1722-10-7Relevant articles and documents
One-Pot and Two-Chamber Methodologies for Using Acetylene Surrogates in the Synthesis of Pyridazines and Their D-Labeled Derivatives
Ananikov, Valentine P.,Ledovskaya, Maria S.,Polynski, Mikhail V.
, p. 2286 - 2297 (2021/07/20)
Acetylene surrogates are efficient tools in modern organic chemistry with largely unexplored potential in the construction of heterocyclic cores. Two novel synthetic paths to 3,6-disubstituted pyridazines were proposed using readily available acetylene surrogates through flexible C2 unit installation procedures in a common reaction space mode (one-pot) and distributed reaction space mode (two-chamber): (1) an interaction of 1,2,4,5-tetrazine and its acceptor-functionalized derivatives with a CaC2?H2O mixture performed in a two-chamber reactor led to the corresponding pyridazines in quantitative yields; (2) [4+2] cycloaddition of 1,2,4,5-tetrazines to benzyl vinyl ether can be considered a universal synthetic path to a wide range of pyridazines. Replacing water with D2O and vinyl ether with its trideuterated analog in the developed procedures, a range of 4,5-dideuteropyridazines of 95–99% deuteration degree was synthesized for the first time. Quantum chemical modeling allowed to quantify the substituent effect in both synthetic pathways.
Microwave-enhanced efficient synthesis of some polyfunctional pyridazines
Kumar Jangid,Yadav,Yadav
, p. 1165 - 1173 (2013/10/21)
Microwave-enhanced highly efficient protocol for the synthesis of polyfunctional pyridazines beginning from 3,6-dichloropyridazine in environmentally benign ionic liquids have been developed. The products obtained were 3-amino-6-chloropyridazine, 3,6-diaminopyridazine, and 3-chloro-6- methoxypyridazine. These derivatives were then be converted to a variety of polyfunctional pyridazine derivatives. The ionic liquids used were 1-n-butyl-3-methylimidazolium hydroxide/tetrafluoroborate/hexafluorophosphate and 1,3-di-n-butylimidazolium hydroxide. This powerful strategy is less time-consuming green methodology. The ionic liquid employed may be recovered and recycled.
2-ARYLBENZOTHIOPHENE DERIVATIVES OR PHARCEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARCEUTICAL COMPOSITION FOR THE DIAGNOSIS OR TREATMENT OF DEGENERATIVE BRAIN DISEASE CONTAINING THE SAME AS ACTIVE INGREDIENT
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Page/Page column 31, (2010/11/03)
2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as an active ingredient. Since the 2-arylbenzothiophene derivatives of Formula 1 have a relatively high binding affinity for β-amyloid, they can be used as diagnostic reagents for diagnosing Alzheimer's disease at an early stage by non-invasive techniques when they are labeled with radioisotopes: wherein R1-R4, V, W, X, Y and Z are as defined in the Detailed Descript of the specification. Further, when the pharmaceutical composition containing the 2-arylbenzothiophene derivative binds with a low-molecular weight β-amyloid peptide binding compound, generation of malignant high-molecular weight β-amyloid deposits is minimized. Accordingly, the pharmaceutical composition can be used as a therapeutic agent of degenerative brain disease such as Alzheimer's disease.
