94283-73-5

Upstream product

• 6314-88-1 1,2,5,6-tetrahydrobenzaldehyde diethyl acetal 
• 100-50-5 3-Cyclohexene-1-carboxaldehyde 
• 67-63-0 isopropyl alcohol 
• 75-30-9 2-iodo-propane 
• 139-85-5 3,4-dihydroxybenzaldehyde 
• 75-26-3 isopropyl bromide 
• 100-44-7 benzyl chloride 

Downstream Products

• 94283-74-6 4-isopropoxy-3-tosyloxybenzaldehyde 
• 16562-14-4 (-)-stepholidine 

Relevant academic research and scientific papers

FOURTH-GENERATION EGFR TYROSINE KINASE INHIBITOR

Provided is a compound having a tyrosine kinase inhibitory activity specific to C797S resistant mutant EGFR (particularly C797S tertiary-resistant mutant EGFR) and is useful as a C797S resistant mutant EGFR (particularly C797S mutant tertiary-resistant EG

NOVEL BENZYLIDENEACETONE DERIVATIVE AND USE THEREOF

The present invention relates to novel benzylideneacetone derivatives or uses thereof, more specifically, the present invention relates to a pharmaceutical composition for preventing or treating, or food composition for ameliorating a cancer or a bone disease comprising a compound defined by Formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. Since compounds according to the present invention exhibit strong inhibitory activity on proliferation and differentiation of osteoclast, and activity on proliferation and differentiation of osteoblast, it can be usefully used to develop safe and effective anti-cancer agents, and therapeutic agents for preventing and treating or foods for ameliorating bone diseases including osteoporosis, and the like.

Benzylideneacetone Derivatives Inhibit Osteoclastogenesis and Activate Osteoblastogenesis Independently Based on Specific Structure-Activity Relationship

(E)-3,4-Dihydroxybenzylideneacetone (compound 1) inhibited receptor activator of NF-κB ligand-induced osteoclastogenesis of C57BL/6 bone marrow monocyte/macrophages with IC50 of 7.8 μM (IC50 of alendronate, 3.7 μM) while stimulating the differentiation of MC3T3-E1 osteoblastic cells, accompanied by the induction of Runt-related transcription factor 2, alkaline phosphatase, and osteocalcin. (E)-4-(3-Hydroxy-4-methoxyphenyl)-3-buten-2-one (compound 2c) showed a dramatically increased osteoclast-inhibitory potency with IC50 of 0.11 μM while sustaining osteoblast-stimulatory activity. (E)-4-(4-Hydroxy-3-methoxyphenyl)-3-buten-2-one (compound 2g) stimulated alkaline phosphatase production 2-fold at 50 μM without changing osteoclast-inhibitory activity, compared with compound 1. Oral administration of compounds 1, 2c, and 2g prevented ovariectomy-induced osteoporosis in ddY mice to a degree proportional to their osteoclastogenesis-inhibitory potencies. The administration of 1 (mg/kg)/d compound 2c ameliorated histomorphometry of osteoporotic bone to a degree comparable with 10 (mg/kg)/d alendronate. Conclusively, the in vitro capacity of a few benzylideneacetone derivatives to inhibit osteoclastogenesis supported by independent osteoblastogenesis activation was convincingly reflected in in vivo management of osteoporosis, suggesting a potential novel therapeutics for osteopenic diseases.

Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant

A series of A-ring-modified lamellarin N analogues were designed, synthesized, and evaluated as potential noncovalent inhibitors of the EGFR T790M/L858R mutant, a causal factor in the drug-resistant non-small cell lung cancer. Several water-soluble ammonium- or guanidinium-tethered analogues exhibited good kinase inhibitory activities. The most promising analogue, 14f, displayed an excellent inhibitory profile against the T790M/L858R mutant [IC50 (WT) = 31.8 nM; IC50 (T790M/L858R) = 8.9 nM]. The effects of A-ring-substituents on activity were rationalized by docking studies.

A (3 - alkoxy - 4 - hydroxy) - cyclohexyl acetal glycol and its isomers of use

The present invention discloses a (3-alkoxy-4-hydroxy)-cyclohexyl methylal diol, an (3-hydroxy-4-alkoxy)-cyclohexyl methylal diol and synthesis methods and use therefor. The (3-alkoxy-4-hydroxy)-cyclohexyl methylal diol and (3-hydroxy-4-alkoxy)-cyclohexyl methylal diol can be used for synthesis of a variety of vanillin and iso-vanillin. Compared to the existing synthetic method, the synthesis method has simple steps, and less discharge of "three wastes".

A 3, 4 - epoxy-cyclohexane METHYLAL glycol and its synthesis and use

The invention discloses a 3,4-epoxy cyclohexyl methylal diol and a synthesis method thereof. The 3,4-epoxy cyclohexyl methylal diol can be used for synthesizing multiple vanillins and isovanillins. Compared with the existing synthesis process, the synthesis method disclosed by the invention has the advantages of simple steps and low discharge amount of three wastes.

Synthesis of 2,3,9,10-Tetraoxygenated benzo[c]phenanthridine derivatives via palladiummediated aryl-Aryl coupling reaction

Two 2,3,9,10-Tetraoxygenated benzo[c]phenanthridine alkaloids, 1 2, originally reported as zanthoxyline and broussonpapyrine, respectively, were synthesized using the Pd-mediated intramolecular aryl-Aryl coupling reaction as the key step.

Preparation method for stepholidine and derivatives thereof

The invention provides a preparation method for stopholidine and derivatives thereof. Specifically, the method comprises the following steps: with a chemical compound as shown in a formula A as an intermediate, carrying out B-N cyclization/sodium borohydride reduction reaction and cyclization reaction so as to obtain a skeleton of a stepholidine compound, wherein definitions of all groups are described in the specification. The method provided by the invention has the advantages of simple operation of related reactions, high yield, cheap reagents, and facilitation to enlargement of the preparation method for methylphenethylamine compounds as shown in a general formula I, and specifically for o-bromobenzeneacetic acid compounds corresponding to 9,10-substituted modes, so the method is applicable to large-scale preparation for optically pure stepholidine or the derivatives thereof.

MONOCYCLIC PYRIDINE DERIVATIVE

The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or —CH2—; E represents a nitrogen-containing non-aromatic heterocycle; R1 represents an alkoxy group or the like; R2 represents a hydrogen atom or the like; and R3 represents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and R2 or R3 is present on a nitrogen atom on the azetidine ring, the R2 or R3 does not represent a hydrogen atom.

Total synthesis of plagiochin D by an intramolecular SNAr reaction

The total synthesis of plagiochin D, a macrocyclic bis(bibenzyl) compound isolated from the liverwort plagiochila acanthophylla, has been accomplished. Closure of the key 16-membered ring, which contained biphenyl ether and biaryl units, was achieved in good yield by an intramolecular SNAr reaction. The Suzuki and Wittig protocols proved to be powerful tools for the construction of a linear precursor that was crucial for ring cyclization. Copyright