- Photo-on-Demand Synthesis of Chloroformates with a Chloroform Solution Containing an Alcohol and Its One-Pot Conversion to Carbonates and Carbamates
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Chloroformates are key reagents for synthesizing carbonates and carbamates. The present study reports a novel photo-on-demand in situ synthesis of chloroformates with a CHCl3 solution containing a primary alkyl alcohol. It further allowed the one-pot synthesis of carbonates and carbamates through subsequent addition of alcohols or amines, respectively.
- Liang, Fengying,Suzuki, Yuto,Tsuda, Akihiko,Yanai, Masaki
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Read Online
- Method for preparing aliphatic (cycloaliphatic) ester compound
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The invention relates to a mild-condition method for preparing an aliphatic (cycloaliphatic) ester compound, particularly preparation of an alkyl cyclohexanecarboxylate compound. The ester compound can serve as an environment-friendly plasticizer in plastics, so that the occurrence of side reactions such as polymerization, etherification and the like of aliphatic alcohol compounds in the existing esterification processes under high-temperature conditions is avoided. The method comprises the specific reaction steps: (a) preparing aliphatic chloro-formate in a reaction rectification tower in the absence of a catalyst/solvent; and (b) catalyzing an aliphatic (cycloaliphatic) Grignard reagent to react with the aliphatic chloro-formate by a metal manganese compound, so as to produce the ester compound.
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Paragraph 0049
(2017/01/02)
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- In vitro radical scavenging and cytotoxic activities of novel hybrid selenocarbamates
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Novel selenocyanate and diselenide derivatives containing a carbamate moiety were synthesised and evaluated in vitro to determine their cytotoxic and radical scavenging properties. Cytotoxic activity was tested against a panel of human cell lines including CCRF-CEM (lymphoblastic leukaemia), HT-29 (colon carcinoma), HTB-54 (lung carcinoma), PC-3 (prostate carcinoma), MCF-7 (breast adenocarcinoma), 184B5 (non-malignant, mammary gland derived) and BEAS-2B (non-malignant, derived from bronchial epithelium). Most of the compounds displayed high antiproliferative activity with GI50 values below 10 μM in MCF-7, CCRF-CEM and PC-3 cells. Radical scavenging properties of the new selenocompounds were confirmed testing their ability to scavenge DPPH and ABTS radicals. Based on the activity of selenium-based glutathione peroxidases (GPxs), compounds 1a, 2e and 2h were further screened for their capacity to reduce hydrogen peroxide under thiol presence. Results suggest that compound 1a mimics GPxs activity. Cytotoxic parameters, radical scavenging activity and ADME profile point to 1a as promising drug candidate.
- Romano, Beatriz,Plano, Daniel,Encío, Ignacio,Palop, Juan Antonio,Sanmartín, Carmen
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p. 1716 - 1727
(2015/03/30)
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- NOVEL VINBLASTINE DERIVATIVES, THEIR PREPARATION, USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAID DERIVATIVES
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The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors.
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Page/Page column 39
(2009/12/05)
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- NOVEL DITHIOLOPYRROLONES AND THEIR THERAPEUTICAL APPLICATIONS
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The present invention provides novel dithiolopyrrolone compounds and their salts, which promote production of white blood cells and are useful as prevention and treatments for microbial infections such as HIV infection and blood disorders such as neutropenia and other related diseases. The present invention also provides therapeutic compositions comprising particularly useful types of dithiolopyrrolones, the salts thereof, and methods and use in the manufacture of a medication for treatment of diseases.
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Page/Page column 36-37
(2008/06/13)
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- Derivatives of imidazole, their preparation process, the new intermediates obtained, their use as medicaments and the pharmaceutical compositions containing them
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The invention relates to the products of formula (I): STR1 in which: R1 =represents hydrogen, aryl, arylcarbonyl, arylthio, alkylcarbonyl, R2, R3 represent in particular halogen, mercapto, acyl, carboxy, nitro, cyano, amino, carbamoyl, R4, --OR4 with R4 representing in particular hydrogen, alkyl, alkenyl, alkynyl, acyl, amino, --(CH2)m1 --S(O)m2 --X--R10 with m1=0 to 4, m2=0 to 2, X represents a single bond or --NH--, --NH--CO--, --NH--CO--NH--, and R10 represents alkyl, alkenyl or aryl, and Y represents optionally substituted aryl, these products being in all isomer forms and salts, their use as medicaments.
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- Compositions for reducing abnormal stimulation of endothelin receptors and novel compounds
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The invention relates to the new use and the new products of formula (I): STR1 in which: R1 =represents hydroxyl, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, formyl, cycloalkyl, optionally interrupted by heteroatoms, R2, R3 represent in particular halogen, mercapto, acyl, carboxy, nitro, cyano, amino, carbamoyl, R4, --OR4 with R4 representing in particular hydrogen, alkyl, alkenyl, alkynyl, acyl, amino, --(CH2)m1 --S(O)m2 --X--R10 with m1=0 to 4, m2=0 to 2, X represents a single bond or --NH--, --NH--CO--, --NH--CO--NH--, and R10 represents alkyl, alkenyl or aryl, and Y represents optionally substituted aryl, these products being in all the isomer forms and the salts, as medicaments.
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- Carbamate series of juvenoids: Variation of the O-alkyl substituent
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By changing the O-alkyl substituents of the carbamate moiety of alkyl N-{2-{4-[(2-oxocyclohexyl)methyl]phenoxy}ethyl}carbamates and subsequent transformation of the oxo group in the cyclohexyl substituent, the juvenoids 1-20 were synthesized (Scheme). The methyl (1-4), propyl (9-12), isopropyl (13-16), and prop-2-ynylcarbamates (17-20) were subjected to biological screening on several non-related insect species (Tenebrio molitor, Galleria mellonella, Dysdercus cingulatus, and Pyrrhocoris apterus). Some of the juvenoids showed high biological activity and excellent selectivity with respect to target insect species (Table 2).
- Wimmer,Saman,Nemec,Francke
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p. 561 - 568
(2007/10/02)
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- KINETICS AND MECHANISM OF THE PHOSGENATION OF ALIPHATIC ALCOHOLS II. EFFECT OF THE SOLVENT ON THE REACTION RATE
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A quantitative analysis of the effect of the characteristics of the medium on the phosgenation rate of alcohols was made by means of the parameters of the Koppel-Palm equation.An equation is proposed which describes the effect of the solvent on the reaction rate and which takes account of the interdependence of the components of nonspecific and specific solvation.The applicability of the proposed equation to other solvolytic reactions was demonstrated.An equation is obtained which makes it possible to asses the phosgenation rate of alcohols in relation to the properties of the medium and the structure of the alcohol.
- Chimishkyan, A. L.,Orlov, S. I.,Elinevskii, A. V.,Grabarnik, M. S.,Shebeko, S. M.
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- Pesticides
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New insecticides are of formula: STR1 wherein R1 represents hydrogen or a methyl group; R2 represents hydrogen or a halogeno or lower alkyl group; R3 represents hydrogen or a halogeno or carbo(lower alkoxy) group which contains at least 2 carbon atoms in the lower alkoxy residue when R2 represents methyl; with the proviso that (a) R2 and R3 each represent hydrogen only when R1 represents methyl, (b) when R1 and R3 each represent hydrogen and R2 represents alkyl, that alkyl group contains at least 2 carbon atoms and (c) when R3 represents halogeno, R2 represents hydrogen or halogeno; and R represents a group which forms insecticidal esters with chrysanthemic acid e.g. 5-benzyl-3-furylmethyl, 3-phenoxybenzyl, α-cyano-3-phenoxybenzyl. The esters are prepared by forming the ester linkage conventionally or by a Wittig reaction using a 3-formyl- or 3-acetyl-2,2-dimethyl cyclopropane carboxylic acid esterified with the desired residue or by an alkyl group which is subsequently converted to the desired residue.
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- KINETICS AND MECHANISM OF PHOSGENATION OF ALIPHATIC ALCOHOLS
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The kinetics of the reaction of phosgene with various aliphatic alcohols were investigated in heptane and dioxane and without a solvent.The effects of the polarity of the medium the structure of the alcohol, and the activation parameters of the process are consistent with an addition-elimination mechanism.
- Orlov, S. I.,Chimishkyan, A. L.,Grabarnik, M. S.
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p. 1977 - 1981
(2007/10/02)
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- Insecticides
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New insecticides are of formula: STR1 wherein R1 represents hydrogen or a methyl group; R2 represents hydrogen or a halogeno or lower alkyl group; R3 represents hydrogen or a halogeno, lower alkyl (which is different to R2 when R2 represents a lower alkyl group) or carbo(loweralkoxy) group which contains at least 2 carbon atoms in the lower alkoxy residue when R2 represents methyl or R2 and R3 together with the carbon atom to which they are attached represent a cycloalkylene ring having at least one endocyclic carbon to carbon double bond; with the proviso that (a) R2 and R3 each represent hydrogen only when R1 represents methyl and (b) R3 contains at least 2 carbon atoms when R1 and R2 each represent hydrogen; and R represents a group which form insecticidal esters with chrysanthemic acid e.g. 5-benzyl-3-furylmethyl, 3-phenoxybenzyl, α-cyano-3-phenoxybenzyl. The esters are prepared by forming the ester linkage conventionally or by a Wittig reaction using a 3-formyl- or 3-acetyl-2,2-dimethyl cyclopropane carboxylic acid esterified with the desired residue or by an alkyl group which is subsequently converted to the desired residue.
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