51230-93-4

Upstream product

• 67031-08-7 methyl 2-(4-fluorophenyl)pent-4-enoate 
• 556-56-9 allyl iodid 
• 405-50-5 p-Fluorophenylacetic acid 
• 34837-84-8 4-fluorobenzeneacetic acid methyl ester 
• 106-95-6 allyl bromide 

Downstream Products

• 1235493-42-1 methyl N-4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl-N'-(2-(4-fluorophenyl)pent-4-enoyl)carbamimidothioate 
• 691873-56-0 N-(3,5-bis-trifluoromethyl-benzyl)-2-(4-fluoro-phenyl)-4-(4-phenyl-piperidin-1-yl)-butyramide 

Relevant academic research and scientific papers

Dual Activation of Unsaturated Amides with Schwartz's Reagent: A Diastereoselective Access to Cyclopentanols and N,O-Dimethylcyclopentylhydroxylamines.

The diastereoselective access to cyclopentanols and N,O-dimethylcyclopentylhydroxylamines from 4-pentenoic acid-derived Weinreb amides is described. Based on the concomitant generation of both the nucleophilic and the electrophilic poles by hydrozirconati

CuX2-mediated oxybromination/aminochlorination of unsaturated amides: Synthesis of iminolactones and lactams

We report herein a CuX2-mediated halocyclization of γ,δ-unsaturated amides for the synthesis of functionalized iminolactones and lactams respectively under mild reaction conditions. Mechanism studies indicated that N-attack cyclization was via a radical route while oxycyclization was via a nucleophilic attack on the activated CC bond.

BICYCLIC COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION

The present disclosure provides a series of compounds of the formula (I) which reduce β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production, wherein

Highly chemo- and enantioselective synthesis of 3-Allyl-3-aryl oxindoles via the direct palladium-catalyzed α-arylation of amides

Figure presented A new NHC·Pd-catalyzed asymmetric α-arylation of amides is reported that gives direct access to synthetically valuable, allylated oxindoles with quaternary carbon centers. The reaction is made possible by the introduction of a new chiral NHC ligand. The palladium complexes derived therefrom combine excellent reactivity with high chemo- and enantioselectivity for the title transformation.

Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: Synthesis and biological evaluation

Within the continuous quest for the discovery of novel compounds able to treat anxiety and depression, the generation of a pharmacophore model for 5-HT2C receptor antagonists and the discovery of a new class of potent and selective 5-HT2C

Novel, orally bioavailable γ-aminoamide CC chemokine receptor 2 (CCR2) antagonists

Through modification of a screening hit we have discovered a structurally distinct new lead, (2S)-N-[3,5-bis(trifluoromethyl)benzyl]-2-(4-fluorophenyl)-4- (4-phenylpiperidin-1-yl)butanamide (11), which has subsequently served as the departure point for an

GAMMA-AMINOAMIDE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY

The present invention is directed to compounds of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R11, R12, W, X, and n are defined herein, which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.

Synthesis and structure-antifungal activity relationships of 3-aryl-5-alkyl-2,5-dihydrofuran-2-ones and their carbanalogues: Further refinement of tentative pharmacophore group

Two series of 3-(substituted phenyl)-5-alkyl-2,5-dihydrofuran-2-ones related to a natural product, (-)incrustoporine, were synthesized and their in vitro antifungal activity evaluated. The compounds with halogen substituents on the phenyl ring exhibited selective antifungal activity against the filamentous strains of Absidia corymbifera and Aspergillus fumigatus. On the other hand, the influence of the lenghth of the alkyl chain at C(5) was marginal. The antifungal effect of the most active compound against the above strains was higher than that of ketoconazole, and close to that of amphotericin B. In order to verify the hypothesis about a possible relationship between the Michael-accepting ability of the compounds and their antifungal activity, a series of simple carbanalogues, 2-(substituted phenyl)cyclopent-2-enones, was prepared and subjected to antifungal activity assay as well.

COMPOUNDS HAVING AFFINITY AT 5HT2C RECEPTOR AND USE THEREOF IN THERAPY

Compounds of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: wherein R1 is hydrogen, hydroxy, fluoro, chloro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy or haloC

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: Structure-activity relationships for substituted 2-aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes

(2S)-2-(3,4-Dichlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2 ,3-dihydrobenzthiophene-3,4′-piperidin-1′yl)]butane S-oxide (3) has been identified as a potent CCR5 antagonist lead structure having an IC50 = 35 nM. Herein, we describe the structure-activity relationship studies directed toward the requirement for and optimization of the C-2 phenyl fragment. The phenyl was found to be important for CCR5 antagonism and substitution was limited to small moieties at the 3-position (13 and 16: X = H, 3-F, 3-Cl, 3-Me).