55245-17-5

Upstream product

• 75-44-5 phosgene 
• 5961-59-1 N-methyl-N-(4-methoxyphenyl)amine 
• 32315-10-9 bis(trichloromethyl) carbonate 

Downstream Products

• 100870-60-8 (4-methoxy-phenyl)-methyl-carbamic acid-[3]pyridyl ester 
• 1415333-25-3 1H-indol-6-yl 4-methoxyphenyl(methyl)carbamate 
• 1415333-76-4 methyl 3-(6-((4-methoxyphenyl)(methyl)carbamoyloxy)-1-methyl-1H-indol-3-yl)propanoate 
• 1415333-54-8 (E)-methyl 3-(6-((4-methoxyphenyl)(methyl)carbamoyloxy)-1-methyl-1H-indol-3-yl)acrylate 
• 1415333-53-7 (E)-methyl 3-(6-((4-methoxyphenyl) (methyl)carbamoyloxy)-1H-indol-3-yl)acrylate 
• 1415333-46-8 (E)-methyl 3-(4-((4-methoxyphenyl)(methyl)carbamoyloxy)-1H-indol-3-yl)acrylate 
• 1415333-39-9 3-formyl-1-methyl-1H-indol-6-yl 4-methoxyphenyl(methyl)carbamate 
• 1415333-38-8 3-formyl-1H-indol-6-yl 4-methoxyphenyl(methyl)carbamate 
• 1415333-32-2 3-formyl-1H-indol-4-yl 4-methoxyphenyl(methyl)carbamate 
• 1415333-27-5 1-methyl-1H-indol-6-yl 4-methoxyphenyl(methyl)carbamate 
• 1415333-22-0 1-methyl-1H-indol-4-yl 4-methoxyphenyl(methyl)carbamate 
• 1415334-09-6 methyl 3-(6-((4-methoxyphenyl)(methyl)carbamoyloxy)-1-methylindolin-3-yl)propanoate hydrochloride 
• 1415334-08-5 methyl 3-(6-((4-methoxyphenyl)(methyl)carbamoyloxy)indolin-3-yl)propanoate hydrochloride 
• 1415333-19-5 1H-indol-4-yl (4-methoxyphenyl)(methyl)carbamate 

Relevant academic research and scientific papers

Structure-reactivity relationships in the pyridinolysis of N-methyl-N-arylcarbamoyl chlorides in dimethyl sulfoxide

Nucleophilic substitution reactions of N-methyl-N-arylcarbamoyl chlorides (YC6H4N(CH3)COCl) with pyridines (XC5H4N) have been investigated in dimethyl sulfoxide at 45.0 °C. A striking trend in the selectivity parameters is that they are constant within experimental errors, ρX = -2.25 ± 0.03, βX = 0.42 ± 0.01, and ρX = 1.10 ± 0.06, with changing reactivities of the electrophiles (6δσY) and nucleophiles (δσX), respectively, and this leads to a vanishingly small cross-interaction constant, ρXY βXY 0. The rate data can be expressed in the Ritchie N+ type equation. Based on this and other results, the mechanism of nucleophile (pyridine) addition to the resonance- stabilized carbocation is proposed. It has been shown from the definition βXY (and ρXY) together with the Marcus equation that the high intrinsic barrier, ΔG±, in the intrinsic-barrier controlled reaction series is a prerequisite for such reactions in which the cross-interaction vanishes and the N+ relationship holds.

Chemoenzymatic Synthesis of Substituted Azepanes by Sequential Biocatalytic Reduction and Organolithium-Mediated Rearrangement

Enantioenriched 2-aryl azepanes and 2-arylbenzazepines were generated biocatalytically by asymmetric reductive amination using imine reductases or by deracemization using monoamine oxidases. The amines were converted to the corresponding N′-aryl ureas, which rearranged on treatment with base with stereospecific transfer of the aryl substituent to the 2-position of the heterocycle via a configurationally stable benzyllithium intermediate. The products are previously inaccessible enantioenriched 2,2-disubstituted azepanes and benzazepines.

Optimization of 1,2,5-thiadiazole carbamates as potent and selective ABHD6 inhibitors

At present, inhibitors of α/β-hydrolase domain 6 (ABHD6) are viewed as a promising approach to treat inflammation and metabolic disorders. This article describes the development of 1,2,5-thiadiazole carbamates as ABHD6 inhibitors. Altogether, 34 compounds were synthesized, and their inhibitory activity was tested using lysates of HEK293 cells transiently expressing human ABHD6 (hABHD6). Among the compound series, 4-morpholino-1,2,5-thiadiazol-3-yl cyclooctyl(methyl)carbamate (JZP-430) potently and irreversibly inhibited hABHD6 (IC50 = 44 nM) and showed ～ 230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL), the main off-targets of related compounds. Additionally, activity-based protein profiling indicated that JZP-430 displays good selectivity among the serine hydrolases of the mouse brain membrane proteome. JZP-430 has been identified as a highly selective, irreversible inhibitor of hABHD6, which may provide a novel approach in the treatment of obesity and type II diabetes.

PIPERIDINE UREA DERIVATIVES

Compounds of the formula I in which R1-R3 have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

INDOLE, INDOLINE DERIVATIVES, COMPOSITIONS COMPRISING THEM AND USES THEREOF

The invention provides indole and indoline derivatives and slats thereof, compositions comprising them and uses thereof for the treatment of diseases and disorders.

Unexpected zirconium-mediated multicomponent reactions of conjugated 1,3-butadiynes and monoynes with acyl cyanide derivatives

Going ber(zirc): Zirconium-butadiyne complexes react with acyl cyanide derivatives through diverse reaction pathways. The complexes react with two molecules of carbamoyl cyanide to form 1,4-benzodiazepin-2-one-derivatives containing azazirconacycles. Reac

Iridium-catalyzed annulation of N -arylcarbamoyl chlorides with internal alkynes

An iridium complex successfully catalyzed the annulation of various N-arylcarbamoyl chlorides with internal alkynes to afford 2-quinolones in good to excellent yields. The present reaction is widely applicable to substrates with various functionalities. An amide-iridacycle complex was isolated, and it is likely that such an iridacycle species is a key intermediate in the catalytic reaction.