425704-52-5

Upstream product

• 458-45-7 3-(3-fluorophenyl)propionic acid 
• 18107-18-1 diazomethyl-trimethyl-silane 
• 20595-30-6 3-Fluorocinnamic acid 
• 103-26-4 Methyl cinnamate 
• 67-56-1 methanol 
• 201230-82-2 carbon monoxide 
• 404-70-6 2-(3-Fluorophenyl)ethylamine 
• 87087-34-1 3-(3-fluorophenyl)acrylic acid methyl ester 
• 124-38-9 carbon dioxide 
• 350-51-6 3-fluorostyrene 
• 456-48-4 3-Fluorobenzaldehyde 
• 74325-03-4 methyl (E)-m-fluorocinnamate 

Downstream Products

• 219828-13-4 [4-(3-fluoro-phenyl)-2-oxo-butyl]-phosphonic acid dimethyl ester 
• 700-84-5 5-fluoro-1-indanone 
• 245070-85-3 3-(3-fluorophenyl)propanal 
• 156868-83-6 3-(3-fluorophenyl)propan-1-ol 
• 156868-84-7 1-(3-bromo-propyl)-3-fluoro-benzene 

Relevant academic research and scientific papers

Synthesis and inhibitory studies of phosphonic acid analogues of homophenylalanine and phenylalanine towards alanyl aminopeptidases

A library of novel phosphonic acid analogues of homophenylalanine and phenylalanine, containing fluorine and bromine atoms in the phenyl ring, have been synthesized. Their inhibitory properties against two important alanine aminopeptidases, of human (hAPN, CD13) and porcine (pAPN) origin, were evaluated. Enzymatic studies and comparison with literature data indicated the higher inhibitory potential of the homophenylalanine over phenylalanine derivatives towards both enzymes. Their inhibition constants were in the submicromolar range for hAPN and the micromolar range for pAPN, with 1-amino-3-(3-fluorophenyl) propylphosphonic acid (compound 15c) being one of the best low-molecular inhibitors of both enzymes. To the best of our knowledge, P1 homophenylalanine analogues are the most active inhibitors of the APN among phosphonic and phosphinic derivatives described in the literature. Therefore, they constitute interesting building blocks for the further design of chemically more complex inhibitors. Based on molecular modeling simulations and SAR (structure-activity relationship) analysis, the optimal architecture of enzyme-inhibitor complexes for hAPN and pAPN were determined.

Cobalt(II)-Catalyzed Alkoxycarbonylation of Aliphatic Amines via C-N Bond Activation

The first cobalt-catalyzed deaminative alkoxycarbonylation reaction was described for the conversion of readily available primary alkyl amines to synthetically versatile esters with moderate to high yields. This transformation shows good functional group compatibility and can serve as a powerful tool for the modification of alkyl amine-containing complex natural products and drug molecules.

7-HYDROXY-PYRAZOLO[1,5-A] PYRIMIDINE COMPOUNDS AND THEIR USE AS CCR2 RECEPTOR ANTAGONISTS

The compounds of formula (I) are antagonists of the CCR2 receptor Wherein R1-7 and A are as defined in the claims.

Catalytic asymmetric cross-dehydrogenative coupling: Activation of C-H bonds by a cooperative bimetallic catalyst system

A cooperative bimetallic catalyst system was applied in the catalytic asymmetric cross-dehydrogenative coupling of β-ketoesters and xanthene. Various optically active xanthene derivatives bearing a quaternary stereogenic carbon center were obtained in moderate to good yields (up to 90%) with excellent enantioselectivities (up to 99% ee). Meanwhile, a transition-state model was proposed to explain the origin of the asymmetric induction.

Nickel-catalyzed reductive hydroesterification of styrenes using CO 2 and MeOH

Complexes [(dippe)Ni(μ-H)]2 (A) (dippe = 1,2-bis-di- isopropylphosphino)ethane) and [(dtbpe)Ni(μ-H)]2 (B) (dtbpe = 1,2-bis-di-tert-butylphospino)ethane) catalyze the reductive hydroesterification of styrenes with the use of CO2 and MeOH. The latter acts as a hydrogen source and as an esterificating agent, to yield the corresponding branched and linear esters in moderate to good yields. In all of the studied reactions the linear esters were obtained in higher amounts than the branched ones. When the hydroesterification reaction was carried out using a stoichiometric metal/substrate ratio, the complexes [(P-P)Ni(CO)2] and [(P-P)Ni(CO3)] (P-P = dippe or dtbpe) were isolated and characterized by standard spectroscopic methods. Compounds [(dtbpe)Ni(CO) 2] and [(dtbpe)Ni(CO3)] were also fully characterized by single-crystal X-ray diffraction.

7-HYDROXY-PYRAZOLO[1,5-A] PYRIMIDINE COMPOUNDS AND THEIR USE AS CCR2 RECEPTOR ANTAGONISTS

The compounds of formula (I) are antagonists of the CCR2 receptor Wherein R1-7 and A are as defined in the claims.

TRICYCLIC NITROGEN CONTAINING COMPOUNDS AND THEIR USE AS ANTIBACTERIALS

Compounds of Formula (I) or a pharmaceutically acceptable salt or N-oxide thereof; Formula (I) (relative stereochemistry shown) wherein: Z1, Z2 , L are as defined, U represents a cyclic group selected from: phenyl, pyridyl, pyridazin

BICYCLIC TRIAZOLONE DERIVATIVES AND HERBICIDES CONTAINING THE SAME

The present invention provides a bicyclic triazolone derivative represented by the formula:J-Ar [wherein, J is and Ar is ], which has excellent selective weeding activity and weed killer containing the said bicyclic triazolone derivative.

Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects

The recent discovery that small molecule ligands for the peptidyl-prolyl isomerase (PPIase) FKBP12 possess powerful neuroprotective and neuroregenerative properties in vitro and in vivo suggests therapeutic utility for such compounds in neurodegenerative disease. The neurotrophic effects of these compounds are independent of the immunosuppressive pathways by which drugs such as FK506 and rapamycin operate. Previous work by ourselves and other groups exploring the structure-activity relationships (SAR) of small molecules that mimic only the FKBP binding domain portion of FK506 has focused on esters of proline and pipecolic acid. We have explored amide and thioester analogues of these earlier structures and found that they too are extremely potent in promoting recovery of lesioned dopaminergic pathways in a mouse model of Parkinson's disease. Several compounds were shown to be highly effective upon oral administration after lesioning of the dopaminergic pathway, providing further evidence of the potential clinical utility of a variety of structural classes of FKBP12 ligands.

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.