52085-96-8

Upstream product

• 2019-34-3 3-(4-chlorophenyl)propanoic acid 
• 1615-02-7 3-(4-chlorophenyl)prop-2-enoic acid 
• 104-88-1 4-chlorobenzaldehyde 
• 1615-02-7 p-chlorocinnamic acid 
• 79-37-8 oxalyl dichloride 
• 501-52-0 3-Phenylpropionic acid 
• 7116-36-1 ethyl 3-(4-chlorophenyl)propanoate 

Downstream Products

• 111302-55-7 3-(4-chlorophenyl)-1-(4-methoxyphenyl) propan-1-one 
• 874488-50-3 1-biphenyl-4-yl-3-(4-chloro-phenyl)-propan-1-one 
• 5739-39-9 3-(4-chlorophenyl)-1-phenylpropan-1-one 
• 14548-38-0 6-chloro-1-indanone 
• 156-41-2 4-chlorophenylethylamine 
• 17052-48-1 3-(4-Chloro-phenyl)-N-(3,4-dimethoxy-benzyl)-propionamide 
• 74631-92-8 ethyl 5-(p-chlorophenyl)-3-oxovalerate 
• 144922-42-9 7-{2-[3-(4-Chloro-phenyl)-propionyl]-thiophen-3-yl}-heptanoic acid ethyl ester 
• 146822-74-4 7-{5-[3-(4-Chloro-phenyl)-propionyl]-thiophen-3-yl}-heptanoic acid ethyl ester 
• 3251-34-1 1-(2-Ethyl-4,5-dimethoxy-phenyl)-3-(4-chlor-phenyl)-propanon-⁽¹⁾ 
• 494783-49-2 (4R)-3-[3-(4-chlorophenyl)propanoyl]-4-benzyl-1,3-oxazolidin-2-one 
• 130340-68-0 N-(p-chlorobenzoyl)-2-(p-chlorophenyl)ethylamine 
• 117240-07-0 2(3(4'-chlorophenyl)propionyl)cyclohexanone 
• 63293-75-4 2-{4-[2-[3-(4-chlorophenyl)-propionylamino]-ethyl]-phenoxy}-2-methylpropionic acid 

Relevant academic research and scientific papers

Enhancement of the carbamate activation rate enabled syntheses of tetracyclic benzolactams: 8-oxoberbines and their 5- And 7-membered C-ring homologues

A route to the direct amidation of aromatic-ring-tetheredN-carbamoyl tetrahydroisoquinoline substrates was developed. This route enabled general access to 8-oxoberberines and their 5- and 7- membered C-ring homologues. It overcomes the undesired tandem side-reactions that result in the destruction of the isoquinoline backbone, which inevitably occurred under our previously reported superacidic carbamate activation method.

Ruthenium-catalyzed intramolecular arene C(sp2)-H amidation for synthesis of 3,4-dihydroquinolin-2(1 H)-ones

We report the [Ru(p-cymene)(l-proline)Cl] ([Ru1])-catalyzed cyclization of 1,4,2-dioxazol-5-ones to form dihydroquinoline-2-ones in excellent yields with excellent regioselectivity via a formal intramolecular arene C(sp2)-H amidation. The reactions of the 2- and 4-substituted aryl dioxazolones proceeds initially through spirolactamization via electrophilic amidation at the arene site, which is para or ortho to the substituent. A Hammett correlation study showed that the spirolactamization is likely to occur by electrophilic nitrenoid attack at the arene, which is characterized by a negative ρ value of -0.73.

Visible-Light Induced C(sp2)?H Amidation with an Aryl–Alkyl σ-Bond Relocation via Redox-Neutral Radical–Polar Crossover

We report an approach for the intramolecular C(sp2)?H amidation of N-acyloxyamides under photoredox conditions to produce δ-benzolactams with an aryl-alkyl σ-bond relocation. Computational studies on the designed reductive single electron transfer strategy led us to identify N-[3,5-bis(trifluoromethyl)benzoyl] group as the most effective amidyl radical precursor. Upon the formation of an azaspirocyclic radical intermediate by the selective ipso-addition with outcompeting an ortho-attack, radical–polar crossover was then rationalized to lead to the rearomative ring-expansion with preferential C?C bond migration.

PSNCBAM-1 analogs: Structural evolutions and allosteric properties at cannabinoid CB1 receptor

Allosteric modulation of the CB1Rs could represent an alternative strategy for the treatment of diseases in which these receptors are involved, without the undesirable effects associated with their orthosteric stimulation. PSNCBAM-1 is a reference diaryl urea derivative that positively affects the binding affinity of orthosteric ligands (PAM) and negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs. In this work we reported the design, synthesis and biological evaluation of three different series of compounds, derived from structural modifications of PSNCBAM-1 and its analogs reported in the recent literature. Almost all the new compounds increased the percentage of binding affinity of CP55940 at CB1Rs, showing a PAM profile. When tested alone in the [35S]GTPγS functional assay, only a few derivatives lacked detectable activity, so were tested in the same functional assay in the presence of CP55940. Among these, compounds 11 and 18 proved to be functional NAMs at CB1Rs, dampening the orthosteric agonist-induced receptor functionality by approximately 30percent. The structural features presented in this work provide new CB1R-allosteric modulators (with a profile similar to the reference compound PSNCBAM-1) and an extension of the structure-activity relationships for this type of molecule at CB1Rs.

MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for the modulation of elF2B, for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

Cyclohexyl-Fused, Spirobiindane-Derived, Phosphine-Catalyzed Synthesis of Tricyclic ?3-Lactams and Kinetic Resolution of ?3-Substituted Allenoates

A C2-symmetric chiral phosphine catalyst, NUSIOC-Phos, which can be easily derived from cyclohexyl-fused spirobiindane, was introduced. A highly enantioselective domino process involving pyrrolidine-2,3-diones and γ-substituted allenoates catalyzed by NUSIOC-Phos has been disclosed. Diastereospecific tricyclic γ-lactams containing five contiguous stereogenic centers were obtained in high yields and with nearly perfect enantioselectivities. A kinetic resolution process of racemic γ-substituted allenoates was developed for the generation of optically enriched chiral allenoates.

Discovery and evolution of aloperine derivatives as novel anti-filovirus agents through targeting entry stage

Preventing filoviruses in the entry stage is an attractive antiviral strategy. Taking aloperine, a Chinese natural herb with an endocyclic skeleton, as the lead, 23 new aloperine derivatives were synthesized and evaluated for their anti-filovirus activiti

MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

Ligand-Assisted Palladium(II)/(IV) Oxidation for sp3C H Fluorination

The direct functionalization of inert sp3C H bonds is limited to a few bond types. Although the activation of sp3C H bonds can be accomplished under mild conditions using palladium catalysts, the subsequent functionalization is not trivial due to the high energy required to convert palladium(II) to palladium(IV). We have systematically studied the palladium oxidation using computation-guided experiments for reactions involving strong chelation control. We find that a mild external ligand could significantly accelerate the oxidation of palladium(II) to palladium(IV) for strong bidentate directing groups. The acceleration is believed to be a result of ligand stabilization of both the palladium(II) and palladium(IV) intermediates. (Figure presented.) .

ISOXAZOLYL SUBSTITUTED BENZIMIDAZOLES

A compound which is a benzimidazolyl isoxazole of formula (I): wherein: R0and R, which are the same or different, are each H or C1-6 alkyl; R9, R9 and R9, which are the same or different, are each H o