157134-36-6

Upstream product

• 589-15-1 1-bromomethyl-4-bromobenzene 
• 108-59-8 malonic acid dimethyl ester 
• 1122-91-4 4-bromo-benzaldehyde 
• 52927-45-4 dimethyl 2-(4-bromobenzylidene)malonate 
• 41841-16-1 (4-bromo-phenyl)-acetic acid methyl ester 
• 616-38-6 carbonic acid dimethyl ester 

Downstream Products

• 706811-25-8 5-(4-bromophenyl)-4,6-dihydroxypyrimidine 
• 25574-11-2 3-(4-bromophenyl)propanol 
• 607744-36-5 4-(3-(4-bromophenyl)propyl)morpholine 
• 607744-33-2 3-(4-bromophenyl)-1-morpholinopropan-1-one 
• 55394-81-5 3-(4-bromophenyl)propanoyl chloride 
• 1643-30-7 3-(4-bromophenyl)propionic acid 
• 92013-18-8 2-[(4-bromophenyl)methyl]propanedioic acid 

Relevant academic research and scientific papers

Photoredox/Nickel Dual Catalysis Enables the Synthesis of Alkyl Cyclopropanes via C(sp3)-C(sp3) Cross Electrophile Coupling of Unactivated Alkyl Electrophiles

A facile synthesis of mono-, 1,1- and 1,2-disubstituted cyclopropanes via visible light-mediated photoredox/nickel dual catalysis is demonstrated. The challenging intramolecular C(sp3)-C(sp3) cross-electrophile coupling of readily available unactivated 1,3-dialkyl electrophiles was performed under mild conditions that allowed traditionally reactive functional groups to be included. Mechanistic inspection and control experiments revealed the importance of dual catalysis and that the reaction proceeds via a stepwise oxidative addition followed by an intramolecular SN2 reaction.

Reductive Knoevenagel Condensation with the Zn-AcOH System

An efficient gram-scale one-pot approach to 2-substituted malonates and related structures is developed, starting from commercially available aldehydes and active methylene compounds. The technique combines Knoevenagel condensation with the reduction of the C=C bond in the resulting activated alkenes with the Zn-AcOH system. The relative ease with which the C=C bond reduction occurs can be traced to the accepting abilities of the substituents in the intermediate arylidene malonates.

Synthetic method for macitentan drug intermediate

The invention discloses a synthetic method for a macitentan drug intermediate. The synthetic method for the macitentan drug intermediate comprises the following raw material components: 20-30 parts ofanhydrous methanol, 6-8 parts of 4-bromophenylacetic acid, 8-10 parts of sulfonyl chloride, 20-40 parts of sodium methoxide, 10-15 parts of dimethyl carbonate, 5-10 parts of formamidine hydrochloride, 60-80 parts of phosphorus oxychloride (newly evaporated) and 1-2 parts of N,N-dimethylaniline. According to the provided synthetic scheme, synthetic raw materials are simple, the purity of the obtained product is higher than that of like products, and the requirement for keeping synthesizing macitentan can be met.

SUBSTITUTED BENZAMIDES AND THEIR USES

Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.

A robust and simple protocol for the synthesis of arylfluorophosphonates

Fluorophosphonates represent powerful probes for the identification and analysis of active serine hydrolases in activity based protein profiling. Although alkylphosphonofluoridates are widely used for such purposes, little is known about the synthesis and purification of arylphosphonofluoridates, which may be useful tools for screening enzyme activities toward aromatic esters. Our optimized route makes this subclass of transition state inhibitors broadly accessible for a diverse series of phosphonic acid derivatives using a combination of selective monoesterification with EDC·HCl and subsequent mild fluorination with DAST. All compounds were isolated as pure materials using a simple acid-base extraction protocol in 76-93% yields over two steps. These probes can be stored under an inert atmosphere at -24 °C for several months without significant degradation.

SUBSTITUTED BENZAMIDES AND THEIR USES

Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.

PYRAZOLO [1,5-A]PYRIMIDINES AS INHIBITORS OF STEAROYL-COA DESATURASE

The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, which are useful as inhibitors of human stearoyl-CoA desaturase (SCD). The invention further relates to pharmaceutical compositions comprising these c

Phosphonic acids derivatives as inhibitors of protein tyrosine phosphate 1B (PTP-1B)

The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases.