13422-80-5

Upstream product

• 2754-27-0 trimethylsilyl acetate 
• 618-46-2 m-Chlorobenzoyl chloride 
• 21667-62-9 3-chlorobenzoylacetonitrile 
• 117855-94-4 bis(trimethylsilyl)malonate 
• 124-38-9 carbon dioxide 
• 99-02-5 3'-Chloroacetophenone 

Downstream Products

• 625095-56-9 (S)-(-)-(3-chlorophenyl)-3-hydroxypropionic acid 
• 1392149-64-2 (3R)-tert-butyl 3-(2-(3-chlorophenyl)-2-oxoethyl)-3-hydroxy-2-oxo-2,3-dihydro-1H-indoline-1-carboxylate 
• 1459140-99-8 C₂₃H₁₈ClNO₃ 
• 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 
• 693223-03-9 (+)-cis-5'-O-[4-(S)-(3-chlorophenyl)-2-oxo-1,3,2-dioxaphosphorinan-2-yl]cytosine-1-β-D-arabinofuranoside 
• 625095-60-5 (+)-cis-9-{2-[4-(S)-(3-chlorophenyl)-2-oxo-1,3,2-dioxaphosphorinan-2-methyleneoxy]eth-1-yl}adenine 
• 693223-08-4 (4S)-(-)-trans-2-(4-nitrophenoxy)-2-oxo-4-(3-chlorophenyl)-1,3,2-dioxaphosphorinane 
• 625095-57-0 (S)-(-)-1-(3-Chlorophenyl)-1,3-propanediol 

Relevant academic research and scientific papers

Characterization of a new nitrilase from Hoeflea phototrophica DFL-43 for a two-step one-pot synthesis of (S)-β-amino acids

A nitrilase from Hoeflea phototrophica DFL-43 (HpN) demonstrating excellent catalytic activity towards benzoylacetonitrile was identified from a nitrilase tool-box, which was developed previously in our laboratory for (R)-o-chloromandelic acid synthesis from o-chloromandelonitrile. The HpN was overexpressed in Escherichia coli BL21 (DE3), purified to homogeneity by nickel column affinity chromatography, and its biochemical properties were studied. The HpN was very stable at 30–40?°C, and highly active over a wide range of pH values (pH 6.0–10.0). In addition, the HpN could tolerate against several hydrophilic organic solvents. Steady-state kinetics indicated that HpN was highly active towards benzoylacetonitrile, giving a KM of 4.2?mM and a kcat of 170?s?1, the latter of which is ca. fivefold higher than the highest record reported so far. A cascade reaction for the synthesis of optically pure (S)-β-phenylalanine from benzoylacetonitrile was developed by coupling HpN with an ω-transaminase from Polaromonas sp. JS666 in toluene-water biphasic reaction system using β-alanine as an amino donor. Various (S)-β-amino acids could be produced from benzoylacetonitrile derivatives with moderate to high conversions (73–99%) and excellent enantioselectivity (> 99% ee). These results are significantly advantageous over previous studies, indicating a great potential of this cascade reaction for the practical synthesis of (S)-β-phenylalanine in the future.

NOVEL 2'-C-METHYL AND 4'-C-METHYL NUCLEOSIDE DERIVATIVES

Novel 2'-C-methyl nucleoside 5 '-monophosphate and 4'-C-methyl nucleoside 5'- monophosphate derivatives, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral inf

LEWIS ACID MEDIATED SYNTHESIS OF CYCLIC ESTERS

Methods for the synthesis of cyclic phosphonic acid diesters from 1,3-diols are described, whereby cyclic phosphonic acid diesters are produced by reacting a chiral 1,3-diol and an activated phosphonic acid in the presence of a Lewis acid.

Novel 2'-C-methyl nucleoside derivatives

Compounds of Formula I, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral infection are described:

Design, Synthesis, and Characterization of a Series of Cytochrome P 450 3A-Activated Prodrugs (HepDirect Prodrugs) Useful for Targeting Phosph(on)ate-Based Drugs to the Liver

A new class of phosphate and phosphonate prodrugs, called HepDirect prodrugs, is described that combines properties of rapid liver cleavage with high plasma and tissue stability to achieve increased drug levels in the liver. The prodrugs are substituted c

Glutamate receptor antagonists

The present invention is a compound of formula wherein X is an ethynediyl group, R1, R2and R3are as defined in the specification.

Process for preparation of cyclic prodrugs of PMEA and PMPA

The method of preparing compounds of Formula I is described: wherein: M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, and (R)-9-(2-phosphonylmethoxypropyl)adenine; wherein V is phenyl, optionally substituted with 1-2 substituents selected from a group consisting of fluoro, chloro, and bromo; comprising: coupling a chiral 1-phenylpropane-1,3-diol, wherein the phenyl may be optionally substituted, with MPOCl2 or an N-6 substituted analogue thereof. Additionally, methods and salt forms are described that enable isolation and purification of the desired isomer.

Novel phosphonic acid based prodrugs of PMEA and its analogues

Prodrugs of Formula I, their uses, their intermediates, and their method of manufacture are described: 1wherein: M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmet

Glutamate receptor antagonists

The present invention relates to compounds of with a base structure of formula 1 The compounds of formula I are shown to have activity as metabotropic glutamate receptor antagonists.