22966-10-5

Upstream product

• 98-86-2 acetophenone 
• 6630-33-7 ortho-bromobenzaldehyde 
• 2039-88-5 2-bromostyrene 
• 611-73-4 Benzoylformic acid 
• 2648-61-5 2,2-dichloroacetophenone 
• 3453-00-7 diethyl benzoylmethylphosphonate 
• 6048-29-9 triphenylphenacylphosphonium bromide 
• 536-74-3 phenylacetylene 

Downstream Products

• 74746-17-1 3-Bromo-4-(3-oxo-indan-1-yl)-benzenesulfonic acid 
• 878206-25-8 (R)-3-(2-bromophenyl)-4-nitro-1-phenylbutan-1-one 
• 735291-43-7 3-acetylamino-4-(2-bromophenyl)-2-oxo-6-phenyl-1,2,3,4-tetrahydropyridine-3-carboxylic acid ethyl ester 
• 18480-82-5 3-phenyl-2,9-dihydro-1H-pyrido[3,4-b]indol-1-one 
• 735291-25-5 2-acetylamino-2-cyano-3-(2-bromophenyl)-5-oxo-5-phenylpentanoic acid ethyl ester 
• 167367-47-7 (E)-1-bromo-2-(3'-hydroxy-3'-phenylprop-1'-enyl)benzene 

Relevant academic research and scientific papers

C3 amino-substituted chalcone derivative with selective adenosine rA1 receptor affinity in the micromolar range

Abstract: To identify novel adenosine receptor (AR) ligands based on the chalcone scaffold, herein the synthesis, characterization and in vitro and in silico evaluation of 33 chalcones (15–36 and 37–41) and structurally related compounds (42–47) are reported. These compounds were characterized by radioligand binding and GTP shift assays to determine the degree and type of binding affinity, respectively, against rat (r) A1 and A2A ARs. The chalcone derivatives 24, 29, 37 and 38 possessed selective A1 affinity below 10?μM, and thus, are the most active compounds of the present series; compound 38 was the most potent selective A1 AR antagonist (Ki (r) = 1.6?μM). The structure–affinity relationships (SAR) revealed that the NH2-group at position C3 of ring A of the chalcone scaffold played a key role in affinity, and also, the Br-atom at position C3′ on benzylidene ring B. Upon in vitro and in silico evaluation, the novel C3 amino-substituted chalcone derivative 38—that contains an α,?-unsaturated carbonyl system and easily allows structural modification—may possibly be a synthon in future drug discovery. Graphic abstract: C3 amino-substituted chalcone derivative (38) with C3′ Br substitution on benzylidene ring B possesses selective adenosine rA1 receptor affinity in micromolar range.[Figure not available: see fulltext.]

LIPOXYGENASE INHIBITORS

Various embodiments of the present disclosure are directed to compounds having Formula (I), Formula (IA), Formula (IB), Formula (IC), Formula (ID), Formula (IE), and/or pharmaceutically acceptable salts thereof. The compounds can be suitable for inhibiting lipoxygenases, and/or treating associated diseases, such as Alzheimer's disease. In some embodiments, the compounds may be administered to a patient as part of a pharmaceutical formulation.

N-Heterocyclic Carbene Catalyzed Synthesis of Trisubstituted Epoxides via Tandem Amidation/Epoxidation Sequence

A tandem amidation/epoxidation sequence between various substituted chalcones and N,N-dimethylformamide (DMF) for the synthesis of trisubstituted epoxides employing N-heterocyclic carbene catalysis was developed. This reaction was performed under metal-free conditions in the presence of tert-butyl hydroperoxide (TBHP) as the oxidant. Trisubstituted epoxides bearing a ketone and an amide functionality (N,N-dimethyl formyl group) were synthesized starting from a wide range of chalcones in moderate to good yields with excellent diastereoselectivity.

1,2-PHENYLENE BRIDGED 1-INDENYL-2-INDENYL METALLOCENE COMPLEXES FOR OLEFIN POLYMERISATION

The invention relates to a metallocene complex according to formula (I), (I) wherein R1 and R2 are independently selected from H, an alkyl or an aryl group, wherein R3 is a C1 -C10 alkyl group, wherein R' is selected from H, an alkyl group, an aryl group and wherein different R' substituents can be connected to form a ring structure and wherein B is a 1,2 phenylene bridging moiety, which can be optionally substituted, wherein Mt is selected from Ti, Zr and Hf, X is an anionic ligand, z is the number of X groups and equals the valence of Mt minus 2. The invention also relates to a catalyst comprising the reaction product of the metallocene complex and a cocatalyst. Further the invention relates to a (co)polymerisation process of olefinic monomers.

Copper-Catalyzed Multicomponent Domino Reaction of 2-Bromobenzaldehydes, Aryl Methyl Ketones, and Sodium Azide: Access to 1 H-[1,2,3]Triazolo[4,5- c]quinoline Derivatives

A practical copper-catalyzed multicomponent reaction has been developed for the synthesis of 1H-[1,2,3]triazolo[4,5-c]quinoline derivatives from commercially available 2-bromobenzaldehydes, aryl methyl ketones, and sodium azide. This protocol integrated consecutive base-promoted condensation, [3 + 2] cycloaddition, copper-catalyzed SNAr, and denitrogenation cyclization sequences. Preliminary mechanistic studies revealed that CuBr2 acted as a multifunctional catalyst to streamline this domino process. The mild catalytic system enabled effective construction of one C-C and four C-N bonds in one operation.

Synthesis of 2-Acylbenzo[b]thiophenes via Cu-Catalyzed α-C-H Functionalization of 2-Halochalcones Using Xanthate

An efficient protocol is described for the synthesis of 2-acylbenzo[b]thiophenes from easily accessible 2-iodochalcones through α-C-H functionalization using Cu(OAc)2 catalyst and xanthate as sulfur source. Less reactive 2-bromochalcones also yielded the corresponding 2-acylbenzothiophenes in good yield. The reaction proceeds via in situ incorporation of sulfur followed by copper-catalyzed cyclization to generate 2-acylbenzothiophenes without external acyl source. The synthetic importance is showcased by synthesis of 1-(5-hydroxybenzothiophene-2-yl)ethanone, which is a known pre-mRNA splicing modulator.

Silver-catalyzed decarboxylative cross-coupling of α-keto acids with alkenes giving approach to chalcones

A silver-catalyzed decarboxylative cross-coupling of α-keto acids with alkenes is reported. The method, with a wide range of substrate tolerance and mild operational conditions, can produce various chalcone derivatives in moderate to high yields from easily available starting materials.

Ortho-substituted Benzene Derivatives and Organic Light Emitting Devices Comprising The Same

The present invention relates to an ortho-substituted benzene derivative organic light-emitting compound and an organic light-emitting device including the same. The compound of the present invention is produced by respectively substituting a benzene derivative (or a carbazole derivative) and a substituted or non-substituted hetero aromatic derivative in first and second positions (ortho substitution) of benzene. High triplet energy is maintained due to a three-dimensional disorder between the ortho-substituted benzene derivative (or carbazole derivative) and the hetero aromatic detivative. A substituent having pore transporting properties is induced in the ortho-substituted benzene derivative (or carbazole derivative) and a substituent having electron transporting properties is induced in the ortho-substituted hetero aromatic derivative. Accordingly, pore injecting and transporting properties and electron injecting and transporting properties are excellent, so that the same can be usefully used as an excellent bipolar-type organic light-emitting compound. The compound of the present invention has excellent heat stability, quantum efficiency, electric current efficiency, electricity efficiency, and phosphorescent (blue, green, and red) properties, so that the same can be usefully used as an effective phosphorescent host material.COPYRIGHT KIPO 2015

One-pot synthesis of 4-substituted 1H-[1,2,3]triazolo[4,5-c]quinolines through CuO-promoted tandem cyclization reactions of (e)-3-(2-bromoaryl)-1- arylprop-2-en-1-ones with Sodium Azide

A facile and efficient protocol for the synthesis of 4-substituted-1H-[1,2, 3]triazolo[4,5-c]quinolines through a CuO-promoted tandem cyclization reaction has been developed. This method allows for the construction of two heterocyclic rings in a one-pot reaction of readily available (E)-3-(2-bromoaryl)-1-arylprop- 2-en-1-ones and sodium azide without the addition of any additive. A series of triazole-fused N-heterocyclic compounds could be prepared in moderate to good yields. Copyright

Synthesis of 2-aryl-substituted chromans by intramolecular C-O bond formation

A synthetic route for the preparation of 2-aryl-substituted chromans from commercially available starting materials and utilizing either a palladium- or copper-catalyzed intramolecular cyclization of aryl bromides is described. Chromans with stereocontrol at C-2 can thus be obtained via a palladium-catalyzed asymmetric allylic etherification procedure utilizing a chiral indole-phosphine oxazoline (IndPHOX) ligand. Georg Thieme Verlag Stuttgart · New York.