169956-61-0

Upstream product

• 524-38-9 N-hydroxyphthalimide 
• 108-93-0 cyclohexanol 
• 870-50-8 di-tert-butyl (E)-azodicarboxylate 
• 953-91-3 cyclohexyl tosylate 
• 110-82-7 cyclohexane 
• 76029-42-0 2-(cyclohex-2-en-1-yloxy)isoindoline-1,3-dione 
• 1521-51-3 rac-3-bromocyclohexene 
• 108-85-0 1-bromocyclohexane 

Downstream Products

• 54488-64-1 O-cyclohexylhydroxylamine hydrochloride 
• 1033779-97-3 (E)-2-[2-(3-chloro-4-methanesulfonyl-phenyl)-2-cyclohexyloxyimino-acetylamino]-thiazole-5-carboxylic acid amide 
• 1033779-96-2 (E)-N-benzothiazol-2-yl-2-(3-chloro-4-methanesulfonyl-phenyl)-2-cyclohexyloxyimino-acetamide 
• 1033779-95-1 (E)-2-(3-chloro-4-methanesulfonyl-phenyl)-2-cyclohexyloxyimino-N-(3-methyl-[1,2,4]thiadiazol-5-yl)-acetamide 
• 1033779-94-0 (E)-2-(3-chloro-4-methanesulfonyl-phenyl)-2-cyclohexyloxyimino-N-(1-methyl-1H-pyrazol-3-yl)-acetamide 
• 1033780-23-2 (E)-(3-chloro-4-methanesulfonyl-phenyl)-cyclohexyloxyimino-acetic acid 
• 1170231-07-8 N-benzyl-O-cyclohexylhydroxylamine 
• 1170235-60-5 (R)-2-benzyl-7-(2-cyano-1-(pyridin-4-yl)guanidino)-N-(cyclohexyloxy)heptanamide 
• 1170235-52-5 (S)-2-benzyl-7-(2-cyano-1-(pyridin-4-yl)guanidino)-N-(cyclohexyloxy)heptanamide 
• 1170235-48-9 (R)-7-(2-cyano-1-(pyridin-4-yl)guanidino)-N-(cyclohexyloxy)-2-methylheptanamide 
• 1170235-59-2 (S)-7-(2-cyano-1-(pyridin-4-yl)guanidino)-N-(cyclohexyloxy)-2-methylheptanamide 

Relevant academic research and scientific papers

Copper-Catalyzed Domino Reactions for the Synthesis of Phenothiazines

A method for the one-pot synthesis of phenothiazines from benzothiazoles and aryl ortho-dihalides was explored. Preliminary work on the mechanism of the reaction suggested that it follows a domino process, including the hydrolysis of benzothiazoles followed by C-S coupling and C-N coupling. The low loading of the catalyst system (5 mol-% for both copper and ligand), the mild experimental conditions (90 °C, 12 h), and the use of a green reaction medium make this synthesis very attractive to academia and industry. A copper-catalyzed domino reaction consisting of the hydrolysis of benzothiazoles followed by C-S and C-N couplings for the synthesis of phenothiazines from benzothiazoles and aryl ortho-dihalides is described. The low loading of the catalyst system, mild experimental conditions, and the use of polyethylene glycol as the solvent make this synthetic approach very attractive to academia and industry.

Copper nitrate-catalyzed oxidative coupling of unactivated C(sp3)-H bonds of ethers and alkanes with: N -hydroxyphthalimide: Synthesis of N -hydroxyimide esters

A copper nitrate-catalyzed cross-dehydrogenative coupling reaction between N-hydroxyphthalimide (NHPI) and ethers/alkanes has been described. The reaction is accomplished smoothly by using simple and green molecular oxygen as the oxidant, providing an alternative for the efficient synthesis of N-alkoxyphthalimides. In addition, it was found that when tert-butyl ethers were used as substrates, unexpected N-hydroxyimide ester derivatives were obtained in moderate to excellent yields. To further understand this unusual transformation, control experiments were performed and a plausible mechanism was proposed.

Copper(II)-catalyzed cross dehydrogenative coupling reaction of N-hydroxyphthalimide with alkanes and ethers via unactivated C(sp3)-H activation at room temperature

A copper(ii)-catalyzed cross dehydrogenative coupling reaction between N-hydroxyphthalimide and unactivated C(sp3)-H bonds of alkanes and ethers using Selectfluor as an oxidant is described. This efficient reaction system shows mild conditions and a broad substrate scope for the generation of O-substituted N-hydroxyphthalimide derivatives.

A New Dioxazolone for the Synthesis of 1,2-Aminoalcohols via Iridium(III)-Catalyzed C(sp3)?H Amidation

Vicinal aminoalcohols are widespread structural motifs in bioactive molecules. We report the development of a new dioxazolone reagent containing a p-nitrophenyldifluoromethyl group, which 1. displays a good safety profile; 2. shows a remarkably high react

Carbon-hydrogen bond activation method for non-metal participated inert alkane

The invention discloses an activation method of a non-metal catalyzed inert alkane carbon-hydrogen bond. The activation method comprises the following steps: S1, dissolving a compound inert alkane andN-hydroxyphthalimide into dichloromethane; S2, adding iodobenzene acetate into the system; S3, after N-hydroxyphthalimide disappears, carrying out reduced pressure distillation on the reaction systemto remove the low-boiling-point organic solvent; and S4, carrying out silica gel column chromatography separation to obtain the compound I. The method disclosed by the invention comprises the step ofadding the inert alkane compound into a solvent system of iodobenzene acetate and Nhydroxyphthalimide, so that the reaction condition is mild, heating is not needed, no metal participates, the methodis simple and efficient, the post-treatment is simple, inert gas or oxygen conditions are not needed, and the development concept of green chemistry is met.

Ligand-Enabled β-Methylene C(sp3)?H Arylation of Masked Aliphatic Alcohols

Despite recent advances, reactivity and site-selectivity remain significant obstacles for the practical application of C(sp3)?H bond functionalization methods. Here, we describe a system that combines a salicylic-aldehyde-derived L,X-type directing group with an electron-deficient 2-pyridone ligand to enable the β-methylene C(sp3)?H arylation of aliphatic alcohols, which has not been possible previously. Notably, this protocol is compatible with heterocycles embedded in both alcohol substrates and aryl coupling partners. A site- and stereo-specific annulation of dihydrocholesterol and the synthesis of a key intermediate of englitazone illustrate the practicality of this method.

Selective C(sp3)?H and C(sp2)?H Fluorination of Alcohols Using Practical Auxiliaries

Selective introduction of fluorine into molecules by the cleavage of inert C?H bonds is of central academic and synthetic interest, yet remains challenging. Given the central role of alcohols in organic chemistry as the most ubiquitous building blocks, a

NOVEL VASCULAR LEAKAGEAGE INHIBITOR

The present disclosure relates to a novel vascular leakage inhibitor. The novel vascular leakage inhibitor of the present invention inhibits the apoptosis of vascular endothelial cells, inhibits the formation of actin stress fibers induced by VEGF, and enhances the cortical actin ring structure, thereby inhibiting vascular leakage. Accordingly, the vascular leakage inhibitor of the present invention can prevent or treat various diseases caused by vascular leakage. Since the vascular leakage inhibitor of the present invention is synthesized from commercially available or easily synthesizable pregnenolones, it has remarkably superior feasibility of commercial synthesis.

Design, Synthesis, and invitro Antibacterial Activity of Fluoroquinolone Derivatives Containing a Chiral 3-(Alkoxyimino)-2-(aminomethyl)azetidine Moiety

A series of novel (R)/(S)-7-(3-alkoxyimino-2-aminomethyl-1-azetidinyl)fluoroquinolone derivatives were synthesized and evaluated for their invitro antibacterial activity against representative strains. Our results reveal that 12 of the target compounds generally show better activity (MIC: -1) against the tested Gram-positive strains including MRSA and MRSE than levofloxacin (LVFX, MIC: 0.125-8μgmL-1). Their activity is similar to that of gemifloxacin (GMFX, MIC: -1). However, they are generally less active than the two reference drugs against Gram-negative strains. Moreover, against clinical strains of S.aureus including MRSA and S.epidermidis including MRSE, the MIC50 values (0.06-16μgmL-1) and MIC90 values (0.5-32μgmL-1) of compounds 16w, y, and z are 2-8- and 2-16-fold less than LVFX, respectively, and 16w (MIC90 range: 0.5-4μgmL-1) was also found to be more active than GMFX (MIC90 range: 1-8μgmL-1).

CONTROLLED RELEASE OF ACTIVE COMPOUNDS FROM DYNAMIC MIXTURES

The present invention relates to a dynamic mixture in the form of a dynamic mixture obtained by reacting together, in the presence of water, at least one O-substituted hydroxylamine or S-substituted thiohydroxylamine derivative with at least one perfuming