- Cycloaddition of annulated cyclohexa-2,4-dienones and novel reduction of halogen at bridgehead: an expedient route to tetracyclo[6.5.2.02,7.09,13]pentadec-2(7),11-dien-14-one and framework of conidiogenol and conidiogenone
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An expedient route to tetracyclo[6.5.2.02,7.09,13]pentadec-2(7),11-dien-14-one and tetracyclic framework of conidiogenol have been reported. Cycloaddition of annulated cyclohexa-2,4-dienone with cyclopentadiene, photochemical oxa-di-π-methane reaction and a highly unusual dehalogenation of bridgehead halogen are the key features of our methodology.
- Singh, Vishwakarma,Singh, Raj Bahadur,Mobin, Shaikh M.
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- Enantioselective Ni-Catalyzed Electrochemical Synthesis of Biaryl Atropisomers
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A scalable enantioselective nickel-catalyzed electrochemical reductive homocoupling of aryl bromides has been developed, affording enantioenriched axially chiral biaryls in good yield under mild conditions using electricity as a reductant in an undivided cell. Common metal reductants such as Mn or Zn powder resulted in significantly lower yields in the absence of electric current under otherwise identical conditions, underscoring the enhanced reactivity provided by the combination of transition metal catalysis and electrochemistry.
- Chen, Song,Chen, Yue-Gang,Gao, Pei-Sen,Liu, Dong,Ma, Hong-Xing,Mei, Tian-Sheng,Qiu, Hui,Shuai, Bin,Wang, Yun-Zhao
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supporting information
p. 9872 - 9878
(2020/06/27)
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- Regioselective and Chemoselective Reduction of Naphthols Using Hydrosilane in Methanol: Synthesis of the 5,6,7,8-Tetrahydronaphthol Core
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A regioselective and chemoselective method for catalytic synthesis of biologically interesting 5,6,7,8-tetrahydronaphthols by reduction of naphthols was described. The side aromatic hydrocarbons in naphthols were site-selectively reduced, using hydrosilanes in methanol, allowing for retaining functional phenol scaffolds intact. It presents a rare example of using low-cost and air-stable hydrosilane for catalytic reduction of unactivated aromatic hydrocarbons under mild conditions. This reaction is scalable and proceeds in high selectivity without the formation of 1,2,3,4-tetrahydronaphthol byproducts with toleration of sensitive functionalities such as bromide, chloride, fluoride, ketone, ester, and amide.
- He, Yuan,Tang, Jinghua,Luo, Meiming,Zeng, Xiaoming
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supporting information
p. 4159 - 4163
(2018/07/29)
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- Experimental and Theoretical Investigations of the Bromination of Phenols with β and γ Aliphatic Substituents, including Rings
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Bromination reactions of substituted and ring fused phenols were studied by both experiment (t-BuNH-Br) and computation (density functional theory). The outcomes support each other, indicating a clear and predictable regioselective preference among 3,4-bis-alkylated and 3,4-ring-fused phenols.
- Zhang, Jinsong,Chang, Xiao,Bowman, Erich C.,Holt, Carter J.,Lodewyk, Michael W.,Miller, Randy M.,Xia, Guangming
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p. 9292 - 9296
(2015/09/28)
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- ORGANIC COMPOUNDS
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Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer (such as prostate or breast cancer), osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
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Page/Page column 81
(2010/11/27)
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- Synthesis and biological evaluation of new 2-(4,5-dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives
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2-(4,5-Dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives and tricyclic analogues with a fused additional ring on the nitrogen atom of the benzoxazine moiety have been prepared and evaluated for their cardiovascular effects as potential antihypertensive agents. The imidazoline ring was generated by reaction of the corresponding ethyl ester with ethylenediamine. Affinities for imidazoline binding sites (IBS) I1 and I2 and α1 and α2 adrenergic receptors were evaluated as well as the effects on mean arterial blood pressure (MAP) and heart rate (HR) of spontaneously hypertensive rats. With few exceptions the most active compounds on MAP were those with high affinities for IBS and α2 receptor. Among these, compound 4h was the most interesting and is now, together with its enantiomers, under complementary pharmacological evaluation.
- Touzeau, Frédérique,Arrault, Axelle,Guillaumet, Gérald,Scalbert, Elizabeth,Pfeiffer, Bruno,Rettori, Marie-Claire,Renard, Pierre,Mérour, Jean-Yves
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p. 1962 - 1979
(2007/10/03)
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- SUBSTITUTED PYRAZINE DERIVATIVES
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The present invention provides substituted pyrazine derivatives of Formula (I), that are CRF1 receptor antagonists, including human CRF1 receptors. This invention also relates to use of compounds of the invention for treating a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders, particularly anxiety-related disorders and mood disorders.
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Page/Page column 55
(2010/02/07)
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- Synthesis and biological activities of new 2-substituted 1,4-benzoxazine derivatives
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A series of new 1,4-benzoxazine derivatives (XI, XII) possessing (4-phenyl-1-piperazinyl)alkyl moieties at the 2-position and related compounds (XIII) were synthesized and tested for calcium antagonistic, calmodulin antagonistic and antihypertensive activ
- Kajino,Shibouta,Nishikawa,Meguro
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p. 2896 - 2905
(2007/10/02)
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