21165-13-9

Upstream product

• 5418-86-0 tris(methylthio)methane 
• 6630-33-7 ortho-bromobenzaldehyde 
• 67-56-1 methanol 
• 7157-15-5 2-bromomandelic acid 
• 18107-18-1 diazomethyl-trimethyl-silane 
• 264882-02-2 2-bromophenyldiazoacetic acid methyl ester 
• 57486-69-8 methyl 2-(2-bromophenyl)acetate 
• 52923-21-4 2-(2-bromophenyl)-2-hydroxyacetonitrile 
• 2142-69-0 2-bromophenyl methyl ketone 
• 70-11-1 α-bromoacetophenone 

Downstream Products

• 43063-97-4 methyl 2-bromo-2-(2-bromophenyl) acetate 
• 181040-14-2 methyl (RS)-(2-bromophenyl)-[2-cyano-5-(thien-3-ylmethoxy)phenoxy]acetate 
• 1021539-52-5 methyl (2-(((4aS,5R)-1-(4-fluorophenyl)-5-hydroxy-4a-methyl-1,4,4a,5,6,7-hexahydrocyclopenta[f]indazol-5-yl)ethynyl)phenyl)hydroxyacetate 
• 1402890-71-4 2-(tert-butoxy)-2-[2-(3,4-dihydro-2H-1-benzopyran-6-yl)phenyl]acetic acid 
• 1402890-79-2 methyl 2-(tert-butoxy)-2-[2-(3,4-dihydro-2H-1-benzopyran-6-yl)phenyl]acetate 
• 1402890-78-1 methyl 2-(2-bromophenyl)-2-(tert-butoxy)acetate 
• 1299474-28-4 methyl {2-[((4aR,5R)-4a-cyclopropyl-1-(4-fluorophenyl)-5-hydroxy-1,4,4a,5,6,7-hexahydrocyclopenta[f]indazol-5-yl)ethynyl]phenyl}(hydroxy)acetate 
• 1299473-04-3 (2S)-{2-[((4aR,5R)-4a-cyclopropyl-1-(4-fluorophenyl)-5-hydroxy-1,4,4a,5,6,7-hexahydrocyclopenta[f]indazol-5-yl)ethyl]phenyl}hydroxyethanamide 
• 1299473-03-2 (2S)-{2-[((4aR,5R)-4a-cyclopropyl-1-(4-fluorophenyl)-5-hydroxy-1,4,4a,5,6,7-hexahydrocyclopenta[f]indazol-5-yl)ethyl]phenyl}hydroxyethanamide 
• 1299474-30-8 {2-[((4aR,5R)-4a-cyclopropyl-1-(4-fluorophenyl)-5-hydroxy-1,4,4a,5,6,7-hexahydrocyclopenta[f]indazol-5-yl)ethyl]phenyl}(hydroxy)acetic acid 
• 1299474-29-5 methyl {2-[((4aR,5R)-4a-cyclopropyl-1-(4-fluorophenyl)-5-hydroxy-1,4,4a,5,6,7-hexahydrocyclopenta[f]indazol-5-yl)ethyl]phenyl}(hydroxy)acetate 
• 122394-38-1 (2-bromophenyl)-oxoacetic acid methyl ester 
• 122283-38-9 (E)-2-(2-Bromo-phenyl)-3-methoxy-acrylic acid methyl ester 

Relevant academic research and scientific papers

(HETERO)ARYL-METHYL-THIO-BETA-D-GALACTOPYRANOSIDE DERIVATIVES

The present invention relates to compounds of Formula (I) wherein Ar1, Ar2, R1a, R1b, and R2 are as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of Formula (I), and especially to their use as Galectin-3 inhibitors.

Silica-supported HClO4 promotes catalytic solvent- and metal-free O-H insertion reactions with diazo compounds

Solvent-free O-H insertion reactions in the presence of diazo carbonyl compounds were carried-out in very mild conditions. Unlike the traditional metal-catalysed version, employing rhodium acetate dimer, this method uses eco-friendly silica-supported HClO4 as the catalyst. Only 0.3 mol% of this Br?nsted acid catalyst, that can also be recycled several times, is necessary to guarantee very good yields (up to 97%) in the O-H insertion reactions. Reaction set-up is simple and permitted the preparation of forty-three α-hydroxy and α-alkoxy esters/ketones in just 1 h and at room temperature.

Thiopheneglyoxylic pyridine derivative and its preparation method and medical use

The invention belongs to the field of pharmaceutical chemistry technology, and particularly discloses thienopyridine derivatives, and preparation methods and a medical use thereof. Through structural modification of clopidogrel and prasugrel, a series of new thienopyridine derivative compounds are synthesized and mainly include derivatives esterified with ligustrazine formic acid and shikimic acid; the compounds go into a body, then are rapidly metabolized into effective metabolites and ligustrazine formic acid or shikimic acid, successfully keep away from metabolism of CYP2C19 enzyme, can be directly metabolized into active compounds to play a pharmacological function, thereby solving the clopidogrel resistance problem, effectively improving the compound antithrombotic activity, and also having no significant effect on hemorrhage risk; and the compounds have relatively ideal protective function on liver and kidney, and also have potential therapeutic significance for other cardiovascular diseases.

P(NMe2)3-Mediated Umpolung Alkylation and Nonylidic Olefination of α-Keto Esters

A commercial phosphorus-based reagent (P(NMe2)3) mediates umpolung alkylation of methyl aroylformates with benzylic and allylic bromides, leading to either Barbier-type addition or ylide-free olefination products upon workup. The reaction sequence is initiated by a two-electron redox addition of the tricoordinate phosphorus reagent with an α-keto ester compound (Kukhtin-Ramirez addition). A mechanistic rationale is offered for the chemoselectivity upon which the success of this nonmetal mediated C-C bond forming strategy is based.

INHIBITORS OF VIRAL REPLICATION, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES

The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.

Inhibitors of viral replication, their process of preparation and their therapeutical uses

The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.

BIPHENYLACETAMIDE DERIVATIVE

The present invention provides a compound of formula (I) or a salt thereof, wherein R1, R2 and R3 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, bromine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R4 and R5 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R6 and R7 are independently selected from the group consisting of hydrogen atom, fluorine atom, methyl, ethyl, hydroxy group, and others; and R8 and R9 are independently selected from the group consisting of hydrogen atom, C1-6 alkyl, and others, which is useful as an agent for treating or preventing various types of epilepsy including partial seizures and/or generalized seizures.

2-[1-PHENYL-5-HYDROXY OR METHOXY-4ALPHA-METHYL-HEXAHYDROCLOPENTA[F]INDAZOL-5-YL]ETHYL PHENYL DERIVATIVES AS GLUCOCORTICOID RECEPTOR LIGANDS

The present invention is directed to 2- [l-phenyl-5 -hydroxy or methoxy-4alpha- methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives of formula I (I) as glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflamma

Selective ET(A) antagonists. 5. Discovery and structure-activity relationships of phenoxyphenylacetic acid derivatives

The fifth paper in this series describes the culmination of our investigations into the development of a potent and selective ETA receptor antagonist for the treatment of diseases mediated by ET-1. Receptor site mapping of several ETA antagonists prepared previously identified a common cationic binding site which prompted synthesis of phenoxyphenylacetic acid derivative 13a, which showed good in vitro activity (IC50 59 nM, rat aortic ET(A)). Optimization of 13a led to the identification of 27b, which exhibited an IC50 of 4 nM. Although this did not translate into the expected in vivo potency, a compound of comparable in vitro activity, 27a (RPR118031A), showed a far better pharmacokinetic profile and in vivo potency (75 μmol/kg) and was duly proposed and accepted as a development candidate.

A Suzuki coupling approach to double bonds locked analogues of strobilurin A

Four double bonds locked analogues of strobilurin A were first synthesized via palladium(0)-catalyzed cross-coupling reaction of arylboronic acids with vinyl and aryl bromides.