85366-46-7

Usage

InChI:InChI=1/C16H14O3/c17-15(12-5-2-1-3-6-12)13-7-4-8-14(11-13)16-18-9-10-19-16/h1-8,11,16H,9-10H2

Upstream product

• 17789-14-9 3-(1,3-dioxolan-2-yl)-phenylbromide 
• 100-52-7 benzaldehyde 
• 98-88-4 benzoyl chloride 
• 6919-61-5 N-methoxy-N-methylbenzamide 
• 177414-57-2 (3-[1,3]dioxolan-2-ylphenyl)phenylmethanol 

Downstream Products

• 71856-95-6 3-benzoylbenzaldehyde 
• 1056465-56-5 (3Z,6Z)-3-((5-(tert-butyl)-1H-imidazol-4-yl)methylene)-6-(3-benzoylbenzylidene)piperazine-2,5-dione 
• 177414-45-8 5-{3-[(4-Chloro-benzenesulfonylamino)-phenyl-methyl]-phenyl}-pentanoic acid methyl ester 
• 177414-58-3 2-[3-(Azido-phenyl-methyl)-phenyl]-[1,3]dioxolane 
• 1025828-33-4 5-[3-(Amino-phenyl-methyl)-phenyl]-pentanoic acid methyl ester 
• 177414-59-4 3-(Azido-phenyl-methyl)-benzaldehyde 
• 177414-57-2 (3-[1,3]dioxolan-2-ylphenyl)phenylmethanol 

Relevant academic research and scientific papers

Generation of Aryl and Heteroaryl Magnesium Reagents in Toluene by Br/Mg or Cl/Mg Exchange

The alkylmagnesium alkoxide sBuMgOR?LiOR (R=2-ethylhexyl), which was prepared as a 1.5 m solution in toluene, undergoes very fast Br/Mg exchange with aryl and heteroaryl bromides, producing aryl and heteroaryl magnesium alkoxides (ArMgOR?LiOR) in toluene. These Grignard reagents react with a broad range of electrophiles, including aldehydes, ketones, allyl bromides, acyl chlorides, epoxides, and aziridines, in good yields. Remarkably, the related reagent sBu2Mg?2 LiOR (R=2-ethylhexyl) undergoes Cl/Mg exchange with various electron-rich aryl chlorides in toluene, producing diorganomagnesium species of type Ar2Mg?2 LiOR, which react well with aldehydes and allyl bromides.

Design, synthesis and biological evaluation of anti-pancreatic cancer activity of plinabulin derivatives based on the co-crystal structure

Based on the co-crystal structures of tubulin with plinabulin and Compound 1 (a derivative of plinabulin), a total of 18 novel plinabulin derivatives were designed and synthesized. Their biological activities were evaluated against human pancreatic cancer BxPC-3 cell lines. Two novel Compounds 13d and 13e exhibited potent activities with IC50 at 1.56 and 1.72 nM, respectively. The tubulin polymerization assay indicated that these derivatives could inhibit microtubule polymerization. Furthermore, the interaction between tubulin and these compounds were elucidated by molecular docking. The binding modes of Compounds 13d and 13e were similar to the co-crystal structure of Compound 1. H-π interaction was observed between the aromatic hydrogen of thiophene moiety with Phe20, which could enhance their binding affinities.

Deuteration dehydrogenation 3-benzoyl phenyl plinabulin compound, preparation method of compound and application of compound to preparation of anti-tumor medicine

The invention provides a deuteration dehydrogenation 3-benzoyl phenyl plinabulin compound, a preparation method of the compound and application of the compound to preparation of anti-tumor medicine. The compound has the structure shown by the general formula (I). A synthesis method comprises the following steps that firstly, diacetyl piperazinedione and deuterium aldehyde compounds b take a condensation reaction to form a deuterium heterocyclic ring containing compound c; then, a condensation reaction is taken with 3-benzoyl benzaldehyde compounds to form the deuteration dehydrogenation 3-benzoyl phenyl plinabulin compound. Meanwhile, the invention also provides an efficient high-deuteration-rate deuterium aldehyde intermediate and a deuterium heterocyclic ring containing the intermediate and a synthesis method thereof, and also provides an efficient synthesis method of the deuteration dehydrogenation 3-benzoyl phenyl plinabulin compound at the same time. Experiments prove that the deuteration dehydrogenation 3-benzoyl phenyl plinabulin compound provided by the invention has the effect of inhibiting the pancreatic cancer growth. The invention provides a method for studying and developing the anti-pancreatic cancer medicine relevant to the related compound.

N-(2-ARYLETHYL) BENZYLAMINES AS ANTAGONISTS OF THE 5-HT6 RECEPTOR

The present invention relates to the use compounds of formula I which are antagonists of the 5-HT 6 receptor, for treating a cognitive disorder selected from the group consisting of age-related cognitive decline, mild cognitive impairment and dementia

Synthesis and thoromboxane A2 antagonistic activity of [[1-aryl(or benzyl)-1-(benzenesulfonamido)methyl]phenyl]alkanoic acid derivatives

In order to find a new antiasthmatic and antithrombotic agents, various [[1-aryl(or benzyl)-1-(benzenesulfonamido)methyl]phenyl]alkanoic acid derivatives were synthesized. Evaluation of these compounds for thromboxane A2 (TXA2) antag