13200-60-7Relevant articles and documents
N, N -Bis-(dimethylfluorosilylmethyl)amides of N -organosulfonylproline and sarcosine: Synthesis, structure, stereodynamic behaviour and in silico studies
Nikolin, Alexey A.,Kramarova, Eugenia P.,Shipov, Alexander G.,Baukov, Yuri I.,Negrebetsky, Vadim V.,Arkhipov, Dmitry E.,Korlyukov, Alexander A.,Lagunin, Alexey A.,Bylikin, Sergey Yu.,Bassindale, Alan R.,Taylor, Peter G.
, p. 75315 - 75327 (2016)
(O→Si)-Chelate difluorides R3R2NCH(R1)C(O)N(CH2SiMe2F)2 (9a-c, R1R2 = (CH2)3, R3 = Ms (a), Ts (b); R1 = H, R2 = Me, R3 = Ms (c)), containing one penta- and one tetracoordinate silicon atoms were synthesized by silylmethylation of amides R3R2NCH(R1)C(O)NH2, subsequent hydrolysis of unstable intermediates R3R2NCH(R1)C(O)N(CH2SiMe2Cl)2 (7a-c) into 4-acyl-2,6-disilamorpholines R3R2NCH(R1)C(O)N(CH2SiMe2O)2 (8a-c) and the reaction of the latter compounds with BF3·Et2O. The structures of disilamorpholines 8a,c and difluoride 9a were confirmed by an X-ray diffraction study. According to the IR and NMR data, the O→Si coordination in solutions of these compounds was weaker than that in the solid state due to effective solvation of the Si-F bond. A permutational isomerisation involving an exchange of equatorial Me groups at the pentacoordinate Si atom in complexes 9a-c was detected, and its activational parameters were determined by 1H DNMR. In silico estimation of possible pharmacological effects and acute rat toxicity by PASS Online and GUSAR Online services showed a potential for their further pharmacological study.
Microwave-assisted synthesis of substituted hexahydropyrrolo[3,2-c] quinolines
Neuschl, Michal,Bogdal, Darek,Potacek, Milan
, p. 49 - 59 (2007)
New compounds with the ethyl hexahydro-1H-pyrrolo[3,2-c]quinoline-2- carboxylate skeleton were prepared by microwave-assisted intramolecular 1,3-dipolar cycloaddition reactions. The reactions were carried out under solvent-free conditions and compared with the same reaction in the presence of a solvent and a catalyst. Steric effects on the selectivity of the reaction were noted and evaluated.
An enzyme and its optional [...] modified ketone and inhibitor composition comprising (by machine translation)
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Paragraph 0392; 0393, (2017/01/23)
PROBLEM TO BE SOLVED: ketone-containing acrylic misuse, abuse or overload is prevented for a new takable amt. provitamin drag pain. SOLUTION: a compound represented by the following formula is represented, in which the drag oxystyrene provitamin hydrocodone ketone-containing acrylic. Pre-selected drug profile is modified and the ketone and schisandrin [...] holding hung contg. compsn. method for administration to a patient. Selected drawing: no (by machine translation)
Efficient synthesis of some new antiproliferative N-fused indoles and isoquinolines via 1,3-dipolar cycloaddition reaction in an ionic liquid
Sutariya, Tushar R.,Labana, Balvantsingh M.,Parmar, Narsidas J.,Kant, Rajni,Gupta, Vivek K.,Plata, Gabriela B.,Padrón, José M.
supporting information, p. 2657 - 2668 (2015/04/14)
Syntheses of some new pyrrolo-fused pyrrolo[1,2-a] indole derivatives have been achieved by combining N-allyl-indole-2-carbaldehyde with a variety of N-alkyl-glycine esters as well as tetrahydroisoquinolines in an ionic liquid, triethylammonium acetate (TEAA), a recyclable reaction medium, via intramolecular [3+2] cycloaddition reaction. This new method is highly efficient, and the ionic liquid employed is recyclable. The stereochemistry of all the compounds was confirmed by 2D NMR NOESY and in some cases single crystal X-ray diffraction data. The in vitro screening of all new candidates against various bacterial strains and representative human solid tumor cell lines, A549 (lung), HeLa (cervix), SW1573 (lung), T-47D (breast) and WiDr (colon), revealed that many of them have good antibacterial, antifungal and antitubercular and antiproliferative activities.
Selective monomethylation of primary amines with simple electrophiles
Lebleu, Thomas,Ma, Xiaolu,Maddaluno, Jacques,Legros, Julien
supporting information, p. 1836 - 1838 (2014/02/14)
Direct monomethylation of primary amines with methyl triflate was achieved with high selectivity (up to 96%). The key point of this single methyl transfer stems from the use of HFIP as the solvent that interferes with amines and avoids overmethylation.
A convenient 1,3-dipolar cycloaddition-reduction synthetic sequence from 2-allyloxy-5-nitro-salicylaldehyde to aminobenzopyran-annulated heterocycles
Parmar, Narsidas J.,Pansuriya, Bhavesh R.,Labana, Balvantsingh M.,Kant, Rajni,Gupta, Vivek K.
, p. 17527 - 17539 (2013/09/24)
A microwave-assisted, one-pot synthesis of some nitro benzopyran-annulated pyrroles as well as pyrrolo-fused isoquinolines via a 1,3-dipolar cycloaddition, which involves the in situ generation of azomethine ylide formed by reacting secondary amines with 2-allyloxy-5-nitro-salicylaldehyde, has been achieved in a solvent-free environment. Compared to methods of conventional and thermal heating, the present microwave-assisted method is rapid and highly efficient. In addition, amino analogous heterocycles were successfully accessed after treating the reaction mass further with iron in acidic medium, which also highlights a one-pot procedure for a new 1,3-dipolar cycloaddition-reduction synthetic sequence. All amino-products are new bioprofiles and anticipated to be effective drug-like candidates. All compounds were characterised based on their elemental analysis, mass, IR, and 1H and 13C NMR spectroscopic data. The stereochemistry of the product was confirmed by 2D NMR COSY and NOESY experiments, which, on the basis of single crystal X-ray diffraction data analysis, was further confirmed and supported.
An improved microwave assisted one-pot synthesis, and biological investigations of some novel aryldiazenyl chromeno fused pyrrolidines
Parmar, Narsidas J.,Pansuriya, Bhavesh R.,Barad, Hitesh A.,Kant, Rajni,Gupta, Vivek K.
supporting information; experimental part, p. 4075 - 4079 (2012/07/03)
An improved microwave assisted one-pot method for the synthesis of twelve new aryldiazenylchromeno [4,3-b] pyrrolidines via intramolecular azomethine ylide cycloaddition route is described. The method is efficient and advantageous over conventional and solvent-free thermal methods. The stereochemistry of the compounds was confirmed on the basis of various NMR experiments, and finally by single crystal X-ray diffraction data. N-Methyl or ethyl pyrrolidine based heterocycles gave good biological activities.
COMPOSITIONS COMPRISING ENZYME-CLEAVABLE PRODRUGS OF ACTIVE AGENTS AND INHIBITORS THEREOF
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Page/Page column 309, (2011/11/06)
The present disclosure provides pharmaceutical compositions, and their methods of use, where the pharmaceutical compositions comprise a prodrug that provides enzymatically-controlled release of a drug and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the drug from the prodrug so as to attenuate enzymatic cleavage of the prodrug. The disclosure provides pharmaceutical compositions which comprise an enzyme inhibitor and a prodrug that contains an enzyme-cleavable moiety that, when cleaved, facilitates release of the drug.
Synthesis of novel diketopiperazine derivative and obsevation of self-assembled structure
Ohta, Yosuke,Terada, Kayo,Masuda, Toshio,Sanda, Fumio
experimental part, p. 2523 - 2530 (2010/04/25)
An N-monomethylated unsymmetrical diketopiperazine was synthesized from D-p-hydroxyphenylglycine and sarcosine, and condensed with trans-1,4-cyclohexanedicarboxylic acid to obtain the ester having diketopiperazine moieties at the both termini. Atomic force microscope measurement indicated that the ester formed a supramolecular structure aligned in a circular pattern based on hydrogen bonding between the amide groups of the diketopiperazine moieties.
Spiro-hydantoin compounds useful as anti-inflammatory agents
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Page/Page column 39, (2008/06/13)
Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, enantiomers, and diastereomers, and prodrugs thereof, are useful as inhibitors of LFA-1/ICAM and as anti-inflammatory agents, wherein L and K are O or S; Z is N or CR4b; Ar is an optionally-substituted aryl or heteroaryl; G is a linker attached to T or M or is absent; J, M and T are selected to define a three to six membered saturated or partially unsaturated non-aromatic ring; and R2 R4a, R4b, and R4c are as defined in the specification.
