172035-83-5

Upstream product

• 10486-61-0 3-thienyl iodide 
• 51934-41-9 4-iodobenzoic acid ethyl ester 
• 872-31-1 3-Bromothiophene 
• 5798-75-4 Ethyl 4-bromobenzoate 
• 4334-88-7 p-ethoxycarbonylphenylboronic acid 
• 6165-69-1 Thien-3-ylboronic acid 
• 17249-80-8 3-chlorothiophene 

Downstream Products

• 337459-25-3 4-(2,5-dibromothiophene-3-yl)benzoic acid ethyl ester 

Relevant academic research and scientific papers

New efficient preparation of functionalized arylzinc or thienylzinc compounds from aryl or thienyl chlorides using cobalt catalysis

A new chemical method is described for the preparation of aryl or thienyl zinc intermediates from their corresponding aromatic or thienyl chlorides in a mixture of acetonitrile-pyridine, using cobalt catalysis. This procedure allows for the synthesis of a

Preparation and coupling reaction of thienylmanganese bromides

3-Thienylmanganese bromide, 3-bromo-4-thienylmanganese bromide and 4-substituted 3-thienylmanganese bromides were prepared from the reactions of Rieke manganese with 3-bromothiophene, 3,4-dibromothiophene and 4-substituted 3-bromothiophenes, respectively. The resulting thienylmanganese bromides underwent cross-coupling reactions under mild reaction conditions.

One-step highly selective borylation/Suzuki cross-coupling of two distinct aryl bromides in pure water

A Na2PdCl4-catalysed B2(OH)4-mediated direct cross-coupling of two distinct aryl bromides in pure water is described. This one-step borylation/Suzuki method exhibits an outstanding cross-coupling selectivity and no tendency to produce homocoupling products, therefore leading to biaryls and heterobiaryls in moderate to good yields. Moreover, the reaction has high regio-selectivity and can be scaled-up. Using such a simple, economical and practical protocol, the unsymmetrical diarylation of 3,5-dibromopryidine is achieved.

Efficient cobalt-catalyzed formation of unsymmetrical biaryl compounds and its application in the synthesis of a sartan intermediate

(Chemical Equation Presented) No prior preparation of the organometallic reagent is required in a cobalt-catalyzed coupling of two different aryl halides under mild conditions (see scheme). A broad spectrum of valuable biaryl compounds can be prepared in this way. Not only may a variety of reactive substituents be present, but heteroaryl halides and aryl triflates are also suitable substrates. DMF = N,N-dimethylformamide, FG = functional group.

Chromatography-free suzuki reactions using a Polymer-Assisted Solution-Phase (PASP) approach

An efficient Suzuki coupling protocol that affords reaction products in high purity without the need for chromatography or aqueous work-up is reported. The reaction, which utilises a combination of polymer-supported reagents, can be performed under thermal or microwave heating conditions and is particularly suited to parallel synthesis. Georg Thieme Verlag Stuttgart.

New carboxamide compounds having melanin concentrating hormone antagonistic activity, pharmaceutical preparations comprising these compounds and process for their manufacture

The present invention relates to carboxamide compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1, R2, R3 and k have the meanings given in claim 1. Moreover the invention relates to process for preparing the above mentioned carboxamides as well as pharmaceutical compositions containing at least one carboxamide according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

Synthesis of unsymmetrical biaryls by electroreductive cobalt-catalyzed cross-coupling of aryl halides

The consumable anode process allows the electrochemical cross-coupling reaction between various functionalized aromatic halides (iodides, bromides and chlorides) in the presence of cobalt halides as catalyst in a mixed solvent acetonitrile/pyridine (9:1). A great variety of unsymmetrical biaryls are obtained in moderate to excellent yields.

Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment

This invention encompasses the novel compounds of formula A, which are useful in the treatment of prostaglandin mediated diseases, or a pharmaceutically acceptable salt, hydrate or ester thereof. The invention also encompasses certain pharmaceutical compositions and methods for treatment of prostaglandin mediated diseases comprising the use of compounds of formula A.

New and efficient access to 3-substituted 2,5-dibromothiophenes. Consecutive nickel-catalyzed electrochemical conversion to thienylzinc species

We have achieved the stepwise synthesis of 3-substituted thienylzinc reagents using both electrochemical methods and an original bromination procedure. For several compounds 3-bromothiophene was the starting substrate, which was functionalized according to recently developed electrochemical procedures. The nickel-catalyzed electrochemical reduction of the resulting 3-substituted 2,5-dibromothiophenes in the presence of zinc salts allowed the formation of monothienylzinc species in good yields. The selectivity of this reaction is discussed within the context of the electrochemical synthesis of regioregular polythiophenes.

Direct Preparation of 3-Thienyl Organometallic Reagents: 3-Thienylzinc and 3-Thienylmagnesium Iodides and 3-Thienylmanganese Bromides and Their Coupling Reactions

3-Thienylzinc and 3-thienylmagnesium iodides can be generated from the direct oxidative addition of Rieke zinc and magnesium to 3-iodothiophene, respectively. The direct preparation of 3-thienylmanganese bromides from the reaction of Rieke manganese with 3-bromothiophene and 3,4-dibromothiophene is also performed. These 3-thienyl organometallic reagents have been found to be regiostable intermediates and undergo coupling reactions with a variety of versatile electrophiles such as acid chlorides, aryl iodides, aldehydes, and disulfide.