336620-03-2

Upstream product

• 201230-82-2 carbon monoxide 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 1122-91-4 4-bromo-benzaldehyde 
• 15226-74-1 dicobalt octacarbonyl 
• 15164-44-0 p-(iodophenyl)carboxaldehyde 
• 16173-52-7 4-formylbenzoyl chloride 
• 619-66-9 4-Carboxybenzaldehyde 
• 1117-97-1 N,0-dimethylhydroxylamine 

Downstream Products

• 1608150-40-8 C₂₄H₂₂BF₂N₅O₂ 
• 1608150-43-1 C₃₁H₂₈BF₂N₅O₃ 
• 1608150-41-9 C₂₂H₁₇BF₂N₄O 
• 1608150-42-0 C₃₅H₃₆BF₂N₅O₃ 
• 1618091-73-8 (E)-N-methoxy-N-methyl-4-(3-oxobut-1-en-1-yl)benzamide 
• 227078-24-2 (E)-4-(4-(hydroxymethyl)phenyl)but-3-en-2-one 
• 623-27-8 terephthalaldehyde, 
• 1357255-96-9 4-(1-hydroxy-1-phenylethyl) benzaldehyde 
• 80463-21-4 4-(1-hydroxyethyl)benzaldehyde 
• 132654-10-5 (+)-4-(1-hydroxyethyl)-benzaldehyde 
• 3457-45-2 p-formylacetophenone 
• 20912-50-9 4-benzoylbenzaldehyde 
• 52010-95-4 4-(1-hydroxy-1-phenylmethyl)benzaldehyde 

Relevant academic research and scientific papers

QUINOLINE DERIVATIVES AND USES IN MANAGING CANCER

Provided herein are compounds, pharmaceutical compositions including such compounds, and methods of using such compounds to treat diseases or disorders associated with MDM2 activity.

Discovery of N-(3,4-Dimethylphenyl)-4-(4-isobutyrylphenyl)-2,3,3a,4,5,9b-hexahydrofuro[3,2- c]quinoline-8-sulfonamide as a Potent Dual MDM2/XIAP Inhibitor

Murine double minute 2 (MDM2) and X-linked inhibitor of apoptosis protein (XIAP) are important cell survival proteins in tumor cells. As a dual MDM2/XIAP inhibitor reported previously, compound MX69 has low potency with an IC50 value of 7.5 μM against an acute lymphoblastic leukemia cell line EU-1. Herein, we report the structural optimization based on the MX69 scaffold, leading to the discovery of a 25-fold more potent analogue 14 (IC50 = 0.3 μM against EU-1). We demonstrate that 14 maintains its mode of action by dual targeting of MDM2 and XIAP through inducing MDM2 protein degradation and inhibiting XIAP mRNA translation, respectively, which resulted in cancer cell growth inhibition and cell death. The results strongly suggest that the scaffold based on 14 is promising for further optimization to develop a new therapeutic agent for leukemia and possibly other cancers where MDM2 and XIAP are dysregulated.

Synthesis of various acylating agents directly from carboxylic acids

A straightforward synthesis of acylating reagents such as Weinreb and MAP amides from aromatic, aliphatic carboxylic acids, and amino acids using PPh3/NBS combination is described. A chemo-selective modification of the carboxylic acid group into Weinreb amide in the presence of more reactive aldehydes and ketones is presented. All reactions were performed at ambient temperature under air using undried commercial grade solvent. Furthermore, the present methodology could be performed at a gram scale under inert-free reaction conditions. In addition, 7-azaindoline amide auxiliary (used for catalytic asymmetric aldol- and Mannich-type reactions), which behaves like Weinreb amide is also synthesized under similar reaction conditions.

Synthesis, evaluation, and biological applications of visible-light-controllable nitric oxide releasers

Nitric oxide (NO) is biologically synthesized in human body and mediates various signal pathway. Because NO is too unstable to handle for biological assay, NO releasers had been developed for NO research. Among them, light-controllable NO releasers are quite useful tool because their NO release can be spatiotemporally controlled by light irradiation. This article shows how to synthesize visible-light controllable NO releasers based on N-nitrosoaminophenol structure, evaluate NO releasing efficiency in various methods, and apply them for biological experiments.

N-NITROSOANILINE DERIVATIVE, NO GENERATOR USING THE SAME, AND GENERATION METHOD OF NO

PROBLEM TO BE SOLVED: To provide an N-nitrosoaniline derivative not containing a poisonous metal, capable of discharging nitrogen monoxide (NO) by irradiation of visible light, and to provide an NO generator using the same, and a generation method of NO. SOLUTION: An N-nitrosoaniline derivative has a pyrromethene boron complex structure shown by following formula 1 synthesized by combining together, for example, 2-(5-amino-2-hydroxyphenyl)-propionate ester, 2,4-dimethyl-3-cyanopyrrole and 4-formylbenzoic acid. COPYRIGHT: (C)2015,JPO&INPIT

One-Pot Direct Synthesis of Weinreb Amides from Aryl and Hetero Aryl Halides Using Co 2(CO) 8 as an Effective CO Source under Conventional Thermal Heating

A successful protocol for the synthesis of Weinreb amides directly from aryl halides via aminocarbonylation with N,O-dimethyl hydroxylamine using Co2(CO)8 as an in situ CO source has been demonstrated. The effects of various reaction parameters such as temperature, base, and CO source have also been investigated and optimized. GRAPHICAL ABSTRACT.

Photomanipulation of vasodilation with a blue-light-controllable nitric oxide releaser

Spatiotemporally controllable nitric oxide (NO)-releasers allow us to analyze the physiological effects of NO, a gaseous mediator that modulates many biological signaling networks, and are also candidate chemotherapeutic agents. We designed and synthesized a blue-light-controllable NO releaser, named NOBL-1, which bears an N-nitrosoaminophenol moiety for NO release tethered to a BODIPY dye moiety for harvesting blue light. Photoinduced electron transfer from N-nitrosoaniline to the antenna moiety upon irradiation with relatively noncytotoxic blue light (470-500 nm) should result in NO release with formation of a stable quinone moiety. NO release from NOBL-1 was confirmed by ESR spin trapping and fluorescence detection. Spatially controlled NO release in cells was observed with DAR-4M AM, a fluorogenic NO probe. We also demonstrated temporally controlled vasodilation of rat aorta ex vivo by blue-light-induced NO release from NOBL-1. This compound should be useful for precise examination of the functions of NO with excellent spatiotemporal control.

An Efficient synthesis of Weinreb amides and ketones via palladium nanoparticles on ZIF-8 catalysed carbonylative coupling

Heterogeneously catalysed carbonylative coupling reactions such as aminocarbonylation and Suzuki-carbonylation are reported using Pd nanoparticles supported on ZIF-8 for efficient and environmentally attractive synthesis of Weinreb amides and ketones from aryl bromides or iodides. The catalyst is air stable, offers high activity with very low palladium leaching and is recyclable. The presence of a phosphine ligand was required when aryl bromides were used as substrates, while no ligand was necessary when aryl iodides were used. the Partner Organisations 2014.

One-pot transition-metal-free synthesis of weinreb amides directly from carboxylic acids

Weinreb amides were prepared directly from carboxylic acids, N,O-dimethylhydroxylamine, and phosphorus trichloride in one pot at 60 °C in toluene in high yields, thus avoiding the separation of the moisture and air sensitive intermediate P[NMe(OMe)]3 in advance. Sterically hindered carboxylic acids also give the corresponding Weinreb amides in excellent yields. Various functional groups are tolerated on the carboxylic acid. The method, which is a simple process and gives high yields, is suitable for large-scale production. Georg Thieme Verlag KG Stuttgart · New York.