31835-64-0

Upstream product

• 13331-27-6 m-nitrobenzene boronic acid 
• 591-19-5 m-Bromoaniline 
• 121-73-3 3-Nitrochlorobenzene 
• 210907-84-9 3-aminophenylboronic acid pinacolate 
• 108-42-9 3-chloro-aniline 
• 68716-48-3 4,4,5,5-tetramethyl-2-(3-nitrophenyl)-1,3,2-dioxaborolane 
• 20442-79-9 3-iodo-1,1'-biphenyl 
• 645-00-1 m-iodonitrobenzene 
• 123-91-1 1,4-dioxane 
• 958-96-3 3,3'-dinitro-1,1'-biphenyl 
• 64-17-5 ethanol 
• 7783-06-4 hydrogen sulfide 
• 7664-41-7 ammonia 
• 108-88-3 toluene 

Downstream Products

• 438247-96-2 4-[3-(3-Nitrophenyl)anilino]-2-(3-pyridinyl)-6-(trifluoromethyl)pyrimidine 

Relevant academic research and scientific papers

DIARYLUREAS AS CB1 ALLOSTERIC MODULATORS

The present invention provides novel diarylurea derivatives (compounds of formula (I)) and their uses. The compounds of the present invention are demonstrated to be allosteric modulators of the CB1 receptor, and therefore useful for the treatment of diseases and conditions mediated by CB1.

Room-temperature borylation and one-pot two-step borylation/Suzuki-Miyaura cross-coupling reaction of aryl chlorides

A highly efficient room-temperature borylation strategy of aryl chlorides is described. Utilizing Buchwald's second-generation preformed catalyst, boronate esters were obtained for a wide range of substrates in high yield. The method was also applied to Suzuki-Miyaura cross-coupling reaction in a one-pot two-step sequential manner, providing a facile and convenient access to the direct synthesis of biaryl compounds from aryl chlorides.

Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution

Allosteric modulators of the cannabinoid CB1 receptor have recently been reported as an alternative approach to modulate the CB1 receptor for therapeutic benefits. In this study, we report the design and synthesis of a series of diarylureas derived from PSNCBAM-1 (2). Similar to 2, these diarylureas dose-dependently inhibited CP55,940-induced intracellular calcium mobilization and [35S]GTP-γ-S binding while enhancing [3H]CP55,940 binding to the CB1 receptor. Structure-activity relationship studies revealed that the pyridinyl ring of 2 could be replaced by other aromatic rings and the pyrrolidinyl ring is not required for CB1 allosteric modulation. 34 (RTICBM-74) had similar potencies as 2 in all in vitro assays but showed significantly improved metabolic stability to rat liver microsomes. More importantly, 34 was more effective than 2 in attenuating the reinstatement of extinguished cocaine-seeking behavior in rats, demonstrating the potential of this diarylurea series as promising candidates for the development of relapse treatment of cocaine addiction.

Cyclic imino derivatives and pharmaceutical compositions containing them

The invention relates to cyclic imino compounds which have, inter alia, valuable pharmacological properties, especially inhibitory effects on cell aggregation, pharmaceutical compositions which contain these compounds and processes for preparing them.

Syntheses and Physical Properties of Several Octiphenyls and a Septiphenyl

Six symmetrical linear octiphenyls were synthesized by the Ullmann homo-coupling reaction of iodoquaterphenyl.Another satisfactory method for synthesizing octiphenyls is also described, i.e., a Kharash-type Grignard cross-coupling of biphenylylmagnesium bromide and diiodoquaterphenyl in the presence of bis(acetylacetonato)nickel(II).Moreover, m-septiphenyl was succesfully synthesized by deamination of the corresponding amino compound.Infrared studies of the polyphenyls indicated that the fine-structure bands in the regions of 770-810 and 870-915 cm-1 may be considered as indicators of the presence of consecutive m-phenylene rings, regardless of the existence of o- or p-phenylene rings.The ultraviolet spectra of the octiphenyls, which contain two kinds of linkages, showed absorption curves closely related to those of quaterphenyls corresponding to the structural units of the former compounds.The nuclear magnetic resonance spectra of the polyphenyls without an o-phenylene ring showed multiplet peaks due to the resonances of an isolated m-phenylene proton at the lowest field within a narrow region (δ 7.81-7.95).Hueckel molecular orbital calculations of the longest wavelength absorption bands of ten polyphenyls were carried out.The calculated and observed wavelengths were in rather good agreement except for the cases of three compounds.Keywords - Ullmann reaction; Ni-complex-catalyzed cross-coupling; octiphenyls; septiphenyls; IR; UV; NMR; MO; quaterphenyl derivatives; polyphenyls