41381-97-9

Upstream product

• 94-02-0 ethyl 3-oxo-3-phenylpropionate 
• 7791-25-5 sulfuryl dichloride 
• 128-09-6 N-chloro-succinimide 
• 28383-65-5 ethyl 2-diazo-3-oxo-3-phenylpropanoate 
• 98-86-2 acetophenone 

Downstream Products

• 107776-42-1 2-(N'-acetyl-hydrazino)-4-phenyl-thiazole-5-carboxylic acid ethyl ester 
• 6528-19-4 2,5-diphenyl-2H-pyrazole-3,4-dione 4-phenylhydrazone 
• 32002-72-5 2-methyl-4-phenyl-1,3-thiazole-5-carboxylic acid 
• 92109-01-8 5-hydroxy-2-methylsulfanyl-5-phenyl-5,6-dihydro-4H-[1,3,4]thiadiazine-6-carboxylic acid ethyl ester 
• 109406-78-2 2-isopropylidenehydrazino-4-phenyl-selenazole-5-carboxylic acid ethyl ester 
• 93879-87-9 5-hydroxy-2,5-diphenyl-5,6-dihydro-4H-[1,3,4]thiadiazine-6-carboxylic acid ethyl ester 
• 41126-61-8 4-hydroxy-3-methyl-4-phenyl-2-thioxo-thiazolidine-5-carboxylic acid ethyl ester 
• 41126-62-9 4-hydroxy-3,4-diphenyl-2-thioxo-thiazolidine-5-carboxylic acid ethyl ester 
• 31089-59-5 7-chloro-2-phenyl-1H-pyrido[2,3-b][1,4]thiazine-3-carboxylic acid ethyl ester 
• 32043-95-1 2-methyl-4-phenyl-thiazole-5-carboxylic acid ethyl ester 
• 97724-16-8 2-(3-methyl-5-oxo-2,5-dihydro-pyrazol-1-yl)-4-phenyl-selenazole-5-carboxylic acid ethyl ester 
• 111639-45-3 2-benzylidenehydrazino-4-phenyl-selenazole-5-carboxylic acid ethyl ester 
• 80304-39-8 ethyl 5-phenylimidazole-4-carboxylate 
• 78978-99-1 2-[(E)-Benzoylimino]-5-phenyl-[1,3]oxathiole-4-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

PHARMACEUTICAL COMPOUNDS

Benzodiazepine derivatives of formula (I): (I) wherein: each of R1 and R2 is independently H or halo; either (i) T is N, Z is C, ---a--- and ---c--- are bonds, and ---b--- and ---d--- are absent; or (ii) T is C, Z is N, ---b--- and ---d--- are bonds, and ---a--- and ---c--- are absent; each of R3 and R4 is independently halo, -OR6, -NR6R7, -COR8, -C(O)OR8, -CON(R8)2 or -R6; R5 is H or halo; each of R6 and R7 is independently H or a group selected from C1-C6 alkyl, C3-C10 cycloalkyl, C6-C10 aryl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, the group being unsubstituted or substituted; R8 is H or C1-C6 alkyl, each R8 being the same or different when two are present; n is 0 or 1; and one of V, W, X and Y is N or CH and the other three are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.

Electrochemical chlorination and bromination of electron-deficient C[sbnd]H bonds in quinones, coumarins, quinoxalines and 1,3-diketones

The electrochemistry-promoted chlorination and bromination of electron-deficient C[sbnd]H bonds was developed, using quinones, coumarins, quinoxalines and 1,3-diketones. This protocol features readily available and safe halogen sources (hydrochloric acid and KBr), high site-selectivity and mild reaction conditions. It could provide an efficient access to a series of chlorinated and brominated quinones, coumarins, quinoxalines and 1,3-diketones.

SAR Studies of the Leupyrrins: Design and Total Synthesis of Highly Potent Simplified Leupylogs

Leupyrrins are highly potent antifungal agents. A structure–activity-relationship study of natural and synthetic derivatives is reported which reveals important insights into the biological relevance of several structural subunits leading to the discovery

Metal-Free Halogenation of N-Substituted Enaminoesters and Enaminones: A Facile Access to Functionalized α,α-Dihaloimines

An efficient and general method for the synthesis of functionalized α,α-dihaloimines via halogenation of N-substituted enaminoesters and enaminones is described. This reaction, in which both α,α-dihaloimines and mixed α,α-dihaloimines could be achieved in

CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF

Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.

Copper Triflate Mediated α-Monohalogenation of α-Diazo β-Ketosulfones with Ammonium Halides

Copper triflate mediated α-monohalogenation of α-diazo β-ketosulfones with ammonium halides provides the corresponding α-halo β-ketosulfones. Different metal triflates are investigated for this facile and efficient transformation. A plausible mechanism is proposed.

Trimethylchlorosilane-Mediated Mild α-Chlorination of 1,3-Dicarbonyl Compounds Promoted by Phenyliodonium Diacetate

Trimethylchlorosilane was used as chlorine source for the α-chlorination of 1,3-dicarbonyl compounds with phenyliodonium diacetate as oxidant at room temperature. The reaction allows the selective synthesis of α-monochlorinated products from different kinds of 1,3-dicarbonyl compounds in good yield. The potential possibility of this conversion for bromination has also been investigated.

Imidazole-based pinanamine derivatives: Discovery of dual inhibitors of the wild-type and drug-resistant mutant of the influenza A virus

We previously reported potent hit compound 4 inhibiting the wild-type influenza A virus A/HK/68 (H3N2) and A/M2-S31N mutant viruses A/WS/33 (H1N1), with its latter activity quite weak. To further increase its potency, a structure-activity relationship study of a series of imidazole-linked pinanamine derivatives was conducted by modifying the imidazole ring of this compound. Several compounds of this series inhibited the amantadine-sensitive virus at low micromolar concentrations. Among them, 33 was the most potent compound, which was identified as being active on an amantadine-sensitive virus through blocking of the viral M2 ion channel. Furthermore, 33 markedly inhibited the amantadine-resistant virus (IC50 = 3.4 μM) and its activity increased by almost 24-fold compared to initial compound, with its action mechanism being not M2 channel mediated.

Preparation of iodonium ylides: Probing the fluorination of 1,3-dicarbonyl compounds with a fluoroiodane

The isolation of iodonium ylide 8, from the reaction of fluoroiodane 1 with ethyl 3-oxo-3-phenylpropanoate 5 in the presence of potassium fluoride, provides strong evidence that 1,3-dicarbonyl compounds undergo an addition reaction with fluoroiodane 1 to form an iodonium intermediate which can be deprotonated to generate an iodonium ylide. In the presence of TREAT-HF, however, the iodonium intermediate reacts to form the 2-fluoro-1,3-dicarbonyl product and we propose that fluoroiodane 1 simulates electrophilic fluorination via an addition/substitution mechanism. Further evidence to support this mechanism was obtained by successfully reacting the isolated iodonium ylide 8 with TREAT-HF, hydrochloric acid, acetic acid and p-toluenesulfonic acid to form the 2-fluoro-, 2-chloro-, 2-acetyl- and 2-tosyl-1,3-ketoesters respectively. This journal is

Vanadium-catalyzed chlorination under molecular oxygen

A catalytic chlorination of ketones was performed by using a vanadium catalyst in the presence of Bu4NI and AlCl3 under atmospheric molecular oxygen. This catalytic chlorination could be applied to the chlorination of alkenes to give the corresponding vic-dichlorides. AlCl3 was found to serve as both a Lewis acid and a chloride source to induce the facile chlorination. A combination of Bu4NI and AlI3 in the presence of a vanadium catalyst under atmospheric molecular oxygen induced the iodination of ketones.