103440-52-4Relevant academic research and scientific papers
Mechanochemical-Cascaded C-N Cross-Coupling and Halogenation Using N-Bromo- And N-Chlorosuccinimide as Bifunctional Reagents
Bera, Shyamal Kanti,Mal, Prasenjit
, p. 14144 - 14159 (2021)
Exploration of alternative energy sources for chemical transformations has gained significant interest from chemists, and mechanochemistry is one of those sources. Herein, we report the use of N-bromosuccinimides (NBS) and N-chlorosuccinimides (NCS) as bifunctional reagents for a cascaded C-N bond formation and subsequent halogenation reactions. Under the solvent-free mechanochemical (ball-milling) conditions, the synthesis of a wide range of phenanthridinone derivatives from N-methoxy-[1,1′-biphenyl]-2-carboxamides is accomplished. During the reactions, NBS and NCS first assisted the oxidative C-N coupling reaction and subsequently promoted a halogenation reaction. Thus, the role of NBS and NCS was established to be bifunctional. Overall, a mild, solvent-free, convenient, one-pot, and direct synthesis of various bromo- and chloro-substituted phenanthridinone derivatives was achieved.
Immobilized Iodosobenzoate Catalysts for the Cleavage of Reactive Phosphates
Moss, Robert A.,Chung, Yong-Chan
, p. 2064 - 2069 (1990)
Titanium dioxide and nylon covalently supported iodosobenzoate reagents 11 and 19 have been prepared by the procedures outlined in Schemes I and II.Both 11 and 19 are good catalysts for the cleavage of p-nitrophenyl diphenyl phosphate (PNPDPP) under heter
Method for preparing iodo-benzoic acid (ester) by improving moral Michael reaction
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, (2021/11/03)
The invention discloses a method for preparing iodo-benzoic acid (ester) by improving a moral reaction, and belongs to the technical field of organic synthesis. The method comprises the following steps: preparing and separating the diazonium tetrafluoroborate through diazotization of aminobenzoic acid (ester) and then performing iodination reaction with the iodinated reagent in an organic medium to obtain the corresponding iodo carboxylic acid (ester). The iodo-benzoic acid (ester) prepared by the method has high purity. The method has the advantages of good quality and simple post-treatment, and the product yield reaches 70 - 90%.
BORON-CONTAINING PHARMACOPHORE
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Paragraph 0207; 0209, (2021/01/29)
Provided herein are boron-containing compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders.
Crystal form of orexin receptor antagonist compound, and preparation method and application thereof
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Page/Page column 13; 19-20, (2020/06/26)
Disclosed are a preparation method of an orexin receptor antagonist compound 5-3, Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of the preparing the orexin receptor antagonist compound 5-3 a
QUINAZOLINE-2,4-DIONE DERIVATIVES AS PARP INHIBITORS
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Page/Page column 62, (2020/11/30)
The present invention relates to compounds of formula (I) and compositions containing said compounds acting as PARP (Poly (ADP- ribose) polymerase) inhibitors. Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine, in particular for the treatment of cell proliferative disorders, such as cancer.
Facile synthesis of phthalides from methyl ortho-iodobenzoates and ketones via an iodinemagnesium exchange reaction using a silylmethyl Grignard reagent
Nakamura, Yu,Yoshida, Suguru,Hosoya, Takamitsu
supporting information, p. 858 - 861 (2017/06/13)
Phthalides have been easily prepared by the treatment of methyl o-iodobenzoates with a silylmethyl Grignard reagent in the presence of ketones. The electron-withdrawing ester moiety of methyl o-iodobenzoates and the low nucleophilicity of the silylmethyl Grignard reagent prompted a smooth iodinemagnesium exchange reaction, at room temperature, without affecting the ester moiety or resulting in an undesired reaction with electrophilic ketones. This simple method, wherein special control of the reaction temperature was unnecessary, has allowed the synthesis of various phthalides, including a phenolphthalein derivative.
Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping Approach
Heidmann, Bibia,Gatfield, John,Roch, Catherine,Treiber, Alexander,Tortoioli, Simone,Brotschi, Christine,Williams, Jodi T.,Bolli, Martin H.,Abele, Stefan,Sifferlen, Thierry,Jenck, Fran?ois,Boss, Christoph
, p. 2132 - 2146 (2016/10/25)
Starting from suvorexant (trade name Belsomra), we successfully identified interesting templates leading to potent dual orexin receptor antagonists (DORAs) via a scaffold-hopping approach. Structure–activity relationship optimization allowed us not only to improve the antagonistic potency on both orexin 1 and orexin 2 receptors (Ox1 and Ox2, respectively), but also to increase metabolic stability in human liver microsomes (HLM), decrease time-dependent inhibition of cytochrome P450 (CYP) 3A4, and decrease P-glycoprotein (Pgp)-mediated efflux. Compound 80 c [{(1S,6R)-3-(6,7-difluoroquinoxalin-2-yl)-3,8-diazabicyclo[4.2.0]octan-8-yl}(4-methyl-[1,1′-biphenyl]-2-yl)methanone] is a potent and selective DORA that inhibits the stimulating effects of orexin peptides OXA and OXB at both Ox1 and Ox2. In calcium-release assays, 80 c was found to exhibit an insurmountable antagonistic profile at both Ox1 and Ox2, while displaying a sleep-promoting effect in rat and dog models, similar to that of the benchmark compound suvorexant.
PYRROLE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Paragraph 0420, (2015/02/19)
Compounds of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, R5 and T are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
USE OF BENZIMIDAZOLE-PROLINE DERIVATIVES
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Page/Page column 18, (2015/06/18)
The present invention relates to compounds of the formula (I), wherein Ar1 and Ar2 are as described in the description and to their use as pharmaceuticals for the treatment of sundown syndrome. The invention also relates to the preparation of such compounds and of pharmaceutically acceptable salts thereof.
