68348-23-2

Upstream product

• 626-19-7 Isophthalaldehyde 
• 107-21-1 ethylene glycol 
• 17789-14-9 3-(1,3-dioxolan-2-yl)-phenylbromide 
• 68-12-2 N,N-dimethyl-formamide 
• 1708-41-4 2-(furan-2-yl)-1,3-dioxolane 
• 107-02-8 acrolein 
• 2591-86-8 N-Formylpiperidine 

Downstream Products

• 796863-74-6 N-[4-[[3-(1,3)dioxolan-2-yl-phenyl]hydroxymethyl]-5-ethyl-2-methoxy-6-methylpyridin-3-yl]-2,2-dimethylpropionamide 
• 328543-03-9 (3-[1,3]Dioxolan-2-yl-phenyl)-8,9-dihydro-7H-2,7,9a-triaza-benzo[cd]azulen-6-one 
• 796863-75-7 3-[(3-amino-5-ethyl-6-methyl-2-oxo-1,2-dihydropyridin)-4-ylmethyl]benzaldehyde 
• 796863-88-2 3-(3-amino-5-ethyl-6-methyl-2-oxo-1,2-dihydro-pyridine-4-carbonyl)-benzaldehyde 
• 796863-99-5 3-amino-5-ethyl-4-(3-hydroxymethyl-benzoyl)-6-methyl-1H-pyridin-2-one 
• 796864-42-1 3-amino-5-ethyl-4-[3-(1-hydroxy-ethyl)-benzoyl]-6-methyl-1H-pyridin-2-one 
• 796864-37-4 2-[3-(3-amino-5-ethyl-6-methyl-2-oxo-1,2-dihydro-pyridine-4-carbonyl)-phenyl]-propionitrile 
• 796864-35-2 [3-(3-amino-5-ethyl-6-methyl-2-oxo-1,2-dihydro-pyridine-4-carbonyl)-phenyl]-acetonitrile 
• 796863-81-5 3-[3-(3-amino-5-ethyl-6-methyl-2-oxo-1,2-dihydropyridin-4-yl-carbonyl)phenyl]acrylonitrile 
• 796863-84-8 3-[3-(3-amino-5-ethyl-6-methyl-2-oxo-1,2-dihydropyridin-4-yl-carbonyl)phenyl]acrylic acid 
• 1025822-93-8 (E)-3-[3-(3-Amino-5-ethyl-6-methyl-2-oxo-1,2-dihydro-pyridine-4-carbonyl)-phenyl]-2-methyl-acrylonitrile 
• 796863-79-1 N-[5-ethyl-4-(3-formylbenzoyl)-2-methoxy-6-methylpyridin-3-yl]-2,2-dimethylpropionamide 
• 1026958-32-6 3-amino-5-ethyl-6-methyl-4-(3-phenoxymethyl-benzoyl)-1H-pyridin-2-one 
• 796864-32-9 N-[4-(3-chloromethylbenzoyl)-5-ethyl-2-methoxy-6-methylpyridin-3-yl]-2,2-dimethylpropionamide 

Relevant academic research and scientific papers

Synthesis of 16β-derivatives of 3-(2-bromoethyl)-estra-1,3,5(10)-trien-17β-ol as inhibitors of 17β-HSD1 and/or steroid sulfatase for the treatment of estrogen-dependent diseases

17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) and steroid sulfatase (STS) are involved in the synthesis of the most potent estrogen in the human body, estradiol (E2). These enzymes are known to play a pivotal role in the progression of estrogen-depen

A Combined Experimental–Theoretical Study on Diels-Alder Reaction with Bio-Based Furfural: Towards Renewable Aromatics

The synthesis of relevant renewable aromatics from bio-based furfural derivatives and cheap alkenes is carried out by using a Diels-Alder/aromatization sequence. The prediction and the control of the ortho/meta selectivity in the Diels-Alder step is an important issue to pave the way to a wide range of renewable aromatics, but it remains a challenging task. A combined experimental-theoretical approach reveals that, as a general trend, ortho and meta cycloadducts are the kinetic and thermodynamic products, respectively. The nature of substituents, both on the dienes and dienophiles, significantly impacts the feasibility of the reaction, through a modulation on the nucleo- and electrophilicity of the reagents, as well as the ortho/meta ratio. We show that the ortho/meta selectivity at the reaction equilibrium stems from a subtle interplay between charge interactions, favoring the ortho products, and steric interactions, favoring the meta isomers. This work also points towards a path to optimize the aromatization step.

(Z)-3-(3-formyl benzylidene) piperazinedione type compound and application thereof to preparation of anti-tumor medicine

The invention discloses a (Z)-3-(3-formyl benzylidene) piperazinedione type compound and application thereof to preparation of anti-tumor medicine. In a general formula (I) shown as the accompanying drawing, Rl is selected from substituted or nonsubstituted saturated nitrogen-containing multivariate heterocycles, substituted or nonsubstituted unsaturated sulfur-containing multivariate heterocycles, and substituted or nonsubstituted unsaturated oxygen containing multivariate heterocycles, and the multivariate heterocycles are 4 to 6 membered heterocycles. R2 is 5-tertiary butyl-1H-imidazole or pyridine. The invention also discloses a purpose of the compound to preparation of medicine composition aspects for treating tumor diseases, particularly, purposes to preparation of medicine compositions for treating pancreatic cancer and/or lung cancer aspects.

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.

Synthesis of optically active thromboxane A2 and Leukotriene D4 receptor antagonists

Both (+)- and (-)-4-{[(2-{4-cUorophenylsulfonylamino}-1-{3-[(Q-2-(7-cWoro- 2-quinolyl)-vinyl]phenyl}ethyl)-thio]methyl}benzoic acid (1), Thromboxane A2 and Leukotriene D4 receptor dual antagonist were synthesized. Racemic methyl 4-({[2-amino-1-(3-hydroxym

Unimolecular binary half-adders with orthogonal chemical inputs

Unimolecular half-adders based upon an arylvinyl-bipyridyl fluorophore platform were demonstrated where all the chemical input combinations were fully processed by half-adder molecules to generate the arithmetic results of the entire truth table. The Roya

CBI analogues of the duocarmycins and CC-1065

An extensive series of CBI analogues of the duocarmycins and CC-1065 exploring substituent effects within the first indole DNA binding subunit is detailed. In general, substitution at the indole C5 position led to cytotoxic potency enhancements that can be ≧1000-fold providing simplified analogues containing a single DNA binding subunit that are more potent (IC50=2-3 pM) than CBI-TMI, duocarmycin SA, or CC-1065. The increases in cytotoxicity correlate well with accompanying increases in the rate and efficiency of DNA alkylation. This effect is more pronounced with the CBI versus DSA or CPI based analogues. Moreover, this effect is largely insensitive to the electronic character of the C5 substituent but is sensitive to the size, rigid length, and shape (sp, sp2, sp3 hybridization) of this substituent consistent with expectation that the impact is due simply to its presence.

Diarylstrylquinoline diacids and pharmaceutical compositions thereof

Compounds having the formula: STR1 are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.

Chiral Porphyrins with C-Connected Menthyl Residues

Chiral porphyrins 9 and 10 with C-connected (-)-menthyl residues are prepared starting from (-)-menthol 1 in eight steps, finally involving cyclization of 3-formyl-β-(p-menth-3-yl)styrene (6) with pyrrole (7) or the 2,2'-dipyrrylmethane 8. Key Words: Porp