28845-94-5

Upstream product

• 51545-26-7 3-chloro-2-phenyl-propionic acid 
• 51-55-8 atropine 
• 27150-91-0 α-phenyl-β-propiolactone 
• 537-29-1 norhyoscyamine 
• 7647-01-0 hydrogenchloride 
• 51-55-8 Atropine 
• 7732-18-5 water 
• 64-17-5 ethanol 
• 7722-84-1 dihydrogen peroxide 
• 5441-68-9 α-phenyl-β-bromopropionic acid 
• 4370-95-0 3-amino-2-phenyl-propionic acid 
• 99155-35-8 2-chloro-3-hydroxy-2-phenyl-propionic acid 
• 492-38-6 2-phenylacrylic acid 
• 100-42-5 styrene 

Downstream Products

• 51545-26-7 3-chloro-2-phenyl-propionic acid 
• 3967-53-1 methyl tropate 
• 51-55-8 atropine 
• 856815-60-6 1-acetylamino-3-phenyl-propane-1,1,3-tricarboxylic acid triethyl ester 
• 20913-74-0 2-amino-4-phenylpentanedioic acid 
• 56038-03-0 3-bromo-2-phenyl-propionic acid ethyl ester 
• 855243-42-4 3-methyl-2-phenyl-butane-1,3-diol 
• 4842-45-9 1,2,3-triphenylpropan-1-one 
• 1528-39-8 3-phenyl-2-pentanone 
• 183245-64-9 3-allyl-3-phenyloxetan-2-one 

Relevant academic research and scientific papers

Preparative Enantioseparation of β-Substituted-2-Phenylpropionic Acids by Countercurrent Chromatography with Substituted β-Cyclodextrin as Chiral Selectors

Preparative enantioseparation of four β-substituted-2-phenylpropionic acids was performed by countercurrent chromatography with substituted β-cyclodextrin as chiral selectors. The two-phase solvent system was composed of n-hexane-ethyl acetate-0.10olL-1 of phosphate buffer solution at pH2.67 containing 0.10olL-1 of hydroxypropyl-β-cyclodextrin (HP-β-CD) or sulfobutylether-β-cyclodextrin (SBE-β-CD). The influence factors, including the type of substituted β-cyclodextrin, composition of organic phase, concentration of chiral selector, pH value of the aqueous phase, and equilibrium temperature were optimized by enantioselective liquid-liquid extraction. Under the optimum separation conditions, 100g of 2-phenylbutyric acid, 100g of tropic acid, and 50g of 2,3-diphenylpropionic acid were successfully enantioseparated by high-speed countercurrent chromatography, and the recovery of the (±)-enantiomers was in the range of 90-91% for (±)-2-phenylbutyric acid, 91-92% for (±)-tropic acid, 85-87% for (±)-2,3-diphenylpropionic acid with purity of over 97%, 96%, and 98%, respectively. The formation of 1:1 stoichiometric inclusion complex of β-substituted-2-phenylpropionic acids with HP-β-CD was determined by UV spectrophotometry and the inclusion constants were calculated by a modified Benesi-Hildebrand equation. The results showed that different enantioselectivities among different racemates were mainly caused by different enantiorecognition between each enantiomer and HP-β-CD, while it might be partially caused by different inclusion capacity between racemic solutes and HP-β-CD.

PYRROLIDINE-PYRAZOLES AS PYRUVATE KINASE ACTIVATORS

The subject matter described herein is directed to pyruvate kinase activating compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for the treatment of diseases associated with PKR and/or PKM2, such as pyruvate kinase deficiency, sickle cell disease, and beta-thalassemia.

Synthesis method of 3-hydroxy-2-phenylpropionic acid

The invention discloses a synthetic method of 3-hydroxyl-2-phenylpropionic acid. The method comprises the following steps: mixing dimethyl sulfoxide, paraformaldehyde, potassium carbonate powder and methyl phenylacetate, heating to 85-95 DEG C, carrying out gas phase monitoring reaction, and cooling to room temperature when the GC content of the product methyl tropine is more than or equal to 70%;adjusting the pH value to be neutral, and performing reduced pressure distillation for desolvation; then adding methanol into the desolventized mixture, dropwise adding a sodium hydroxide solution, and reacting to obtain a mixed solution containing sodium tropine salt; adjusting the pH value of the mixed solution to 2-3, and completely reacting to obtain a crude product; and finally, recrystallizing the crude product sequentially by using methylbenzene of which the ratio of m product to m methylbenzene is 1: (4-6), methylbenzene/water of which the ratio of m product to m methylbenzene to m water is 1: (1-2): (4-6), and water of which the ratio of m product to m water is 1: (4-6) to obtain a pure product of 3-hydroxyl-2-phenylpropionic acid. According to the method, GC is adopted to monitor the reaction, control points are judged quickly and accurately, purification of methyl tropinate is not needed, operation procedures are reduced, and production cost is reduced. According to the method, the purity of the prepared 3-hydroxyl-2-phenylpropionic acid reaches 99% or above while the yield is ensured to reach 76.5% or above.

PYRROLOPYRROLE COMPOSITIONS AS PYRUVATE KINASE (PKR) ACTIVATORS

The disclosure relates to modulating pyruvate kinase and provides novel chemical compounds of formula (I) useful as activators of PKR, as well as various uses of these compounds. PKR activating compounds are useful in the treatment of diseases and disorders associated with PKR and/or PKM2, such as pyruvate kinase deficiency (PKD), sickle cell disease (SCD), and thalassemia.

SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS

Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.

Regioselective Copper-Catalyzed Boracarboxylation of Vinyl Arenes

Regioselective copper-catalyzed boracarboxylation of vinyl arenes with bis(pinacolato)diboron and carbon dioxide has been achieved. New boron-functionalized α-aryl carboxylic acids, including nonsteroidal anti-inflammatory drugs (NSAIDs), are obtained in moderate to excellent yields. The synthetic utility of the transformation was shown through subsequent derivatization of the carbon-boron bond yielding formal hydroxy- and fluorocarboxylation products as well as anionic difluoroboralactones.

Gold(I)/copper(II)-cocatalyzed tandem cyclization/semipinacol reaction: Construction of 6-Aza/Oxa-Spiro[4.5]decane skeletons and formal synthesis of (±)-halichlorine

A simple and efficient strategy for the construction of 6-aza/oxa-spiro[4.5]decane skeletons under the cocatalysis of gold(I)/copper(II) was developed, and its potential utility was demonstrated by a formal synthesis of the biologically active marine alkaloid (±)-halichlorine.

Enantioseparation of typical pesticides using cellulose carbamate stationary phases by capillary liquid chromatography

Cellulose-tris(3,5-dimethylphenylcarbamate) was initially synthesized as the chiral selector, then stable coated and bonded chiral stationary phases were prepared, respectively, using aminopropyl-functionalized silica gel as the support media. The prepared stationary phases were used for micro-column chiral separation by self-installed capillary high performance liquid chromatography system. Eighteen kind of chiral compounds including some typical pesticides were tested on both prepared chiral stationary phases and different chromatographic parameters such as resolution and retention time were comparatively investigated.

High-performance liquid chromatography separation of enantiomers of mandelic acid and its analogs on a chiral stationary phase

The enantiomers of mandelic acid and its analogs have been chromatographically separated on a chiral stationary phase (CSP) derived from 4-(3,5-dinitrobenzamido) tetrahydrophenanthrene. The rationale of separations of these compounds is discussed with respect to the method development for determining enantiomeric purity and possibility of obtaining enantiomerically pure materials by high-pressure liquid chromatography. The relationship of analyte structure to the extent of enantiomeric separation has been examined and separation factors (a) are presented for various groups of structurally related compounds. Chiral recognition models have been suggested to account for the observed separations. These models provide mechanistic insights into the chiral recognition process.

Selective reductions of cyclic 1,3-diesters by using SmI2 and H2O

SmI2/H2O reduces cyclic 1,3-diesters to 3-hydroxyacids with no over reduction. Furthermore, the reagent system is selective for cyclic 1,3-diesters over acyclic 1,3-diesters, and esters. Radicals formed by one-electron reduction of the ester carbonyl group have been exploited in intramolecular additions to alkenes. The ketal unit and the reaction temperature have a marked impact on the diastereoselectivity of the cyclizations. Cyclization cascades are possible when two alkenes are present in the starting cyclic diester and lead to the formation of two rings and four stereocenters with excellent stereocontrol.