193151-11-0

Upstream product

• 67-56-1 methanol 
• 42287-97-8 3-(3-cyanophenyl)propanoic acid 
• 103-25-3 3-phenylpropanoic acid methyl ester 
• 557-21-1 zinc(II) cyanide 
• 79432-87-4 methyl m-bromocinnamate 
• 61389-68-2 methyl 3-(3-hydroxyphenyl)propionate 
• 621-54-5 3-(3-hydroxyphenyl)-propanoic acid 
• 18107-18-1 diazomethyl-trimethyl-silane 
• 52116-81-1 methyl 3-(3-cyanophenyl) acrylate 
• 73183-34-3 bis(pinacol)diborane 
• 193151-10-9 3-(3-cyano-phenyl)-acrylic acid methyl ester 
• 24964-64-5 3-Cyanobenzaldehyde 
• 16642-93-6 (3E)-3-(3-cyanophenyl)acrylic acid 
• 557-21-1 dicyanozinc 

Downstream Products

• 223491-44-9 2-Methyl-3-{3-[(4-pyrazol-1-yl-benzylamino)-methyl]-phenyl}-propionic acid methyl ester 
• 223491-45-0 3-(3-{[benzenesulfonyl-(4-pyrazol-1-yl-benzyl)-amino]-methyl}-phenyl)-2-methyl-propionic acid methyl ester 
• 223489-88-1 3-(3-{[Benzenesulfonyl-(4-pyrazol-1-yl-benzyl)-amino]-methyl}-phenyl)-2-methyl-propionic acid 
• 1000895-59-9 3-[2-(5-amino-2H-pyrazol-3-yl)ethyl]benzonitrile 
• 100511-83-9 methyl 3-(3-aminomethylphenyl)propionate 
• 223491-41-6 3-(3-cyano-phenyl)-2-methyl-propionic acid methyl ester 
• 223491-46-1 3-(3-{[(1-Methyl-1 H-imidazole-4-sulfonyl)-(4-pyrazin-2-yl-benzyl)-amino]-methyl}-phenyl)-propionic acid methyl ester 
• 193151-12-1 3-(3-cyanophenyl)propionic acid thiopyridyl ester 
• 202208-74-0 3-(3-Cyano-phenyl)-propionyl chloride 
• 927187-49-3 3-(3-{4-[2-(2,4-dichloro-phenoxy)-ethylcarbamoyl]-5-phenyl-isoxazol-3-yl}-phenyl)-propionic acid methyl ester 
• 62876-44-2 3-(3-Formyl-phenyl)-propionic acid methyl ester 

Relevant academic research and scientific papers

Manganese-catalyzed homogeneous hydrogenation of ketones and conjugate reduction of α,β-unsaturated carboxylic acid derivatives: A chemoselective, robust, and phosphine-free in situ-protocol

We communicate a user-friendly and glove-box-free catalytic protocol for the manganese-catalyzed hydrogenation of ketones and conjugated C[dbnd]C[sbnd]bonds of esters and nitriles. The respective catalyst is readily assembled in situ from the privileged [Mn(CO)5Br] precursor and cheap 2-picolylamine. The catalytic transformations were performed in the presence of t-BuOK whereby the corresponding hydrogenation products were obtained in good to excellent yields. The described system offers a brisk and atom-efficient access to both secondary alcohols and saturated esters avoiding the use of oxygen-sensitive and expensive phosphine-based ligands.

Dual Ligand-Enabled Nondirected C-H Cyanation of Arenes

Aromatic nitriles are key structural units in organic chemistry and, therefore, highly attractive targets for C-H activation. Herein, the development of an arene-limited, nondirected C-H cyanation based on the use of two cooperatively acting commercially available ligands is reported. The reaction enables the cyanation of arenes by C-H activation in the absence of directing groups and is therefore complementary to established approaches.

Chemoselective Cu(I) catalyzed bis(pinacolato)diboron conjugate addition and reduction onto α,β-unsaturated carbonyl compounds

Ligand-free CuI-catalyzed bis(pinacolato)diboron (B2(pin)2) conjugate addition and reduction onto α,β-unsaturated carbonyl compounds in moderate to excellent yields has been demonstrated.

Novel Compounds

There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.

3,4,5-Trisubstituted isoxazoles as novel PPARδ agonists. Part 2

A series of PPARδ-selective agonists was investigated and optimized for a favorable in vivo pharmacokinetic profile. Isoxazole LCI765 (17d) was found to be a potent and selective PPARδ agonist with good in vivo PK properties in mouse (Cmax = 5.1 μM, t1/2 = 3.1 h). LCI765 regulated expression of genes involved in energy homeostasis in relevant tissues when dosed orally in C57BL6 mice. A co-crystal structure of compound LCI765 and the LBD of PPARδ is discussed.

Prostaglandin agonists and their use to treat bone disorders

This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues

The in vitro evaluation of a series of saturated prostaglandins revealed that compounds with omega chin aromatic rings retain nanomolar potency for the human prostaglandin F receptor (hFP receptor), exemplified by compound 8. In contrast, the double bonds are required for activity in the series with an acyclic omega chain as in PGF(2α). (C) 2000 Published by Elsevier Science Ltd.

Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa

The discovery and some of the basic structure-activity relationships of a series of novel nonpeptide inhibitors of blood coagulation Factor Xa is described. These inhibitors are functionalized β-alanines, exemplified by 2a. Docking experiments placing 2a in the active site of Factor Xa implied that the most expeditious route to enhancing in vitro potency was to modify the group occupying the S3 site of the enzyme. Increasing the hydrophobic contacts between the inhibitor and the enzyme in this region led to 8, which has served as the prototype for this series. In addition, an enantioselective synthesis of these substituted β-alanines was also developed.