Showing papers on "Derivative (chemistry) published in 1990"
Patent•
09 Feb 1990
TL;DR: In this paper, a new camptothecin derivative (salt) is represented by the formula (R 1 is H or a 1-6C alkyl; R 2 is 0 to four 1- 6C groups, halogen atoms, alkoxy or hydroxyl groups).
Abstract: PROBLEM TO BE SOLVED: To obtain the subject new derivative comprising a specific camptothecin derivative, improving water solubility so as to be advantageous to administration and the stability in a basic aqueous solution without reducing antitumor activities and having excellent antitumor activities. SOLUTION: This new camptothecin derivative (salt) is represented by the formula (R 1 is H or a 1-6C alkyl; R 2 is 0 to four 1-6C alkyl groups, halogen atoms, alkoxy or hydroxyl groups; R 3 is a lower alkylamino, a dilower alkylamino, an arylamino, a cyclic amino or a lower alkoxy) [e.g. 7-ethyl-17- methylcarbamoyloxycamptothecin-21-(2-dimethylamino)ethylamide] and is useful as an oral administration agent or the like excellent in antitumor activities. The compound is obtained by treating 7-ethylcamptothecin with N,N- dimethylethylenediamine, opening the E ring lactone moiety, then reacting the produced hydroxymethyl group with methyl isocyanate or the like and forming a carbamate. COPYRIGHT: (C)1999,JPO
181 citations
147 citations
Patent•
24 Oct 1990
TL;DR: In this paper, the parenteral administration of 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine or 1-(2-hydroxy-2-methylpropyl)-1-H-IMIDO[4.5]-quinolin- 4-amine is described.
Abstract: Pharmaceutical formulations for the parenteral administration of 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine or 1-(2-hydroxy-2-methylpropyl)-1-H-imidazo[4,5-c] quinolin-4-amine are described.
128 citations
TL;DR: The individual enantiomers of the 1,1-dimethylheptyl homolog of 7-hydroxy Δ 6 -tetrahydrocannabinol, (1) and (2a), which exhibit distinct pharmacological profiles, have been obtained with very high e.g. by synthesis from the antipodes of myrtenol.
Abstract: The individual enantiomers of the 1,1-dimethylheptyl homolog of 7-hydroxy- Δ 6 -tetrahydrocannabinol, (1) and (2a), which exhibit distinct pharmacological profiles, have beenobtained with very high e.e. by synthesis from the antipodes of myrtenol.
122 citations
117 citations
105 citations
85 citations
TL;DR: The data suggest that the direct product of thealpha-amidating reaction is not an alpha-amidated peptide but a hydroxyl derivative at the alpha-carbon of the carboxyl-terminal glycine.
81 citations
TL;DR: Asymmetric allylic alkylation of 1,3-diphenyl-2-propenyl acetate with sodium salt of acetamidomalonate ester has been carried out in the presence of a palladium catalyst containing (S )-BINAP to give a chiral α-allyl-αacetamidalonate derivative of high optical purity (94±1% ee).
73 citations
TL;DR: Optically active 2-iodobinaphthyl (S)-(I) is transformed into iodo(III) derivative (S-III) by two ways as discussed by the authors.
Abstract: Optically active 2-iodobinaphthyl (S)-(I) is transformed into iodo(III) derivative (S)-(III) by two ways.
69 citations
TL;DR: The fluorescence quantum yield of dibenzocryptand derivative (6) shows alkali cation-induced enhancements of up to 10 with virtually no other electronic spectral changes.
TL;DR: In this article, the bicyclic compounds 4a and 4b were synthesized via Li2Cu(CN)Ph2, and the desired compound 23 was obtained from 20.
Abstract: Starting from D-glutamic acid (5), the bicyclic compounds 4a and 4b were synthesized via17 (Schemes 1 and 2). The reaction leading to 4g and 4h with LiCuPh2 was not successful. But treatment of the N-protected model lactams 19, 21, and 22 with Li2Cu(CN)Ph2 gave the amino ketones 24, 26, and 27, respectively (Scheme 3). The desired compound 23 was obtained from 20. Conversion of the unprotected lactams 28, 31, and 32 gave the phenyl derivative 34 in excellent yields. Ester 35 was transformed to the α -amino-γ- oxo-acid derivative 36. This conversion opens a novel access to this type of compounds.
TL;DR: In this article, the first stable organometallic derivative of the starting tetrahalide was synthesized with lithium-bis(trimethylsilyl)methyl in n-pentane and the crystal structure showed monomeric molecules with two trigonal planar coordinated metal atoms.
TL;DR: The ground-state conformation of a rotationally constrained tryptophan derivative, 3-carboxy-1,2,3,4-tetrahydro-2-carboline, W(1), is determined from single-crystal X-ray diffraction, MM2 calculations, and 1 H NMR coupling constants as discussed by the authors.
Abstract: The ground-state conformation of a rotationally constrained tryptophan derivative, 3-carboxy-1,2,3,4-tetrahydro-2-carboline, W(1), is determined from single-crystal X-ray diffraction, MM2 calculations, and 1 H NMR coupling constants. The solid-state structure represents the predominant solution conformation. W(1) populates only two minimum-energy conformations in solution, which correspond to the half-chair forms of cyclohexene. The conformers are distinguished mainly by distance of the carboxylate from the indole ring
Patent•
21 Sep 1990
TL;DR: In this article, the authors present methods and compositions for detecting and measuring the concentration in solution of polyhydroxyl compounds, such as sugars, using certain dye compositions that, when linked to a derivative of boronic acid (or boronate ion), arsenious acid, or arsenite ion, exhibit quantitative responses to the presence of poly hydroxyl species.
Abstract: Methods and compositions for detecting and measuring the concentration in solution of polyhydroxyl compounds, such as sugars. The invention makes use of certain dye compositions that, when linked to a derivative of boronic acid (or boronate ion), arsenious acid (or arsenite ion), or germanic acid (or germanate ion), exhibit quantitative responses to the presence of polyhydroxyl species.
TL;DR: In this paper, the relative esters of 4-substituted 2-amino-, 2-methyl- or 2-phenyl-5-pyrimidine carboxylic acids were obtained in moderate yields by reaction of the above dinucleophiles with ethyl 2,2-diformylacetate.
Patent•
3M1
TL;DR: A flexible and resilient, nonwoven, surface treating article formed of entangled synthetic fibers bonded together at points where they contact one another by a binder resin comprising plasticized vinyl resin and polymerized amine-formaldehyde derivative as mentioned in this paper.
Abstract: A flexible and resilient, nonwoven, surface treating article formed of entangled synthetic fibers bonded together at points where they contact one another by a binder resin comprising plasticized vinyl resin and polymerized amine-formaldehyde derivative.
TL;DR: High and long lasting activities were found for the pyridyloxy compounds 3a and 3d, the pryidazinyloxy compound 11a, and its N-alkylation products, as well as for the 3S,4R-enantiomers 20a and 22a.
Abstract: The reaction of 2,4-dihydroxypyridine (2) with 3,4-epoxy-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-6-carbonitrile (1) yielded the 4-[(1,2-dihydro-2-oxo-4-pyridyl)oxy] compound 3a, accompanied by small amounts of the isomeric 4-(1,2-dihydro-4-hydroxy-2-oxo-1-pyridyl) compound 4. This could also be prepared by hydrogenation of the benzyloxy derivative 5. Reaction of 3,6-pyridazinediol (10) with 1 (R = CN) gave the 4-[(1,6-dihydro-6-oxo-3-pyridazinyl)oxy] compound 11a, which in turn rearranged on heating with NaH in DMSO into the 4-(1,6-dihydro-3-hydroxy-6-oxo-1-pyridazinyl) compound 12. A series of 6-substituted analogues (R = CO2Me, CSNH2, NO2, Br) of 3a and 11a were synthesized. N-Alkylation led to compounds 14a-c (R = Me, Et, CHMe2). The 4-heterocyclyloxychromenes 9 and 16a were obtained by alkaline hydrolysis of their 3-camphorsulfonates. The racemic pyridazinyloxy compounds 11a and 14a could be resolved via their diastereomeric camphorsulfonates or camphanates. The differences between the 4-heterocyclyloxychromanols and the isomeric N-substituted compounds 4 and 12 were elucidated in the course of extensive NMR investigations. While in DMSO the former appeared to be conformationally flexible molecules the latter were rigid. All compounds were tested for oral antihypertensive activity in spontaneously hypertensive rats, using doses of 1 mg/kg. High and long lasting activities were found for the pyridyloxy compounds 3a and 3d, the pyridazinyloxy compound 11a, and its N-alkylation products, as well as for the 3S,4R-enantiomers 20a and 22a. (-)-(3S,4R)-3,4-Dihydro-4-[(1,6-dihydro-1-methyl-6-oxo-3- pyridazinyl)oxy]-3-hydroxy-2,2-dimethyl-2H-1-benzopyran-6-carbonitrile (22a) was selected for further development.
Patent•
05 Apr 1990
TL;DR: Biocidally active surface coating compositions have excellent resistance to attack by algae, fungi, and other microorganisms and have high activity against the deposition of biota The surface coatings exhibit antimicrobial activity against a broad range of microoganisms when bonded to a variety of surfaces The active chemical is not removed from these surfaces even after repeated washing with water or submerging the surfaces in water for an extended period of time as discussed by the authors.
Abstract: Biocidally active surface coating compositions have excellent resistance to attack by algae, fungi, and other microorganisms and have high activity against the deposition of biota The surface coatings exhibit antimicrobial activity against a broad range of microoganisms when bonded to a variety of surfaces The active chemical is not removed from these surfaces even after repeated washing with water or submerging the surfaces in water for an extended period of time This antimicrobial activity is not attributed to a slow release of the active ingredient, but rather to the active non-leachable surface The active quaternary ammonium compounds in monomeric forms have the structural formulas as follows: ##STR1## wherein R 1 , R 2 , and R 3 each represents an unsubstituted or substituted alkyl or hydroxalkyl group or a derivative thereof having from 1 to 20 carbon atoms; Y represents hydrogen, an unsubstituted or substituted alkyl group, or a derivative thereof having up to 10 carbon atoms; and X - represents an anionic group such as Cl - , Br - , I - , OH - , or HSO 4 -
TL;DR: The benzylidene-aniline derivative with an electron-donating group at the 4-position and an electron accepting group at 4′-position has been suggested, by MO calculations, to have a small molecular dipole moment in spite of the large secondorder hyperpolarizability, and hence to be a promising molecule in the search for new organic crystals with large second-order optical nonlinearity as discussed by the authors.
Patent•
31 Aug 1990TL;DR: The refrigeration oil composition comprises a hydrogenated fluoroethane and an ester compound obtained from an aliphatic polyhydric alcohol having 1 to 6 primary hydroxyl groups.
Abstract: The refrigeration oil composition comprises (1) a hydrogenated fluoroethane and (2) an ester compound obtained from (2-a) an aliphatic polyhydric alcohol having 1 to 6 primary hydroxyl groups, (2-b) a saturated aliphatic monocarboxylic acid having 2 to 9 carbon atoms, straight or branched, or a derivative thereof and (2-c) a saturated aliphatic dicarboxylic acid having 2 to 10 carbon atoms, straight or branched, or a derivative thereof, said ester compound having a kinematic viscosity at 100 degree C of 1 to 100 cst.
Patent•
10 Aug 1990
TL;DR: In this article, an improved process for the preparation of cyclic amino acids by a novel synthesis is described where a dinitrile derivative is converted in two steps to the desired products, as well as valuable intermediates used in the process.
Abstract: An improved process for the preparation of cyclic amino acids by a novel synthesis is described where a dinitrile derivative is converted in two steps to the desired products, as well as valuable intermediates used in the process.
TL;DR: In this article, the synthesis of the title compounds could be achieved by featuring the Pd-catalyzed coupling reaction of stereo-defined (E)-and (Z)-enol triflates with an acetylene derivative.
Patent•
08 Feb 1990
TL;DR: In this article, a biphenyl derivative of the formula (B) was disclosed, where R1, R3, R4, R5 and Rc are as defined or its salt, and a process for preparing a phenyl derivative contained in the composition.
Abstract: There is disclosed a biphenyl derivative of the formula (B): ##STR1## wherein R1, R3, R4, R5 and Rc are as defined or its salt, a composition for nerve cell degeneration repairing or protecting agent containing a phenyl derivative selected from compounds (1) to (4) and (B) as defined, and a process for preparing a phenyl derivative contained in the composition.
TL;DR: In this paper, a flash pyrolytically and trapped with thiophenol and sulphur dioxide and in the case of the oxazole derivative with methyl acrylate.