- Preparation, characterization and application of 1,4-disulfopiperazine-1,4-diium chloride ([Piper-(SO3H)2]·2Cl) as an efficient dicationic ionic catalyst for the N-Boc protection of amines
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In this work, 1,4-disulfopiperazine-1,4-diium chloride ([Piper-(SO3H)2]·2Cl), as a novel Br?nsted acidic ionic catalyst is synthesized and characterized using a series of techniques including FT-IR, TGA, DTA, SEM, pH analysis and Hammett acidity function. This substance can significantly catalyze the N-Boc protection of amines without solvent interference at room temperature. The advantages of this manner are chemoselectivity, short reaction times, suitable yields, excellent yields of the products, without solvent interference and ease of preparation as well as reusability of the catalyst.
- Koodehi, Tahereh Ghauri,Shirini, Farhad,Goli-Jolodar, Omid
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p. 443 - 456
(2017/01/10)
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- Synthetic method of artificial selenium enzyme
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The invention discloses a synthetic method of artificial selenium enzyme and relates to a synthetic method of a compound. The synthetic method mainly comprises three steps of synthesis of a double-seleniumcompound with a benzene ring, synthesis of a butan
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Paragraph 0008; 0009; 0010; 0011; 0012; 0013
(2017/07/20)
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- Silver-Catalyzed Three-Component 1,1-Aminoacylation of Homopropargylamines: α-Additions for Both Terminal Alkynes and Isocyanides
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The reaction of secondary homopropargylamines, isocyanides, and water in the presence of a catalytic amount of silver acetate and subsequent purification by chromatography on silica gel afforded substituted proline amides in good to excellent yields. Primary homopropargylamines underwent a cyclizative Ugi–Joullié three-component reaction with isocyanides and carboxylic acids to afford functionalized N-acyl proline amides. High diastereoselectivity was observed in the synthesis of 4-alkoxy and 4,5-disubstituted proline derivatives. This work represents the first examples of a three-component cyclizative 1,1-aminoacylation of terminal alkynes.
- Tong, Shuo,Piemontesi, Cyril,Wang, Qian,Wang, Mei-Xiang,Zhu, Jieping
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supporting information
p. 7958 - 7962
(2017/06/27)
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- SELECTIVE HDAC6 INHIBITORS
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The present invention provides hydroxamic acids of the formula described herein, that have activity toward inhibiting histone deacetylases, and in particular HDAC6. Also contemplated are pharmaceutical compositions and methods of use of an effective amount of the hydroxamic acid compounds provided, for treating a disease in a subject. In certain embodiments, the subject is afflicted with cancer, neurodegenerative disease, or HIV infection.
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Page/Page column 56
(2015/07/15)
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- CONTROLLED HNO RELEASE THROUGH INTRAMOLECULAR CYCLIZATION-ELIMINATION
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Protected HNO donors designed to undergo non-enzymatic release at neutral pH via an intramolecular cyclization-elimination are disclosed. The rate of cyclization, and therefore HNO release, can be controlled by substituents and chain length. Thus, biologi
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Page/Page column 42
(2014/05/24)
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- An iron-promoted aldehyde-diene cyclocoupling reaction
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(Chemical Equation Presented) A stereospecific intramolecular iron tricarbonyl-promoted aldehyde-diene cyclocoupling reaction was investigated by using simple substrates 6 and more complicated substrates 30a/30b. Demetalation of the initial products conve
- Pearson, Anthony J.,Sun, Huikai
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p. 7693 - 7700
(2008/02/13)
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- A rate enhancement of tert-butoxycarbonylation of aromatic amines with Boc2O in alcoholic solvents
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A rate enhancement of tert-butoxycarbonylation of aromatic amines by Boc2O in alcohols compared to aprotic solvents was demonstrated. Kinetic analysis by NMR suggested that the reaction in CD3OD was faster than in CDCl3 by a factor of 70. Reactions between Boc2O and various aliphatic and aromatic amines in ethanol provided the N-Boc derivatives in good to excellent yields in short reaction times.
- Vilaivan, Tirayut
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p. 6739 - 6742
(2007/10/03)
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- Piperidinyl and piperazinyl compounds substituted with bicyclo-heterocyclylalkyl groups useful as CCR3 receptor antagonists
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Compounds having the Formula (I), are useful as CCR3 receptor antagonists, wherein Ar is aryl or heteroaryl; Q is —C(═O)— or C1-2alkylene; X is N(+)R9a, or N; Y is CR9b, or N; R2 is hydrogen or alkyl; R3 and R4 are as defined in the specification; Uc is a mono- or bicyclic group as defined in the specification; n is 0 or 1; and p is 0, 1, 2, 3 or 4.
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Page/Page column 14
(2010/02/11)
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- Pyridinium derivatives, their production and use
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Novel pyridinium derivatives represented by the formula (I): STR1 wherein STR2 is an optionally substituted pyridinium ring; R1 is a lower alkyl group or aralkyl group; R7 and R10 are independently hydrogen, a lower alkyl group, aryl group or aralkyl group; l is 0 or 1; R5 is a phenylene group or an alkylene group which may be substituted; R11 is an alkyl group or aryl group; X is a group of the formula: --CH2 OCH2 -- or a group of the formula: STR3 wherein R6 is hydrogen, a lower alkyl or a lower alkoxy, and m is an integer of 0 to 3; U is a group of the formula: STR4 wherein R4 is hydrogen, a lower alkyl group, aryl group or aralkyl group; Y and Z are independently a divalent chain group consisting of one to six members which is selected from the class consisting of groups of the formulae: STR5 wherein R is hydrogen, a lower alkyl group, acyl group or aryl group and at least one of which is a group of the formula: STR6 with the proviso that R may be the same or different from each other, or may form a ring together when two or more groups of the formula: STR7 are present, that R may be bonded to R4 when Y contains a group of the formula: STR8 and that R may be bonded to R11 when Z contains a group of the formula: STR9 and W? is a counter anion; are useful as a platelet activating factor antagonist.
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