7448-86-4

Upstream product

• 2125-49-7 3-dimethylamino-1-(4-methoxy-phenyl)-propan-1-one; hydrochloride 
• 100-66-3 methoxybenzene 
• 625-36-5 2-chloropropionyl chloride 
• 51410-44-7 1-(4-methoxylphenyl)-2-propen-1-ol 
• 33994-11-5 α-Bromoethyl p-methoxaphenyl ketone 
• 95605-45-1 [3-(4-methoxy-phenyl)-3-oxo-propyl]-trimethyl-ammonium; bromide 
• 18096-70-3 3-dimethylamino-4'-methoxyacrylophenone 
• 87015-46-1 1-(4-methoxyphenyl)-3-tosylpropan-1-one 
• 87015-44-9 3-((4-chlorophenyl)sulfonyl)-1-(4-methoxyphenyl)propan-1-one 
• 77253-67-9 trifluoroethanol-d₃ 
• 81112-07-4 2-chloro-1-(4'-methoxyphenyl)-propan-1-one 
• 3153-44-4 4-(4-methoxy-phenyl)-4-oxo-butyric acid 
• 201230-82-2 carbon monoxide 
• 7486-35-3 tri-n-butyl(vinyl)tin 

Downstream Products

• 103990-59-6 N,N-bis-[3-(4-methoxy-phenyl)-3-oxo-propyl]-O-methyl-hydroxylamine 
• 121-97-1 4-Methoxypropiophenone 
• 3314-43-0 3-(4-methoxy-phenyl)-1-phenyl-4,5-dihydro-1H-pyrazole 
• 67756-15-4 1-(4-Methoxyphenyl)-1,4-decandion 
• 60755-22-8 1-(4-methoxyphenyl)-4-phenyl-1,4-butanedione 
• 15982-64-6 1,4-bis(4-methoxyphenyl)butane-1,4-dione 
• 2108-54-5 1-(4-methoxyphenyl)pentane-1,4-dione 
• 54605-99-1 (4-methoxyphenyl)(3-methyl-4,5-dihydroioxazol-5-yl)methanone 
• 87015-46-1 1-(4-methoxyphenyl)-3-tosylpropan-1-one 
• 143619-29-8 (S)-2-Cyano-5-(4-methoxy-phenyl)-2-methyl-5-oxo-pentanoic acid isopropyl ester 
• 143619-29-8 (R)-2-Cyano-5-(4-methoxy-phenyl)-2-methyl-5-oxo-pentanoic acid isopropyl ester 
• 87015-44-9 3-((4-chlorophenyl)sulfonyl)-1-(4-methoxyphenyl)propan-1-one 
• 130767-31-6 (E)-3-(2,4-Dimethoxy-pyrimidin-5-yl)-1-(4-methoxy-phenyl)-propenone 
• 14006-70-3 3-indol-3-yl-1-(4-methoxy-phenyl)-propan-1-one 

Relevant academic research and scientific papers

Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation

The current chemotherapy against Chagas disease is inadequate and insufficient. A series of ten Mannich base-type derivatives have been synthesized to evaluate their in vitro antichagasic activity. After a preliminary screening, compounds 7 and 9 were sub

Substituent Effects on the Photosolvolyses of 2-Chloropropiophenones in 2,2,2-Trifluoroethanol

The substituent effects on the product distribution of the photosolvolyses of 2-chloropropiophenones in 2,2,2-trifluoroethanol were investigated.A ?-electron-donating methoxy substituent at p- and m-position enhanced the heterolytic product of the nucleophilic substitution over that of phenyl-rearrangement.

Rongalite as C1 Synthon and Sulfone Source: A Practical Sulfonylmethylation Based on the Separate-Embedding Strategy

Rongalite has been used in several challenging synthetic transformations with operationally simple and effective protocols. However, the employment of multiple characteristics of rongalite in synthetic chemistry is comparatively little known. Herein we report a separate-embedding type sulfonylmethylation of sulfoxonium ylides in which rongalite concurrently acted as a sulfone source, C1 synthon, radical initiator, and potential reducing reagent for the first time. Notably, this facile and easy-handling reaction does not require a catalyst or prefunctionalized sulfonylmethylation reagents.

Nickel-Catalyzed C(sp3)-H Functionalization of Benzyl Nitriles: Direct Michael Addition to Terminal Vinyl Ketones

An efficient nickel(0)-catalyzed addition of benzyl nitriles to terminal vinyl ketones via C(sp3)-H functionalization has been developed. The reaction provides a novel and efficient protocol for the synthesis of α-functionalized benzyl nitriles with a wide range of structural diversity under mild reaction conditions while obviating the use of a strong base. The work might be potentially useful toward the development of an enantioselective variant using chiral nitrogen ligands.

Metabolically stable vanillin derivatives for the treatment of hypoxia

Vanillin derivative compounds that bind covalently with hemoglobin are provided. Methods of treating sickle cell disease and other hypoxia-related disorders by administering such compounds are also provided.

Design and synthesis of Mannich base-type derivatives containing imidazole and benzimidazole as lead compounds for drug discovery in Chagas Disease

The protozoan parasite Trypanosoma cruzi is the causative agent of Chagas disease, the most important parasitic infection in Latin America. The only treatments currently available are nitro-derivative drugs that are characterised by high toxicity and limited efficacy. Therefore, there is an urgent need for more effective, less toxic therapeutic agents. We have previously identified the potential for Mannich base derivatives as novel inhibitors of this parasite. To further explore this family of compounds, we synthesised a panel of 69 new analogues, based on multi-parametric structure-activity relationships, which allowed optimization of both anti-parasitic activity, physicochemical parameters and ADME properties. Additionally, we optimized our in vitro screening approaches against all three developmental forms of the parasite, allowing us to discard the least effective and trypanostatic derivatives at an early stage. We ultimately identified derivative 3c, which demonstrated excellent trypanocidal properties, and a synergistic mode of action against trypomastigotes in combination with the reference drug benznidazole. Both its druggability and low-cost production make this derivative a promising candidate for the preclinical, in vivo assays of the Chagas disease drug-discovery pipeline.

Mild Darzens Annulations for the Assembly of Trifluoromethylthiolated (SCF3) Aziridine and Cyclopropane Structures

We report mild new annulation approaches to trisubstituted trifluoromethylthiolated (SCF3) aziridines and cyclopropanes via Darzens inspired protocols. The products of these anionic annulations, rarely studied previously, possess attractive features rendering them valuable building blocks for synthesis platforms. In this study, trisubstituted acetophenone nucleophiles bearing SCF3 and bromine substituents in their α position were shown to undergo [2 + 1] annulations with vinyl ketones and tosyl-protected imines under mild reaction conditions.

Generation of α-Boryl Radicals and Their Conjugate Addition to Enones: Transition-Metal-Free Alkylation of gem-Diborylalkanes

A transition-metal-free method for the alkylation of gem-diborylalkanes with α,β-unsaturated ketones has been developed. It is demonstrated that the α-boryl radicals can be generated efficiently from gem-diborylalkanes with the aid of catechol and oxidants. The α-boryl radicals formed through such process can be engaged in conjugate addition reaction with α,β-unsaturated ketones. This transformation is a straightforward method for the synthesis of γ-borylketones.

Enantioselective Copper-Catalyzed Electrophilic Sulfenylation of Cyclic Imino Esters

Herein we report an enantioselective sulfenylation of cyclic imino esters with the efficient and versatile sulfenylation reagent S-alkyl 4-methylbenzenesulfonothioates. By utilizing the Cu/tBu-Phosferrox catalytic system, we can assemble diverse S-alkyl groups into the cyclic imino esters under mild conditions in good yields and with excellent enantioselectivities. Remarkably, this method demonstrates a high tolerance of diverse functional groups and proves to be applicable in the late-stage functionalization of pharmaceuticals.

An investigation of structure‐activity relationships of azolylacryloyl derivatives yielded potent and long‐acting hemoglobin modulators for reversing erythrocyte sickling

Aromatic aldehydes that bind to sickle hemoglobin (HbS) to increase the protein oxygen affinity and/or directly inhibit HbS polymer formation to prevent the pathological hypoxia‐induced HbS polymerization and the subsequent erythrocyte sickling have for s