127404-77-7

Upstream product

• 1117-71-1 methyl 4-bromocrotonate 
• 136294-92-3 Tributyl-(3,4-dichloro-phenyl)-stannane 
• 51114-94-4 (2-carboxyethyl)triphenylphosphonium bromide 
• 6287-38-3 3,4-dichlorobenzaldehyde 
• 36626-29-6 (2-carboxyethyl)triphenylphosphonium chloride 

Downstream Products

• 1439488-56-8 (E)-4-(3,4-dichlorophenyl)-N-(4-oxo-4H-3,1-benzothiazin-2-yl)-but-3-enamide 
• 25157-66-8 4-(3,4-dichlorophenyl)butanoic acid 
• 501426-95-5 methyl (E,4R)-4-(2,5-cyclohexadienyl)-4-(3,4-dichlorophenyl)-2-butenoate 
• 234084-70-9 methyl (E)-2-diazo-4-(3,4-dichlorophenyl)-3-butenoate 
• 147255-16-1 (4R)-4-(3,4-dichlorophenyl)-4-phenylbutanoic acid 
• 124379-29-9 (4S)-4-(3,4-dichlorophenyl)-1-tetralone 
• 155748-61-1 (4R)-(3,4-Dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone 
• 304021-48-5 methyl (4R)-4-(3,4-dichlorophenyl)-4-phenylbutanoate 
• 949568-47-2 (R,E)-methyl 4-(3,4-dichlorophenyl)-4-phenylbut-2-enoate 

Relevant academic research and scientific papers

Dual targeting of adenosine A2A receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones

Blockade of A2A adenosine receptors (A2AARs) and inhibition of monoamine oxidase B (MAO-B) in the brain are considered attractive strategies for the treatment of neurodegenerative diseases such as Parkinson's disease (PD). In the present study, benzothiazinones, e.g., 2-(3-chlorophenoxy)- N-(4-oxo-4H-3,1-benzothiazin-2-yl)acetamide (13), were identified as a novel class of potent MAO-B inhibitors (IC50 human MAO-B: 1.63 nM). Benzothiazinones with large substituents in the 2-position, e.g., methoxycinnamoylamino, phenylbutyrylamino, or chlorobenzylpiperazinylbenzamido residues (14, 17, 27, and 28), showed high affinity and selectivity for A 2AARs (Ki human A2AAR: 39.5-69.5 nM). By optimizing benzothiazinones for both targets, the first potent, dual-acting A2AAR/MAO-B inhibitors with a nonxanthine structure were developed. The best derivative was N-(4-oxo-4H-3,1-benzothiazin-2-yl)-4-phenylbutanamide (17, Ki human A2A, 39.5 nM; IC50 human MAO-B, 34.9 nM; selective versus other AR subtypes and MAO-A), which inhibited A 2AAR-induced cAMP accumulation and showed competitive, reversible MAO-B inhibition. The new compounds may be useful tools for validating the A2AAR/MAO-B dual target approach in PD.

Synthesis of 1-tetralone derivatives using a Stille cross coupling/friedel crafts acylation sequence

An efficient method of synthesis of 1-tetralones has been achieved featuring a Stille cross-coupling reaction as the key step.

Catalytic asymmetric synthesis of diarylacetates and 4,4-diarylbutanoates. A formal asymmetric synthesis of (+)-sertraline

(equation presented) The intermolecular C-H insertion chemistry of phenyldiazoacetates catalyzed by dirhodium tetrakis((S)-N-(dodecylbenzenesulfonyl)prolinate) (Rh2(S-DOSP)4) can be effectively carried out on cyclohexadienes, leading to the asymmetric synthesis of diarylacetates. The reaction of vinyldiazoacetates with cyclohexadienes results in an unprecedented carbenoid reaction that is formally a combined C-H insertion/Cope rearrangement. The synthetic utility of this novel transformation was demonstrated by its utilization in a formal asymmetric synthesis of (+)-sertraline.

Synthesis and cardiovascular activity of phenylalkylamine derivatives. I. Potential specific bradycardic agents

A series of acyclic amide derivatives of N-(ω-aminoalkyl)-N-methylhomoveratrylamine was synthesized and evaluated for their bradycardic activity in isolated guinea pig right atria. Among these compounds, (E)-N-[3[N'-[2-(3,4-dimethoxyphenyl)ethyl]-N'-methy

Synthesis of 6/7-halotetralones

The title compounds were prepared from halobromobenzenes via a palladium catalysed coupling followed by cyclisation.