities between 1.1 and 1.2. Both types of block copolymers display critical aggregate concentrations in the range of 6?10-8-3?10-7 mol/L and aggregates possess hydrodynamic radii in a range of 40-100 nm. PEG based systems, however, have a slightly lower CAC and tend to form smaller micelles, while PSar based systems have commonly smaller mu2 parameter indication more uniform aggregates.

If you¡¯re interested in learning more about 38028-67-0, below is a message from the blog Manager. 1676-86-4

Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H2716NO – PubChem

 

1676-86-4, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 1676-86-4, molcular formula is C15H18N2O5, introducing its new discovery.

A charge conversion nano medicament carrier and its preparation method (by machine translation)

The invention is applicable to the field of medical technology, provides a charge conversion nano medicament carrier and its preparation method. The charge conversion nano medicament carrier comprises a core and of which the, the kernel as a carrier body, the carrier body is outside states the nucleus to the conversion of the electric charge carrier lock, the kernel with the role of the through positive and negative charge of which the combination; said carrier body which is a positive targeting peptide modified polyethylene glycol – hydrophobic modified chitosan; the side chain modified carrier lock is 2, 3 – dimethyl maleic acid of a polylysine. The present invention provides a charge conversion nano medicament carrier with double-charge conversion, this kind of charge conversion nano medicament carrier surface with negative charge, under weak acid environment, carrier lock is opened, the carrier charge inversion occurs, by the negative charge is converted into a positive charge, targeting leakage in the micelle surface, begin to play a role in targeting, overcome the blood-brain barrier. (by machine translation)

Because enzymes can increase reaction rates by enormous factors and tend to be very specific, 1676-86-4, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 1676-86-4

Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H2688NO – PubChem

 

875444-08-9, The molecularity of an elementary reaction is the number of molecules that collide during that step in the mechanism. If there is only a single reactant molecule in an elementary reaction, that step is designated as unimolecular. 875444-08-9, name is (4S,5R)-5-(3,5-Bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one. A new synthetic method of this compound is introduced below.

The chiral intermediate (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one (compound of formula XV; cf. also compound 11 in Scheme 3) (280 mg) prepared by procedure of WO 2007/005572 is dissolved in DMF (30 mL) and cooled to -15C. 2 M NaHMDS (3.90 mL, 1.05 eq) was then added over 1 h, followed by addition of the biaryl chloride EBFCI (270 mg) in DMF (5 mL), maintaining the internal temperature below-10 C. The mixture was warmed to +12 C and was aged until complete conversion took place. Then 5M HCl (3.5 mL) was added, followed by 20 mL of 10% IPAC/Heptanes and 40 mL of water, keeping the temperature between 10C and 20C throughout. The layers were cut and the organic layer was washed twice with 20 mL of 1/1 DMF/water followed by two 15 mL water washes. The organic layer was then removed under reduced pressure and the resulting residue was purified by flash chromatography (EtOActhexanes) to remove the excess oxazolidinone (compound of formula XV). The pure (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-3-((5′-ethyl-4′-fluoro-2′-methoxy-4-(trifluoromethyl)biphenyl-2-yl)methyl)-4-methyloxazolidin-2-one (DMAP, compound of formula XII”) was obtained as a colorless oil (388 mg, 80%).

Any one of these steps may be slow and thus may serve as the rate determining step. In general, however, in the presence of the catalyst, the overall rate of the reaction is faster than it would be if the reactants were in the gas or liquid phase.

Reference£º
Patent; LEK Pharmaceuticals d.d.; EP2468736; (2012); A1;,
Oxazolidine – Wikipedia
Oxazolidine | C3H7NO – PubChem

 

One of the major reasons is to use measurements of the macroscopic properties of a system, the rate of change in the concentration of reactants or products with time, to discover the sequence of events that occur at the molecular level. 875444-08-9, introduce a new downstream synthesis route., 875444-08-9

875444-08-9, [2-{[2-(t-butyldimethylsiloxy)ethyl](tetrahydro-2H-pyran-4-yl)amino}-5- (trifIuorornethyl)pyridin-3-yl]methyl methanesulfonate of step 2 and (4S,5f?)-5-[3,5- bis(trifluoromethyl)phenyl])-4-methyl-oxazolidin-2-one were used in the same manner as in step 4 of Example 3 to afford the title compound (55mg, 63%). 1H NMR (400MHz, CDCI3) 8.46 (s, 1H), 7.88 (s, 1 H), 7.77 (s, 1H), 7.73 (s, 2H), 5.72 (d, J = 8.0Hz, 1H), 4.75 (d, J = 16.0Hz, 1 H), 4.33 (d, J = 16.0Hz, 1H), 4.04-3.87 (m, 3H), 3.67 (m, 1 H), 3.50 (m, 2H), 3.38-3.17 (m, 6H), 1.91-1.72 (m, 4H), 0.78 (s, 9H), 0.61 (d, 3H), -0.03 (d, 3H).

This molecular description is the mechanism of the reaction; it describes how individual atoms, ions, or molecules interact to form particular products.If you are interested, you can also browse other articles of 875444-08-9. We look forward to the emergence of more reaction modes in the future. 875444-08-9

Reference£º
Patent; DONG-A ST CO.,LTD; PARK, Jang Hyun; SONG, Seung Hyun; CHUNG, Han Kook; KIM, Heung Jae; LEE, Ji Hye; JANG, Byeong Jun; KIM, Eun Jung; JUNG, Hae Hum; RYU, Chae Lim; HWANG, Jae-Sung; LEE, Hyung Ki; KANG, Kyung Koo; KIM, Soon Hoe; WO2014/157994; (2014); A1;,
Oxazolidine – Wikipedia
Oxazolidine | C3H7NO – PubChem

 

We know that the rate of many reactions can be accelerated by catalysts. A catalyst speeds up the rate of a reaction by lowering the activation energy; in addition, the catalyst is regenerated in the process. 875444-08-9, name is (4S,5R)-5-(3,5-Bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one,below Introduce a new synthetic route., 875444-08-9

875444-08-9, The chiral intermediate (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one (compound of formula XV; cf. also compound 11 in Scheme 3) (28.0 g) prepared by the procedure of WO 2007/005572 is dissolved in DMF (300 mL) and cooled to -15C. 2 M NaHMDS (39.2 mL, 1.05 eq) was then added over 1 h, followed by addition of the blaryl chloride 7 (Scheme 3) (28.0 g) in DMF (50 mL), maintaining the internal temperature below-10 C. The mixture was warmed to + 12 C and was aged until complete conversion took place. Then 5M HCl (35 mL) was added, followed by 160 mL of 10% IPAC/Heptanes and 340 mL of water, keeping the temperature between 10C and 20C throughout. The layers were cut and the organic layer was washed twice with 150 mL of 1/1 DMF/water followed by two 140 mL water washes. The organic layer was then removed under reduced pressure and the resulting residue was purified by flash chromatography (EtOAclhexanes) to remove the excess oxazolidinone 11 (Scheme 3). The obtained colorless oil was then dissolved in refluxing heptanes (200 mL) and the solution was slowly cooled to -20 C. The resulting slurry was then stirred at -20 C for 2 hours and filtered. The filter cake was washed with cold heptanes and was then dried, yielding 44.0 g (88%) of the desired product of compound of formula XV” (anacetrapib) as an amorphous material. An impurity of compound of formula XVII” (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-3-((5′-ethyl-4′-fluoro-2′-methoxy-4-(triftuoromethyl) biphenyl-2-yl)methyl-4-methyloxazolidin-2-one (DMAP) is present in the thus obtained anacetrapib in an amount of about 3 % by weight relative to the total amount of anacetrapib product. DMAP originates from 2′-(chloromethyl)-5-ethyl-4-fluoro-2-mothoxy-4′-trifluoromethyl)biphenyl (EBFCI) representing an impurity which forms in the preparation path of 2′-(chloromethyl)-4-fluoro-5-isopropyl-2-methoxy-4′-(trifluoromethyl)biphenyl under the above described conditions.

Other significant industrial processes that involve the use of heterogeneous catalysts include the preparation of sulfuric acid, the preparation of ammonia, the oxidation of ammonia to nitric acid, and the synthesis of methanol. 875444-08-9, if you are interested, you can browse my other articles.

Reference£º
Patent; LEK Pharmaceuticals d.d.; EP2468736; (2012); A1;,
Oxazolidine – Wikipedia
Oxazolidine | C3H7NO – PubChem

 

875444-08-9, We know that the rate of many reactions can be accelerated by catalysts. A catalyst speeds up the rate of a reaction by lowering the activation energy; in addition, the catalyst is regenerated in the process. 875444-08-9, name is (4S,5R)-5-(3,5-Bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one,below Introduce a new synthetic route.

875444-08-9, To a solution of (45′,5J?)-5-[3}5-bis(trifluoromethyl)phenyl]-4-methyl-li3-oxazoIidin-2-one (4.94 g, 15.77 mmol) in THF (75 mL) was added NaH (60% dispersion in mineral oil) (0.526 g, 13.14 mmol). After stirring the reaction at room temperature for 10 minutes, 3-bromo-2- (bromomethyl)-6-chloropyridine (3.0 g, 10.51 mmol) was added as a solution in THF (20 mL). The reaction was stirred at room temperature for 16 hours and then quenched with saturated NH4CI (40 mL). The mixture was diluted with EtOAc (100 mL) and hexanes (50 mL). The organic layer was washed with water (2 x 100 mL) and brine (50 mL), dried over Na2S0 , filtered, and concentrated. Purification of the residue by flash chromatography on silica gel with 0 to 50% EtOAc/hexanes afforded (4555^)-5-[3,5-bis(trifiuoromethyl)phenyl]-3-t(3-bromo-6- chloropyridin-2-yl)methyl]-4-methyl-1,3-oxazolidin-2-one. LCMS = 518.8 (M+H)+ 1H MR (CD<, 500 MHz) delta 7.90 (s, 1H), 7.81-7.83 (m, 3H), 7.18 (d, J- 8.5 Hz, 1H), 5.87 (d, J- 8.5 Hz, 1H), 5.02 (d, J= 17.2 Hz, 1H)5 4.42 (m, IE), 4.32 (d, J= 17.1 Hz, 1H), 0.80 (d, J= 6.6 Hz, 3H). Other significant industrial processes that involve the use of heterogeneous catalysts include the preparation of sulfuric acid, the preparation of ammonia, the oxidation of ammonia to nitric acid, and the synthesis of methanol. 875444-08-9, if you are interested, you can browse my other articles. Reference£º
Patent; MERCK SHARP & DOHME CORP.; LU, Zhijian; CHEN, Yi-Heng; SMITH, Cameron; LI, Hong; THOMPSON, Christopher, F.; SWEIS, Ramzi; SINCLAIR, Peter; KALLASHI, Florida; HUNT, Julianne; ADAMSON, Samantha, E.; DONG, Guizhen; ONDEYKA, Debra, L.; QIAN, Xiaoxia; SUN, Wanying; VACHAL, Petr; ZHAO, Kake; WO2012/58187; (2012); A1;,
Oxazolidine – Wikipedia
Oxazolidine | C3H7NO – PubChem

 

875444-08-9, One of the major reasons is to use measurements of the macroscopic properties of a system, the rate of change in the concentration of reactants or products with time, to discover the sequence of events that occur at the molecular level. 875444-08-9, introduce a new downstream synthesis route.

875444-08-9, Synthesis of (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-3-((4′-fluoro-5′-isopropyl-2′-methoxy-4-(trifluoromethyl)biphenyl-2-yl)d2-methyl)-4-methyl-1,3-oxazolidin-2-one (Compound 176). A solution of 18a (495 mg) in DMF (6 mL) was cooled to -20 C. and a 1M solution of NaHMDS in THF (1.7 mL) was added slowly at <-15 C. Five minutes after the addition was complete, a solution of 17b (480 mg) in DMF (3.5 mL) was added dropwise, keeping the temperature at <-15 C. The reaction was allowed to warm slowly to 16 C. over 2 hr, and stirred for an additional 2 hr. The reaction mixture was diluted with MTBE (200 mL), washed with water (10 mL*2), dilute HCl, then brine, dried (Na2SO4), filtered and the solvent concentrated under reduced pressure to give crude Compound 176. MS m/z=640 (M=H), 662 (M+Na). There are, however, a few established termolecular elementary reactions. The reaction of nitric oxide with oxygen appears to involve termolecular steps. you can also browse my other articles about875444-08-9 Reference£º
Patent; CONCERT PHARMCEUTICALS, INC.; US2008/242711; (2008); A1;,
Oxazolidine – Wikipedia
Oxazolidine | C3H7NO – PubChem

 

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.875444-08-9,(4S,5R)-5-(3,5-Bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one,as a common compound, the synthetic route is as follows.

875444-08-9, To a solution of (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyloxazolidin-2-one (1.84g, 5.89mmol) in DMF (10ml) was dropwise added NaHMDS (5.4ml, 5.4mmol) at – 40C. After being stirred for 30 min, the reaction mixture was slowly added with drops of a dilution of 2-chloro-3-(chloromethyl)pyrazine, obtained in step 2, in DMF (10ml). The resulting reaction mixture was warmed to room temperature, stirred for 3 hrs, diluted with ethyl acetate (200ml), and quenched with water (200ml). The organic layer was washed with water, dried over anhydrous magnesium sulfate, filtered, and concentrated in a vacuum. The residue was purified by chromatography to afford the title compound (900mg, 35%). H NMR (400MHz, CDCI3) 8.51 (d, 1 H), 8.36 (d, 1 H), 7.90 (s, 1 H), 7.83 (s, 2H), 5.85 (d, 1 H), 5.05 (d, 1 H), 4.50 (d, 1 H), 4.45 (m, 1 H), 0.81 (d, 3H).

The synthetic route of 875444-08-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DONG-A ST CO.,LTD; PARK, Jang Hyun; SONG, Seung Hyun; CHUNG, Han Kook; KIM, Heung Jae; LEE, Ji Hye; JANG, Byeong Jun; KIM, Eun Jung; JUNG, Hae Hum; RYU, Chae Lim; HWANG, Jae-Sung; LEE, Hyung Ki; KANG, Kyung Koo; KIM, Soon Hoe; WO2014/157994; (2014); A1;,
Oxazolidine – Wikipedia
Oxazolidine | C3H7NO – PubChem