51699-40-2

Upstream product

• 105-36-2 ethyl bromoacetate 
• 587-04-2 m-Chlorobenzaldehyde 
• 141-78-6 ethyl acetate 
• 64-17-5 ethanol 
• 632327-19-6 methyl 3-(3-chlorophenyl)-3-oxopropanoate 
• 99-02-5 3'-Chloroacetophenone 
• 33167-21-4 3-(3-chloro-phenyl)-3-oxo-propionic acid ethyl ester 

Downstream Products

• 51699-45-7 (S)-(-)-1-(3'-Chlorophenyl)-1,3-Propanediol 
• 872354-90-0 [4-(3-chloro-phenyl)-[1,3,2]dioxaphosphinan-2-yl]-diisopropyl-amine 
• 852948-35-7 1-(3-Chloro-phenyl)-3-methyl-butane-1,3-diol 
• 804561-62-4 2',3'-di-O-tert-butyldimethylsilyl-5'-O-cis-[4-(S)-(3-chlorophenyl)-2-oxo-1,3,2-dioxaphoshorinan-2-yl]cytosine-1-β-D-arabinofuranoside 
• 804561-63-5 2',3'-di-O-tert-butyldimethylsilyl-5'-O-cis-[4-(R)-(3-chlorophenyl)-2-oxo-1,3,2-dioxaphosphorinan-2-yl]cytosine-1-β-D-arabinofuranoside 
• 693223-08-4 (4S)-(-)-trans-2-(4-nitrophenoxy)-2-oxo-4-(3-chlorophenyl)-1,3,2-dioxaphosphorinane 
• 805235-83-0 (4R)-(+)-trans-2-(4-nitrophenoxy)-2-oxo-4-(3-chlorophenyl)-1,3,2-dioxaphosphorinane 
• 804561-30-6 (2S,8R,11S)-2-(3-chlorophenyl)-8-methyl-11-(1-methylethyl)-1,5-dioxaspiro[5.5]undecane 
• 804561-32-8 (2R,8R,11S)-2-(3-chlorophenyl)-8-methyl-11-(1-methylethyl)-1,5-dioxaspiro[5.5]undecane 
• 51699-52-6 1-(3-chlorophenyl)-1-hydroxy-3-(p-toluenesulfonyloxy)propane 
• 804560-96-1 (+/-)-1-(1,3-bistrimethylsilyloxypropyl)-3-chlorobenzene 
• 625095-57-0 (S)-(-)-1-(3-Chlorophenyl)-1,3-propanediol 
• 632327-18-5 (R)-(+)-1-(3-chlorophenyl)-1,3-propanediol 
• 160388-09-0 1-(3-chlorophenyl)prop-2-en-1-one 

Relevant academic research and scientific papers

RADIO-AND CHEMO-PROTECTIVE COMPOUNDS

The present disclosure relates to prodrugs, double prodrugs, derivatives and analogues of 3-(methylamino)-2-((methylamino)methyl)propane-l-thiol. Their use as radio- and chemo-protectors is also described.

Preparation method of 3-(substituted/non-substituted phenyl)-3-hydroxy propionyl hydroxamic acid

The invention discloses a preparation method of 3-(substituted/non-substituted phenyl)-3-hydroxy propionyl hydroxamic acid. Diethyl carbonate and acetophenone or acetophenone derivatives thereof are used as starting raw materials; through three-step react

Umpolung of protons from H2O: A metal-free chemoselective reduction of carbonyl compounds: Via B2pin2/H2O systems

H2O is routinely described as a proton donor, however, in the presence of diboron compounds, the umpolung reaction of H2O under metal-free conditions was successfully developed, which could afford hydride species, leading to a highly efficient and chemoselective reduction of CO bonds. This strategy exhibits excellent chemoselectivities toward carbonyl groups in the presence of ester, olefin, halogen, thioether, sulfonyl, cyano as well as heteroaromatic groups.

3-Arylpropionylhydroxamic acid derivatives as Helicobacter pylori urease inhibitors: Synthesis, molecular docking and biological evaluation

Helicobacter pylori urease is involved in several physiologic responses such as stomach and duodenal ulcers, adenocarcinomas and stomach lymphomas. Thus, inhibition of urease is taken for a good chance to treat H. pylori-caused infections, we have therefore focused our efforts on seeking novel urease inhibitors. Here, a series of arylpropionylhydroxamic acids were synthesized and evaluated for urease inhibition. Out of these compounds, 3-(2-benzyloxy-5-chlorophenyl)-3-hydroxypropionylhydroxamic acid (d24) was the most active inhibitor with IC50of 0.15?±?0.05?μM, showing a mixed inhibition with both competitive and uncompetitive aspects. Non-linear fitting of kinetic data gives kinetics parameters of 0.13 and 0.12?μg·mL?1for Kiand Ki′, respectively. The plasma protein binding assays suggested that d24 exhibited moderate binding to human and rabbit plasma proteins.

Studies on the chemoenzymatic synthesis of (R)- and (S)-methyl 3-aryl-3-hydroxypropionates: The influence of toluene-pretreatment of lipase preparations on enantioselective transesterifications

Two series (para- and meta-substituted) of racemic methyl esters of 3-aryl-3-hydroxypropionic acid were prepared after which the enantiomers were separated by an enzyme-catalyzed transesterification. Several lipases were investigated as the catalyst. The influence of the enzyme pretreatment, as well as substrate concentration, reaction temperature, stirring manner, and substrate conversion on the stereochemical outcome of the biotransformation process were investigated in detail. The best results were achieved by using solvent-pretreated lipase from Pseudomonas fluorescens or Burkholderia cepacia suspended in toluene, and vinyl acetate as the acetyl group donor.

Synthesis, molecular docking and kinetic properties of β-hydroxy- β-phenylpropionyl-hydroxamic acids as Helicobacter pylori urease inhibitors

Inhibition of urease results in Helicobacter pylori growth arrest in the stomach, promoting urease as promising targets for gastrointestinal ulcer therapy. Twenty hybrid derivatives of flavonoid scaffold and hydroxamic acid, β-hydroxy-β-phenylpropionylhydroxamic acids, were therefore synthesized and evaluated against H. pylori urease. Biological evaluation of these compounds showed improved urease inhibition exhibiting micromolar to mid-nanomolar IC50 values. Most importantly, 3-(3-chlorophenyl)-3- hydroxypropionyl-hydroxamic acid (6g) exhibited high potency with IC 50 of 0.083 ± 0.004 μM and Ki of 0.014 ± 0.003 μM, indicating that 6g is an excellent candidate to develop novel antiulcer agent. A mixture of competitive and uncompetitive mechanism was putatively proposed to understand the inconsistency between the crystallographic and kinetic studies for the first time, which is supported by our molecular docking studies.

Novel Phosphinic Acid-Containing Thyromimetics

The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome x and diabetes.

Pradefovir: A prodrug that targets adefovir to the liver for the treatment of hepatitis B

Adefovir dipivoxil, a marketed drug for the treatment of hepatitis B, is dosed at submaximally efficacious doses because of renal toxicity. In an effort to improve the therapeutic index of adefovir, 1-aryl-1,3-propanyl prodrugs were synthesized with the r

Synthesis and characterization of a novel liver-targeted prodrug of cytosine-1-β-D-arabinofuranoside monophosphate for the treatment of hepatocellular carcinoma

Cytotoxic nucleosides have proven to be ineffective for the treatment of hepatocellular carcinoma (HCC) due, in part, to their inadequate conversion to their active nucleoside triphosphates (NTP) in the liver tumor and high conversion in other tissues. Th

NOVEL PHOSPHORUS-CONTAINING THYROMIMETICS

The present invention relates to compounds of phosphonic acid containing T3 mimetics, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndromex and diabetes.