81245-32-1Relevant academic research and scientific papers
2-(3-Hydroxybenzyl)benzo[d]isothiazol-3(2H)-one Mannich base derivatives as potential multifunctional anti-Alzheimer’s agents
He, Yuxi,Xiao, Ganyuan,Yu, Guangjun,Song, Qing,Zhang, Heng,Liu, Zhuoling,Tan, Zhenghuai,Deng, Yong
, p. 1249 - 1264 (2021/05/11)
A series of 2-(3-hydroxybenzyl)benzo[d]isothiazol-3(2H)-one Mannich base derivatives were designed as potential multifunctional agents against Alzheimer’s disease. The twelve derivatives were synthesized and evaluated with various biological activities. I
Enantioselective total synthesis of (+)-stephadiamine through bioinspired aza-benzilic acid type rearrangement
Odagi, Minami,Matoba, Taisei,Hosoya, Keisuke,Nagasawa, Kazuo
supporting information, p. 2699 - 2704 (2021/03/01)
We report the first enantioselective total syntheses of the hasubanan alkaloid (-)-metaphanine and the norhasubanan alkaloid (+)-stephadiamine. Key features of these syntheses include diastereoselective oxidative phenolic coupling reaction and subsequent
Nucleophilic Substitutions of Alcohols in High Levels of Catalytic Efficiency
Stach, Tanja,Dr?ger, Julia,Huy, Peter H.
supporting information, p. 2980 - 2983 (2018/05/28)
A practical method for the nucleophilic substitution (SN) of alcohols furnishing alkyl chlorides, bromides, and iodides under stereochemical inversion in high catalytic efficacy is introduced. The fusion of diethylcyclopropenone as a simple Lewis base organocatalyst and benzoyl chloride as a reagent allows notable turnover numbers up to 100. Moreover, the use of plain acetyl chloride as a stoichiometric promotor in an invertive SN-type transformation is demonstrated for the first time. The operationally straightforward protocol exhibits high levels of stereoselectivity and scalability and tolerates a variety of functional groups.
HYDANTOIN DERIVATIVES USEFUL AS KV3 INHIBITORS
-
Paragraph 0765-0768, (2013/10/22)
The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
Photochemical generation of oxa-dibenzocyclooctyne (ODIBO) for metal-free click ligations
McNitt, Christopher D.,Popik, Vladimir V.
supporting information, p. 8200 - 8202,3 (2020/09/09)
Oxa-dibenzocyclooctynes (ODIBO, 2a-c) are prepared by photochemical decarbonylation of corresponding cyclopropenones (photo-ODIBO, 1a-c). While photo-ODIBO does not react with azides, ODIBO is one of the most reactive cyclooctynes exhibiting rates of cycloaddition over 45 M-1 s -1 in aqueous solutions. ODIBO is stable under ambient conditions and has low reactivity towards thiols. Photo-ODIBO survives heating up to 160 °C and does not react with thiols.
HYDANTOIN DERIVATIVES USEFUL AS KV3 INHIBITORS
-
Page/Page column 108-109, (2012/06/30)
The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists
Asada, Masaki,Obitsu, Tetsuo,Nagase, Toshihiko,Sugimoto, Isamu,Yamaura, Yoshiyuki,Sato, Kazutoyo,Narita, Masami,Ohuchida, Shuichi,Nakai, Hisao,Toda, Masaaki
experimental part, p. 6567 - 6582 (2009/12/09)
A series of acrylic acids and their structurally related compounds were evaluated for their binding affinity to four EP receptor subtypes (EP1-4). Starting from the initial hit 3, which was discovered in our in-house library, compounds 4 and 5 were identified as new chemical leads as candidates for further optimization towards a selective EP3 receptor antagonist. The identification process of these compounds and their pharmacokinetic profiles are presented.
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists
Ando, Makoto,Sekino, Etsuko,Haga, Yuji,Moriya, Minoru,Ito, Masahiko,Ito, Junko,Iwaasa, Hisashi,Ishihara, Akane,Kanatani, Akio,Ohtake, Norikazu
scheme or table, p. 5186 - 5190 (2010/03/24)
Novel phenethylpyridone derivatives were identified as potent human melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. A search for surrogates for the 4-(2-aminoethoxy)phenyl moiety of 1 resulted in discovery of 2-[4-(aminomethyl)phenyl]ethyl substructure as in 6a. Successive optimization of the right-hand moiety led to the identification of a number of potent derivatives.
SUBSTITUTED PHENETHYLAMINES
-
Page/Page column 29-30, (2009/01/20)
Disclosed herein are substituted phenethylamine alpha adrenergic receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
4-amino-thieno[3,2-c] pyridine-7-carboxylic acid derivatives
-
Page/Page column 36, (2010/11/26)
The present invention relates to compounds of the formula medicaments containing them and the use of these compounds as pharmaceutically active agents. The compounds exhibit activity as Raf kinase inhibitors and therefore may be useful for the treatment of diseases mediated by said kinases, especially as anticancer agents.
