51738-07-9Relevant academic research and scientific papers
Mild, Efficient, and Highly Regioselective Synthesis of 2,6-Diiodobenzaldehyde Derivatives
Al-Jammal, Walid K.,Al-Zoubi, Raed M.,Jaradat, Khaled T.,McDonald, Robert
, p. 953 - 958 (2020)
An efficient and versatile synthesis of 2,6-diiodobenzaldehydes via highly regioselective metal-iodine exchange (MIE) of 5-substituted 1,2,3-triiodobenzenes is reported. The nature of substituents (R) on the phenyl has a large influence on the reactivity of reaction but not on the regioselectivity. The regioselectivity of the MIE can be controlled by the use of ethyl formate as a formylating agent providing only the internal benzaldehyde derivatives in excellent site-selectivity. The best reactivity and the highest isolated yields were furnished with products bearing electron-rich substituents. Several chemical transformations of the target compound as a valuable precursor in synthesis were also demonstrated providing the desired derivatives in good isolated yields. This report discloses a protocol for the synthesis of 2,6-diiodobenzaldehyde derivatives that is scalable, general in scope, and indeed difficult to be made by other means.
Monodentate Transient Directing Group-Assisted Palladium-Catalyzed Direct ortho-C-H Iodination of Benzaldehydes for Total Synthesis of Hernandial
Chen, Xuerong,La, Ming,Liu, Dandan,Zhang, Fang-Lin,Zhou, Yirong
supporting information, p. 9184 - 9188 (2021/11/30)
The first palladium-catalyzed direct o-C-H iodination of benzaldehydes was successfully developed with the assistance of commercially available 2,5-bis(trifluoromethyl)aniline as the optimal monodentate transient directing group (MonoTDG). Moderate to exc
Palladium-Catalyzed, Norbornene-Mediated, ortho-Amination ipso-Amidation: Sequential C-N Bond Formation
Whyte, Andrew,Olson, Maxwell E.,Lautens, Mark
, p. 345 - 348 (2018/01/27)
A palladium-catalyzed, norbornene-mediated ortho- and ipso-C-N bond-forming Catellani reaction is reported. This reaction proceeds through a sequential intermolecular amination followed by intramolecular cyclization of a tethered amide. The products, ortho-aminated dihydroquinolinones, were generated in moderate to good yields and are present in bioactive molecules. This work highlights the challenge of competing intra- vs intermolecular palladium-catalyzed processes.
Synthesis and fungicidal activities of novel indene-substituted oxime ether strobilurins
Tu, Song,Xu, Long-He,Ye, Li-Yi,Wang, Xi,Sha, Yong,Xiao, Zong-Yuan
experimental part, p. 5247 - 5253 (2010/04/06)
Nineteen novel indene-substituted oxime ether strobilurins, which used an indene group to stabilize the (E)-styryl group in SYP-Z071 (an unsaturated oxime strobilurin fungicide under development by the Shenyang Research Institute of Chemical Industry), were designed and synthesized. The biological assay results showed that all compounds possessed good or excellent fungicidal activities. It was found that most of the compounds showed higher fungicidal activities against Pyricularia oryzae, Phytophthora infestans, Erysiphe graminis, and Colletotrichum lagenarium than SYP-Z071 at the tested concentration. The biological assay results also indicated that most of the compounds exhibited higher in vivo fungicidal activities against cucumber Pseudoperonospora cubensis and C. lagenarium than the commercial fungicides trifloxystrobin and kresoxim-methyl at a concentration of 6.25 mg/L. Furthermore, it was found that α-(methoxyimino)-N-methylphenylacetamide oxime ethers 6m-s exhibited a broad spectrum and remarkably higher activities against all tested fungi. Especially, the 6-methylindene-substituted compound 6p was identified as the most promising candidate for further study.
Method for the treatment of CNS disorders with substituted 2-imidazoles or imidazole derivatives
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Page/Page column 58, (2010/11/28)
The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, R1, R2, A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.
