- Synthesis of oxazolidin-2-ones and imidazolidin-2-ones directly from 1,3-diols or 3-amino alcohols using iodobenzene dichloride and sodium azide
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A general and efficient method for the synthesis of oxazolidin-2-ones and imidazolidin-2-ones directly from 1,3-diols and 3-amino alcohols has been developed using the same reagent combination of iodobenzene dichloride (PhICl2) and sodium azide (NaN3).
- He, Tian,Gao, Wen-Chao,Wang, Wei-Kun,Zhang, Chi
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supporting information
p. 1113 - 1118
(2014/04/03)
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- β-aryl nitrile construction via palladium-catalyzed decarboxylative benzylation of α-cyano aliphatic carboxylate salts
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The palladium-catalyzed decarboxylative benzylation of α-cyano aliphatic carboxylate salts with benzyl electrophiles was discovered. This reaction exhibits good functional group compatibility and proceeds under relatively mild conditions. A diverse range of quaternary, tertiary and secondary β-aryl nitriles can be conveniently prepared by this method. Copyright
- Shang, Rui,Huang, Zheng,Xiao, Xiao,Lu, Xi,Fu, Yao,Liu, Lei
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supporting information
p. 2465 - 2472,8
(2020/08/31)
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- Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists
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The pharmacokinetic based optimisation of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB1 receptor is disclosed. Compound 24 was found to be a highly potent and selective cannabinoid CB1 antagonist with high
- Cowley, Phillip M.,Baker, James,Buchanan, Kirsteen I.,Carlyle, Ian,Clark, John K.,Clarkson, Thomas R.,Deehan, Maureen,Edwards, Darren,Kiyoi, Yasuko,Martin, Iain,Osbourn, Dawn,Walker, Glenn,Ward, Nick,Wishart, Grant
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scheme or table
p. 2034 - 2039
(2011/05/02)
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- Efficient preparation of α,α-dialkyl-α-(phenylselanyl) acetates and α,β-unsaturated esters from the corresponding α,α-dialkyl-α-cyanoacetates by a lithium naphthalenide induced reductive selenenylation process
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An array of α,α-dialkyl-α-(phenylselanyl)acetates has been synthesized very efficiently from readily available α,α- dialkyl-α-cyanoacetates, by use of lithium naphthalenide induced reductive α-selenenylation as a key operation. Moreover, the selanyl esters thus generated in situ could be converted further, in a one-pot treatment with hydrogen peroxide and acetic acid, into the corresponding α,β- unsaturated esters in moderate to high yields. The C=C bond formation was highly regio- and/or diastereoselective in some cases. Georg Thieme Verlag Stuttgart.
- Ko, Yen-Chun,Zhu, Jia-Liang
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p. 3659 - 3665
(2008/09/19)
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- 1-BENZYLINDOLE-2-CARBOXAMIDE DERIVATIVES
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The present invention relates to i-benzylindole-2-carboxamide derivatives of formula I, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 1-benzylindole-2-carboxamide deriva
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Page/Page column 49
(2010/11/24)
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- Imidazolium salts as phase transfer catalysts for the dialkylation and cycloalkylation of active methylene compounds
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The efficient synthesis of 1,1-disubstituted derivatives and the construction of cyclopropane and cyclopentane ring systems via dialkylation and cycloalkylation reactions of active methylene compounds using imidazolium salts as phase transfer catalyst is described. The dialkylation and cycloalkylation reactions of active methylene compounds in the presence of readily available imidazolium salts (ionic liquids) as phase transfer catalysts were performed to afford the respective dialkylated or cycloalkylated products. This method is very efficient for the synthesis of 1,1-disubstituted derivatives and cyclopropane and cyclopentane ring systems in a facile manner.
- Muthusamy, Sengodagounder,Gnanaprakasam, Boopathy
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p. 635 - 638
(2007/10/03)
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- Pharmaceutical compounds
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The invention provides novel cryptophycin compounds which can be useful for disrupting the microtubulin system, as antineoplastic agents, antifungal, and for the treatment of cancer. The invention further provides a formulation for administering the novel cryptophycin compounds.
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- The design and synthesis of potent cyclic peptide VCAM-VLA-4 antagonists incorporating an achiral Asp-Pro mimetic
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The Asp-Pro sequence of the cyclic peptide Ac-HN-Tyr-Cys*-Asp-Pro-Cys*-OH (1) could be replaced with the achiral dipeptide mimetic 1-(2-aminoethyl)cyclpentylcarboxylic acid with retention of potent inhibition of the VCAM-VLA-4 interaction. (C) Elsevier Science Ltd. All rights reserved.
- Fotouhi, Nader,Joshi, Pramod,Fry, David,Cook, Charles,Tilley, Jefferson W.,Kaplan, Gerry,Hanglow, Angela,Rowan, Karen,Schwinge, Virginia,Wolitzky, Barry
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p. 1171 - 1173
(2007/10/03)
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- Synthesis and biological evaluation of cryptophycin analogs with substitution at C-6 (fragment C region)
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Analogs of the antitumor agents cryptophycins 1 and 8 with dialkyl substitution at C-6 (fragment C) were synthesized and evaluated for in vitro cytotoxicity against human leukemia cells (CCRF-CEM). The activity of these analogs decreased as the size of the substituents at C-6 increased. The C-6 spirocylopropyl compound (2g) was highly potent in vitro and showed excellent antitumor activity in animal models.
- Varie, David L.,Shih, Chuan,Hay, David A,Andis, Sherri L.,Corbett, Tom H.,Gossett, Lynn S.,Janisse, Samantha K.,Martinelli, Michael J.,Moher, Eric D.,Schultz, Richard M.,Toth, John E.
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p. 369 - 374
(2007/10/03)
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- A convenient new procedure for the construction of highly substituted acetates. Reductive alkylation of α-cyano esters
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A convenient, highly efficient general method for the preparation of highly substituted acetates has been developed, making use of reductive alkylation of α-cyano esters as a key operation.
- Shia, Kak-Shan,Chang, Nien-Yin,Yip, Judy,Liu, Hsing-Jang
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p. 7713 - 7716
(2007/10/03)
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- N-SUBSTITUTED HETEROCYCLIC DERIVATIVES, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT
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The invention relates to N-substituted heterocyclic derivatives and its salts. These derivatives have the formula (I) in which the substituents are as defined in the specification. Application: Angiotensin II antagonists
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- SYNTHESIS OF CYCLOPENTANE DERIVATIVES IN THE CATHODIC ELECTROLYSIS OF COMPOUNDS WITH AN ACTIVATED METHYLENE GROUP IN THE PRESENCE OF 1,4-DIBROMOBUTANE
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The cathodic electrolysis of compounds with an activated methylene group in the presence of 1,4-dibromobutane leads to 1,1-disubstituted cyclopentanes.
- Tatarinova, V. I.,Vasil'ev, A. A.,Petrosyan, V. A.
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p. 2399 - 2401
(2007/10/02)
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- A FACILE PROCEDURE FOR THE PREPARATION OF ALICYCLIC α-AMINO ACIDS
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A convenient method for the preparation of alicyclic α-amino acids is described which utilizes ethyl isocyanoacetate and the appropriate dibromo-substituted aliphatic alkylating agent.
- Kalvin, Douglas,Ramalingam, Kondareddiar,Woodward, Ronald
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p. 267 - 272
(2007/10/02)
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