250656-24-7

Upstream product

• 72784-67-9 N-(4-hydroxybenzilidene)-tert-butylamine 
• 767-00-0 4-cyanophenol 
• 75-65-0 tert-butyl alcohol 
• 540-88-5 acetic acid tert-butyl ester 
• 119072-55-8 tert-butylisonitrile 
• 540-38-5 p-Iodophenol 
• 28141-24-4 4-hydroxybenzoyl chloride 
• 75-64-9 tert-butylamine 

Relevant academic research and scientific papers

SSAO INHIBITOR

The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.

Oxidative C?H/C?H Cross-Coupling Reactions between N-Acylanilines and Benzamides Enabled by a Cp*-Free RhCl3/TFA Catalytic System

By making use of a dual-chelation-assisted strategy, a completely regiocontrolled oxidative C?H/C?H cross-coupling reaction between an N-acylaniline and a benzamide has been accomplished for the first time. This process constitutes a step-economic and highly efficient pathway to 2-amino-2′-carboxybiaryl scaffolds from readily available substrates. A Cp*-free RhCl3/TFA catalytic system was developed to replace the [Cp*RhCl2]2/AgSbF6 system generally used in oxidative C?H/C?H cross-coupling reactions between two (hetero)arenes (Cp=pentamethylcyclopentadienyl, TFA=trifluoroacetic acid). The RhCl3/TFA system avoids the use of the expensive Cp* ligand and AgSbF6. As an illustrative example, the procedure developed herein greatly streamlines the total synthesis of the naturally occurring benzo[c]phenanthridine alkaloid oxynitidine, which was accomplished in excellent overall yield.

Transition Metal-catalyzed Protocarboxylation of alpha-Halo-acrylic Acid Derivatives

The present invention relates to a method for the synthesis of a halo olefin of formula (I) wherein Hal, R1, R2, R3, R4, X and Y are as defined herein, or a salt thereof.

Amidation of aryl halides with isocyanides using a polymer-supported palladium-n-heterocyclic carbene complex as an efficient, phosphine-free and heterogeneous recyclable catalyst

The amidation of aryl halides with alkyl/aryl isocyanides to give the corresponding amides using polymer-supported palladium-N-heterocyclic carbene complex (PS-Pd-NHC) as an efficient heterogeneous recyclable catalyst is described. The catalytic system was optimized with respect to various reaction parameters giving excellent yields of the desired products. The catalyst can be easily separated by a simple filtration process and recycled further for up to four consecutive recycle without any loss of activity and selectivity. The protocol is advantageous due to the ease in handling of the catalyst, simple workup procedure, phosphine-free, and effective catalyst recyclability. Georg Thieme Verlag Stuttgart New York.

SO42-/CexZr1-xO2-catalyzed synthesis of N-tert-butylamides from various nitriles under solvent-free conditions

The synthesis of N-tert-butylamides using SO4 2-/CexZr1-x O2 catalysts under solvent-free conditions is reported. The methodology has several advantages such as reusability of the catalyst, solvent-free conditions, easy workup, and comparable yield of N-tert-butylamides. A variety of aliphatic, aromatic, and acid-sensitive substrates give high to moderate yields of the corresponding N-tert-butylamides. Surface acidities of the catalysts were correlated with the results obtained. To the best of our knowledge, this is the first report of a modified Ritter reaction on SO42-/CexZr1-x O2 using tert-butyl acetate as carbocationic source.

Amberlyst-15 as a recyclable heterogeneous catalyst for synthesis of N-tert-butylamides via Ritter-type reaction

Highly efficient method for the preparation of N-tert-butylamides by reaction of nitriles with tert-butylacetate is described using Amberlyst-15 as a recyclable heterogeneous catalyst. Selective amidation of benzonitrile in the presence of acetonitrile was also achieved.

Polyvinylpolypyrrolidone-supported boron trifluoride; Highly efficient catalyst for the synthesis of N-tert-butyl amides

Highly efficient method for the preparation of N-tert-butyl amides by reaction of nitriles with tert-butyl acetate is described using polyvinylpolypyrrolidone-supported boron trifluoride (PVPP-BF3) at 70 °C in good to excellent yields. Selective amidation of benzonitrile in the presence of acetonitrile was also achieved. polyvinylpolypyrrolidone-boron trifluoride complex shows non-corrosive and stable solid catalyst elevated Lewis acid property.

Synthesis of amides using the Ritter reaction with bismuth triflate catalysis

N-tert-Alkyl and aryl amides were obtained by a Ritter reaction of various nitriles with tertiary alcohols in the presence of a catalytic amount of bismuth triflate.

Rearrangement Reactions of Oxaziridines to Nitrones. X-Ray Crystal and Molecular Structure of N-t-Butyl-α(o-hydroxyphenyl)nitrone

Substituted N-benzylidene-t-butylamines are oxidized with m-chloroperoxybenzoic acid to oxaziridines which can rearrange to the corresponding nitrones when electron-donating groups are present in the phenyl ring.The oxaziridine-to-nitrone rearrangement, which has been considered as a 'pseudo-abnormal' reaction, can also be catalysed by Lewis acids.It has been found that the rearrangement of 2-t-butyl-3-(o-hydroxyphenyl)oxaziridine to the corresponding nitrone is of first order.The rearrangement has been investigated for different substituents in the phenyl ring, andin the case of 2-t-butyl-3-phenyloxaziridine substituted in the ortho position with electron-donating groups it has been found that the presence of protons of a Lewis acid is necessary.An X-ray structure of α-(o-hydroxyphenyl)-N-t-butylnitrone shows strong hydrogen bonding between the nitrone oxygen and the hydrogen in the hydroxy group.The oxaziridine-to-nitrone rearrangement is also analysed from a theoretical point of view using ab initio calculations.A Mulliken-population analysis of the C-O and N-O bonds in the oxaziridine ring for para-substitued 2-t-butyl-3-phenyloxaziridines shows a reduction of the C-O bond population when an electron-donating group is present in the para position of the phenyl ring compared with an electron-withdrawing group; the N-O bond populations show the reverse picture.A state-correlation diagram for the oxaziridine-to-nitrone rearrangement is also presented and the experimental and theoretical results support each other.