769-30-2Relevant articles and documents
Amide derivatives and their medical use
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, (2018/04/21)
The invention relates to novel amide derivatives shown in a structural formula I in the specification or a pharmaceutically acceptable salt thereof, a medicine composition which takes the compounds as active components, and an application of the derivatives or the pharmaceutically acceptable salt of the derivatives to preparation of analgesia medicines. In the structural formula I, R1 and R2 are a hydrogen atom and a C1-C3 alkyl; R3 is hydrogen atom, C1-C3 alkyl, phenyl or a hydroxyl-substituted alkyl.
Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase
Lingel, Andreas,Sendzik, Martin,Huang, Ying,Shultz, Michael D.,Cantwell, John,Dillon, Michael P.,Fu, Xingnian,Fuller, John,Gabriel, Tobias,Gu, Justin,Jiang, Xiangqing,Li, Ling,Liang, Fang,McKenna, Maureen,Qi, Wei,Rao, Weijun,Sheng, Xijun,Shu, Wei,Sutton, James,Taft, Benjamin,Wang, Long,Zeng, Jue,Zhang, Hailong,Zhang, Maya,Zhao, Kehao,Lindvall, Mika,Bussiere, Dirksen E.
supporting information, p. 415 - 427 (2017/04/26)
PRC2 is a multisubunit methyltransferase involved in epigenetic regulation of early embryonic development and cell growth. The catalytic subunit EZH2 methylates primarily lysine 27 of histone H3, leading to chromatin compaction and repression of tumor suppressor genes. Inhibiting this activity by small molecules targeting EZH2 was shown to result in antitumor efficacy. Here, we describe the optimization of a chemical series representing a new class of PRC2 inhibitors which acts allosterically via the trimethyllysine pocket of the noncatalytic EED subunit. Deconstruction of a larger and complex screening hit to a simple fragment-sized molecule followed by structure-guided regrowth and careful property modulation were employed to yield compounds which achieve submicromolar inhibition in functional assays and cellular activity. The resulting molecules can serve as a simplified entry point for lead optimization and can be utilized to study this new mechanism of PRC2 inhibition and the associated biology in detail.
Practical and chemoselective reduction of acyl chloride to alcohol by borohydride in aqueous dichloromethane
Rajan, Ramya,Badgujar, Sachin,Kaur, Kamaljit,Malpani, Yashwardhan,Kanjilal, Pranab R.
experimental part, p. 2897 - 2907 (2010/11/18)
A simple methodology for the reduction of acid chlorides to their corresponding alcohols has been developed. Various carboxylic acids were converted to alcohols in excellent yields using NaBH4-K2CO3 in a mixed solvent system of dichloromethane and water (1:1) in the presence of a phase-transfer catalyst at low temperature. The importance of the work is its simplicity, selectivity, excellent yield, and very short reaction time. This new reduction condition has proved to be an excellent chemoselective method for a range of acid chlorides in the presence of various functional groups.
Green and efficient procedure for the trimethylsilylation of hydroxy groups and their regeneration using sulfamic acid as recyclable catalyst
Rostami, Amin,Ahmad-Jangi, Firoz,Zarebin, Mohammad Rezgar,Akradi, Jamal
experimental part, p. 1500 - 1507 (2010/07/15)
Structurally diverse alcohols and phenols were efficiently transformed into their corresponding trimethylsilyl ethers with hexamethyldisilazane (HMDS) in the presence of catalytic amounts of sulfamic acid (SA) at room temperature under both acetonitrile and solvent-free conditions. Deprotection of these trimethylsilyl ethers to their parent alcohols and phenols was also achieved using this catalyst in water at room temperature. Copyright Taylor & Francis Group, LLC.
Boric acid as cost-effective and recyclable catalyst for trimethylsilyl protection and deprotection of alcohols and phenols
Rostami, Amin,Akradi, Jamal,Ahmad-Jangi, Firoz
experimental part, p. 1587 - 1592 (2010/11/04)
Boric acid has been used as a green, selective and recyclable catalyst for trimethysilylation of alcohols and phenols using hexamethyldisilazane in acetonitrile. Deprotection of trimethylsilyl ethers to their parent alcohols and phenols was also achieved using this catalyst in water at room temperature. The salient features of this methodology are cheap processing, mild acidity conditions, excellent yields of products and easy availability of the catalyst.
P-toluenesulfonyl chloride (p-TsCl)-catalyzed trimethylsilylation of hydroxyl groups using hexamethyldisilazane and their regeneration under mild conditions: The first example for catalytic application of p-toluenesulfonyl chloride
Khazaei, Ardeshir,Rostami, Amin,Mantashlo, Fatemeh
experimental part, p. 2288 - 2296 (2010/04/06)
The first catalytic application of p-toluenesulfonyl chloride (p-TsCl) for the efficient and selective trimethylsilylation of various types of hydroxyl groups with hexamethyldisilazane (HMDS) in dichloromethane and desilylation of these compounds in water is reported. The reactions were carried out at room temperature and were found to proceed in good to excellent yields.
ARYL FLUOROETHYL UREAS ACTING AS ALPHA 2 ADRENERGIC AGENTS
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Page/Page column 29, (2008/12/07)
The invention provides well-defined aryl fluoroethyl ureas that are useful as selective alpha2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of alpha2 adrenergic receptors.
Practical synthesis of biaryl colchicinoids containing 3′,4′- catechol ether-based A-rings via Suzuki cross-coupling with ligandless palladium in water
Deveau, Amy Morin,Macdonald, Timothy L.
, p. 803 - 807 (2007/10/03)
Eight new biaryl colchicinoids containing 3′,4′-methylene or benzodioxy ether bridges were synthesized. The key synthetic step employed a ligandless, aqueous Suzuki cross-coupling reaction catalyzed by Pd(OAc) 2 with tetrabutylammonium bromide (TBAB) and potassium carbonate (K2CO3). The biaryl Suzuki products were typically formed in 5-30min and always in less than 1h.
Nonsteroidal antiinflammatory agents
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Page 9, (2010/02/08)
The invention relates to compounds of general formula I and their use for the production of pharmaceutical agents for treatment and prophylaxis of diseases that coincide with inflammatory, allergic and/or proliferative processes.
BENZOFURAN AND BENZOTHIOPHENE DERIVATIVES USEFUL IN THE TREATMENT OF HYPER-PROLIFERATIVE DISORDERS
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Page/Page column 17-18, (2008/06/13)
This invention relates to novel benzofuran and benzothiophene derivatives of the general formula and their use for the treatment of hyper-proliferative disorders.
