- Electron Impact and Ammonia Chemical Ionization Mass Spectra of n-Azabicycloalkan-(n+1)-ones (m=3-6, n=6-9)
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Electron impact induced fragmentation of the title compounds obeys a route where the lactam moiety, OCNH, is cleaved first, with the accompanying formation of a cycloalkene ion.This can be verified by low-resolution, high-resolution, B/E and B2/E spectra as well as by collisional activation spectra of, for example, the ions m/z 82 and 67 from 7-azaabicyclooctan-8-one and from cyclohexene.The only, and fairly weak, fragment ions including O and N are +, kH2k-2N>+ (k=5-8) and +.The ammonia chemical ionization spectra are also characteristic for all four lactams and show the same dominant ions in all cases, namely +, +. and +..
- Pihlaja, Kalevi,Vainiotalo, Pirjo,Bernath, Gabor,Goendoes, Gyoergy,Gera, Lajos
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Read Online
- Design, synthesis and biological evaluation of novel bicyclic β-lactams as potential antimalarials
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A series of bicyclic N-substituted and unsubstituted β-lactams were synthesized and evaluated as targeted potential antimalarials. The compounds MNR4 and MNR5 were found to have highest potency against Plasmodium falciparum in vitro.
- Nivsarkar, Manisha,Thavaselvam,Prasanna,Sharma, Mamta,Kaushik
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Read Online
- SUBSTITUTED PYRROLO-PYRIDINONE DERIVATIVES AND THERAPEUTIC USES THEREOF
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Compounds of formula (I), processes for their production and their use as pharmaceuticals.
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Page/Page column 94-95
(2022/02/09)
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- N-acyl-β-lactam derivative, macromolecular compound, and photoresist composition
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Provided are N-acyl-β-lactam derivatives represented by the following general formula, from which a photoresist composition capable of controlling an acid diffusion length to be short is obtained; a polymer obtained by polymerizing the N-acyl-β-lactam derivative represented by the following general formula as one of starting materials; and a photoresist composition containing the polymer, where the structural variables are as defined herein.
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Paragraph 0230-0233
(2014/10/28)
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- Nylon-3 polymers that enable selective culture of endothelial cells
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Substrates that selectively encourage the growth of specific cell types are valuable for the engineering of complex tissues. Some cell-selective peptides have been identified from extracellular matrix proteins; these peptides have proven useful for biomat
- Liu, Runhui,Chen, Xinyu,Gellman, Samuel H.,Masters, Kristyn S.
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supporting information
p. 16296 - 16299
(2013/12/04)
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- N-ACYL-B-LACTAM DERIVATIVE, MACROMOLECULAR COMPOUND, AND PHOTORESIST COMPOSITION
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Disclosed are an N-acyl-β-lactam derivative represented by the following general formula, from which a photoresist composition capable of controlling an acid diffusion length to be short is obtained; a polymer obtained by polymerizing the N-acyl-β-lactam derivative represented by the following general formula as one of starting materials; and a photoresist composition containing the polymer. In the formula, R1 represents a hydrogen atom, a methyl group, or a trifluoromethyl group; W represents an alkylene group or a cycloalkylene group; n represents 0 or 1; and each of R2, R3, R4, and R5 independently represents a hydrogen atom, an alkyl group, a cyclic hydrocarbon group, or an acyloxy group, provided that 1) R2 and R3, or R4 and R5, may be connected to each other to form a substituted or unsubstituted ring which may have an oxygen atom at an arbitrary position, 2) R3 and R4 may be connected to each other to form a substituted or unsubstituted ring which may have an oxygen atom at an arbitrary position, and 3) all of R2, R3, R4, and R5 are not a hydrogen atom at the same time.
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- Hairpin folding behavior of mixed α/β-peptides in aqueous solution
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The invention of new strategies for the design of protein-mimetic oligomers that manifest the folding encoded in natural amino acid sequences is a significant challenge. In contrast to the α-helix, mimicry of protein β-sheets is less understood. We report
- Lengyel, George A.,Frank, Rebecca C.,Horne, W. Seth
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supporting information; experimental part
p. 4246 - 4249
(2011/06/21)
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- New compounds
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The present invention encompasses compounds of general formula (1) wherein R1, R2, R4, X, m, n and p are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.
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Page/Page column 9
(2009/07/10)
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- Efficient synthesis of (1R,2S) and (1S,2R)-2-aminocyclopentanecarboxylic acid ethyl ester derivatives in enantiomerically pure form
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A 4-step synthesis of an optically active synthetic intermediate [(1R,2S)-2-(4′-fluorobenzylamino)cyclopentanecarboxylic acid ethyl ester complex with (S)-(+)-mandelic acid; compound 12, >99% de] required for the preparation of a promising HCV NS5B polymerase inhibitor is reported. This process utilizes mandelic acid as a resolving agent, which can be recovered in good yield by a simple extraction. An optimized version of the chemistry described avoids the use of chromatographic purifications making it suitable for large-scale applications. In addition, the straightforward conversion of compound 12 to enantiomerically pure (1R,2S)-2-aminocyclopentanecarboxylic acid ethyl ester and the corresponding Boc and Cbz derivatives is reported. The preparation of the enantiomer of 12 (compound 15) in enantiomerically pure form and the conversion of this entity to (1S,2R)-2-aminocyclopentanecarboxylic acid ethyl ester and the corresponding Boc and Cbz derivatives is also described.
- Dragovich, Peter S.,Murphy, Douglas E.,Dao, Kimkim,Kim, Sun Hee,Li, Lian-Sheng,Ruebsam, Frank,Sun, Zhongxiang,Tran, Chinh V.,Xiang, Alan X.,Zhou, Yuefen
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experimental part
p. 2796 - 2803
(2009/06/28)
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- Synthesis and antimalarial evaluation of cyclic β-amino acid-containing dipeptides
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This paper describes an efficient synthesis and the antiparasitic evaluation of cyclic β-amino acid-containing dipeptides 3.1-3.6 and 4.1-4.5. The antimalarial properties of all these dipeptides have been evaluated in vitro against Plasmodium falciparum a
- Sathe, Manisha,Thavaselvam, Duraipandian,Srivastava, Ashish Kumar,Kaushik, Mahabir Parshad
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p. 432 - 443
(2008/09/17)
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- NEW COMPOUNDS
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The present invention encompassescompounds of general formula (1) wherein R1 to R4 , X and n are defined as in claim 1, which are suitable for the treatment of ailments characterised byexcessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
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Page/Page column 18
(2008/12/06)
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- 2,4-diamino-pyrimidines as aurora inhibitors
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The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
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Page/Page column 18
(2008/06/13)
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- Large-scale syntheses of FMOC-protected non-proteogenic amino acids: Useful building blocks for combinatorial libraries
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Convenient and reliable large-scale procedures for the protection of various amino acids with N-(9-fluorenylmethoxycarbonyl)oxysuccinimide (FMOC-OSu) are described. Commercially available 4-aminomethylbenzoic acid and trans-4-(aminomethyl)cyclohexanecarbo
- Dener, Jeffrey M.,Fantauzzi, Pascal P.,Kshirsagar, Tushar A.,Kelly, Daphne E.,Wolfe, Aaron B.
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p. 445 - 449
(2013/09/07)
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- STEREOCHEMICAL STUDIES, 144. SATURATED HETEROCYCLES, 151. PREPARATION OF cis AND trans-CYCLOALKANE-CONDENSED PYRIMIDINEDIONES BY AZETIDINONE RING TRANSFORMATION
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N-substituted derivatives (3 and 4) obtained from cyclopentane- and cyclohexane-azetidinones (1 and 2) were isomerized with polyphosphoric acid to give cyclopentane-cis- (6) and cyclohexane-trans-condensed (7) 2,4-pyrimidinediones.The structures of the dihydrouracils prepared by the ring transformation were proved by 1H- and 13C-nmr spectroscopy and by comparison with the compounds synthesized from cis- and trans-2-amino-1-cycloalkanecarboxamides (11-13) with 1,1'-carbonyldiimidazole.
- Stajer, Geza,Szoeke-Molnar, Zsolt,Bernath, Gabor,Sohar, Pal
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p. 1943 - 1950
(2007/10/02)
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