75059-30-2

Upstream product

• 18362-51-1 1,3-bis(4'-methoxyphenyl)propane-1,3-dione 
• 76973-45-0 3,5-di(4-methoxyphenyl)-2-pyrazoline 
• 123-11-5 4-methoxy-benzaldehyde 
• 2373-89-9 4,4'-dimethoxychalcone 
• 100-07-2 4-methoxy-benzoyl chloride 
• 768-60-5 4-methoxyphenylacetylen 
• 65418-71-5 1,3-bis-(4-methoxyphenyl)-2-ethynyl-1-one 
• 46318-58-5 4-methoxybenzoylnitromethane 
• 5953-85-5 p-anisaldehyde hydrazone 
• 4181-97-9 phenyl 4-methoxybenzoate 
• 41564-67-4 (E)-1,3-bis(4-methoxyphenyl)-2-propene-1-one 
• 94-30-4 ethyl 4-methoxybenzoate 
• 105782-42-1 (2RS,3SR)-2,3-epoxy-1-(4-methoxyphenyl)-3-(4-methoxyphenyl)propan-1-one 
• 563-41-7 semicarbazide hydrochloride 

Downstream Products

• 207689-35-8 [Au(3,5-bis(4'-methoxyphenyl)pyrazolate)]3 
• 234093-22-2 1,2,5-tri-(4-anisyl)-1H-pyrazole 

Relevant academic research and scientific papers

Synthesis, structure and acetylcholinesterase inhibition activity of new diarylpyrazoles

A variety of diarylpyrazole derivatives III-VI were synthesized and structurally characterized using FTIR, 1H and 13C NMR spectroscopy, and in case of compound VIb by X-ray single crystal analysis. The in vitro biological studies rev

Denitrative imino-diaza-Nazarov cyclization: Synthesis of pyrazoles

An iodine-catalyzed denitrative imino-diaza-Nazarov cyclization (DIDAN) methodology has been developed for the synthesis of pyrazoles with high to excellent yields by using α-nitroacetophenone derivatives and in situ generated hydrazones. The key transformation of this oxidative 4π-electrocyclization proceeds through an enamine-iminium ion intermediate. This rapid one-pot DIDAN protocol results in the selective generation of C-C and C-N bonds and cleavage of a C-N bond. This journal is

A highly efficient heterogeneous palladium-catalyzed cascade three-component reaction of acid chlorides, terminal alkynes and hydrazines leading to pyrazoles

In the presence of 0.5 mol% of 3-(2-aminoethylamino)propyl-functionalized MCM-41-immobilized palladium(II) complex [MCM-41-2N-Pd(OAc)2] and 1.0 mol% of CuI, acid chlorides were coupled with terminal alkynes in Et3N at 50 °C to give α,β-unsaturated ynones, which were converted in situ into pyrazoles by the cycloaddition of hydrazines at room temperature with acetonitrile as cosolvent. The cascade reactions generated a variety of pyrazole derivatives in moderate to good yields, and this heterogeneous palladium catalyst exhibited higher catalytic activity than PdCl2(PPh3)2 and could be recovered and reused for at least 10 consecutive trials without any decreases in activity.

Transition-Metal-Free N-Arylation of Pyrazoles with Diaryliodonium Salts

A new synthetic method was developed for the N-arylation of pyrazoles using diaryliodonium salts. The transformation does not require any transition-metal catalyst and provides the desired N-arylpyrazoles rapidly under mild reaction condition in the presence of aqueous ammonia solution as a mild base without the use of inert atmosphere. The chemoselectivity of unsymmetric diaryliodonium salts was also explored with large number of examples.

One-pot synthesis of 3,5-diphenyl-1h-pyrazoles from chalcones and hydrazine under mechanochemical ball milling

A highly efficient and environmentally friendly method has been developed for facile synthesis of 3,5-diphenyl-1H-pyrazoles under mechanochemical ball-milling conditions. The advantages of short reaction time, high efficiency, no separation of in situ generated intermediate, using cheap sodium persulfate as the oxidant, together with very simple work-up procedure, make this one-pot and solvent-free protocol a green and powerful alternative to traditional methods for the synthesis of these kinds of compounds.

17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS FOR THE TREATMENT OF HORMONE-RELATED DISEASES

The invention relates to 17beta-hydroxysteroid dehydrogenase type 1 (17betaHSD1) inhibitors, the preparation thereof and the use thereof for the treatment and prophylaxis of hormone-related, especially estrogen-related or androgen-related, diseases.

New one step synthesis of 3,5-disubstituted pyrazoles under microwave irradiation and classical heating

(Chemical Equation Presented) A convenient one pot procedure for the synthesis of 3,5-disubstituted pyrazoles by condensation of chalcones, hydrazine hydrate and sulfur in ethanol under microwave irradiation and conventional heating method is reported. The hydrogen sulfide is produced during the reaction. The pyrazoles are obtained in good yields and excellent state of purity. The structures of new compounds were confirmed by IR, 1H, and 13C NMR, MS and elemental analysis.

Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases

The 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyses the reduction of the weakly active estrone (E1) into the most potent estrogen, 17β-estradiol (E2). E2 stimulates the growth of hormone-dependent diseases via activation of the estrogen receptors (ERs). 17β-HSD1 is often over-expressed in breast cancer cells. Thus, it is an attractive target for the treatment of mammary tumours. The combination of a ligand- and a structure-based drug design approach led to the identification of bis(hydroxyphenyl) azoles as potential inhibitors of 17β-HSD1. Different azoles and hydroxy substitution patterns were investigated. The compounds were evaluated for activity and selectivity with regard to 17β-HSD2, ERα and ERβ. The most potent compound is 3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]phenol (18, IC50 = 0.31 μM), showing very good selectivity, high cell permeability and medium CaCo-2 permeability.

A facile and convenient approach to the synthesis of 3,5-diaryl-1H- pyrazoles

A simple and convenient one-pot synthesis route is described for the synthesis of 3,5-diaryl-1H-pyrazoles in short reaction times from the reaction of α-epoxyketones with semicarbazide hydrochloride under mild conditions.