- The Insertion Reaction of NH Singlet Radicals into the C-H Bonds of Cyclopropane and Isobutane in the Liquid Phase
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Hydrogen azide was photolyzed in liquid cyclopropane at the temperature of Dry Ice-methanol.The main products observed were nitrogen, cyclopropylamine, and ammonia.The relative yields of the products depended slightly on the concentration of hydrogen azide.The results were then compared with those obtained with paraffin and olefin.The isobutane solution of hydrogen azide was photolyzed at 0 deg C.The products observed were the same as those obtained at the temperature of Dry-Ice-methanol.The relative yields of the products and the concentration dependence, however, were different.
- Hamada, Jun-ich,Tsunashima, Shigeru,Sato, Shin
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- Method for preparing amine through catalytic reduction of nitro compound by cyclic (alkyl) (amino) carbene chromium complex
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The cyclic (alkyl) (amino) carbene chromium complex is prepared from corresponding ligand salt, alkali and CrCl3 and used for catalyzing pinacol borane to reduce nitro compounds in an ether solvent under mild conditions to generate corresponding amine. The method for preparing amine has the advantages of cheap and accessible raw materials, mild reaction conditions, wide substrate application range, high selectivity and the like, and is simple to operate.
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Paragraph 0015
(2021/04/17)
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- Novel method and technology for synthesizing cyclopropyl ammonia
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The invention discloses a synthesis process route of a cyclopropane synthetic route. In the process route, cyanocyclopropane 1 - formic acid (-1 -) and (1) are subjected to hydrolysis under the action of a strong base to generate 1-cyanocyclopropane 1 - formic acid (-1 -), (2) decarboxylation to generate cyclopropanecarboxamide (2 3), and (4 4 3) subjected to Hoffman rearrangement to obtain the target product cyclopropysite. The process route is longer than the production process in the present stage, the reaction route is long, the use of high-temperature and high-pressure is avoided, the danger is reduced, and the safety is improved. The requirement of the reaction equipment is reduced, the used raw materials are easy to obtain, operation is easy, safety and environmental protection are achieved, and industrial production can be realized.
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Paragraph 0019
(2021/09/21)
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- NHC-based coordination polymers as solid molecular catalysts for reductive amination of biomass levulinic acid
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A class of robust solid molecular NHC-based catalysts were readily fabricated via self-assembly from a p-phenylene-bridged bis-benzimidazolium salt with selected metal precursors. Among them, the NHC-Ru polymer demonstrated high catalytic activity and excellent stability as a solid molecular catalyst for the solvent-free reductive amination of biomass levulinic acid with inexpensive ammonium formate, furnishing a challenging unprotected 5-methyl-2-pyrrolidone quantitatively at a 0.15 mol% catalyst loading. The solid catalyst was readily recovered and reused for 37 runs without obvious loss of activity. Remarkably, a TON value up to 6.7 × 104 was achieved in a molar-scale reaction with a catalyst loading at 0.001 mol%. Inspired by the results of a preliminary mechanistic study, notably, one-pot tandem reductive reactions of LA with aldehydes or ketones were successfully developed, affording a variety of structurally intriguing and functional N-substituted 5-methyl-2-pyrrolidones in high chemo-selectivity with good to excellent yields.
- Sun, Zheming,Chen, Jiangbo,Tu, Tao
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p. 789 - 794
(2017/08/18)
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- O -Phthalaldehyde catalyzed hydrolysis of organophosphinic amides and other P(O)-NH containing compounds
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Over 50 years ago, Jencks and Gilchrist showed that formaldehyde catalyses the hydrolysis of phosphoramidate through electrophilic activation, induced by covalent attachment to its nitrogen atom. Given our interest in the use of aldehydes as catalysts, this work was revisited to identify a superior catalyst, o-phthalaldehyde, which facilitates hydrolyses of various organophosphorus compounds bearing P(O)-NH subunits under mild conditions. Interestingly, chemoselective hydrolysis of the P(O)-N bonds could be accomplished in the presence of P(O)-OR bonds.
- Li, Bin-Jie,Simard, Ryan D.,Beauchemin, André M.
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supporting information
p. 8667 - 8670
(2017/08/10)
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- Tryptophan Lyase (NosL): A Cornucopia of 5′-Deoxyadenosyl Radical Mediated Transformations
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Tryptophan lyase (NosL) is a radical S-adenosyl-l-methionine (SAM) enzyme that catalyzes the formation of 3-methyl-2-indolic acid from l-tryptophan. In this paper, we demonstrate that the 5′-deoxyadenosyl radical is considerably more versatile in its chem
- Bhandari, Dhananjay M.,Fedoseyenko, Dmytro,Begley, Tadhg P.
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supporting information
p. 16184 - 16187
(2016/12/27)
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- HIV INTEGRASE INHIBITORS
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The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
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- Polymethylhydrosiloxane derived palladium nanoparticles for chemo- and regioselective hydrogenation of aliphatic and aromatic nitro compounds in water
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Chemo- and regioselective hydrogenation of a wide range of aliphatic, unsaturated, aromatic and heteroaromatic nitro compounds into their corresponding amines has been achieved with highly efficient polysiloxane-stabilised "Pd" nanoparticles on NAP-magnesium oxide supports using an environmentally friendly hydrogenating agent, polymethylhydrosiloxane [PMHS] in water. Highly stable and active Pd nanoparticles were prepared by the reduction of NAP-Mg-PdCl4 with PMHS, which serves as a reducing agent as well as a capping agent. The well-dispersed palladium nanoparticles on NAP-MgO catalysts also exhibit excellent regioselectivity in the hydrogenation of dinitrobenzenes to the corresponding nitroanilines. The catalyst has high durability against sintering during the hydrogenation reaction and can be reused with no loss in its activity. This journal is the Partner Organisations 2014.
- Damodara, Dandu,Arundhathi, Racha,Ramesh Babu, T. Venkata,Legan, Margaret K.,Kumpaty, Hephzibah J.,Likhar, Pravin R.
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p. 22567 - 22574
(2014/06/23)
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- Generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, their preparation, compositions and use as medicaments
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This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.
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- Oligomeric aminodiol-containing compounds, libraries thereof, and process of preparing the same
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Oligomeric compounds comprising a plurality of aminodiol monomer subunits joined by linking groups are provided, as well as libraries of such compounds and processes for preparing the oligomeric compounds and libraries.
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- Continuous process for the preparation of amines
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Disclosed is a process for the preparation of amines by continuously feeding a carboxamide, aqueous alkaline hypohalite, and aqueous alkaline hydroxide to a first reaction zone to form a N-halocarboxamide, measuring the concentration of at least one reaction component in the effluent from the first reaction zone, and using the result of that measurement to control the feed rate of at least one of the feed components of to achieve at least 90% conversion of the carboxamide in the first reaction zone. The effluent from the first reaction zone is fed continuously to a second reaction zone where it further reacts to form an aqueous solution of an amine. The effluent from the second reaction zone may be fed continuously to a distillation column. The process is particularly useful for the preparation of cyclopropylamine.
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Page column 12-17
(2008/06/13)
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- Fused pyrazole derivatives bieng protein kinase inhibitors
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Compounds of Formula (I): salts or solvates or physiologically functional derivatives thereof, wherein Z is CH or N, and R1, (R2, and R4 are various substituent groups, are protein kinase inhibitors.
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- Pharmaceutically active pyrrolidine derivatives as bax inhibitors
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The present invention is related to new substituted pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of neurodegenerative disorders, diseases associated with polygultamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders renal hypoxia, hepatitis and AIDS. Said pyrrolidine derivatives display a modulatory and most notably a down-regulating-up to an inhibitory-activity with respect to the cellular death agonist Bax and/or the activation pathways leading to Bax and allows therefore to block the release of cytochrome (c). The present invention is furthermore related to novel pharmaceutically activity substituted pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of O, S, CRR, NOR, NNRR; A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO2-, —SO2NH—; —CH2-; B is either a group —(C═O)—NRR or represents a heterocyclic residue having the formula (II) wherein Q is NR, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5-6 membered aryl or heteroaryl ring.
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- Pharmaceutically active pyrrolidine derivatives
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The present invention is related to pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of CR6R7, NOR6, NNR6R7; A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO22—, —SO2NH—, —CH2—,B is either a group —(C═O)—NR8R9 or represents a heterocyclic residue having the formula (a) wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5-6 membered aryl or heteroaryl ring.
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- Tetracyclic benzimidazole derivatives and combinatorial libraries thereof
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The present invention relates to novel tetracyclic benzimidazole derivative compounds of the following formula: wherein R1to R10have the meanings described in here. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing tetracyclic benzimidazole derivative compounds.
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- 2-aminobenzoxazole derivatives and combinatorial libraries thereof
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The present invention relates to novel 2-aminobenzoxazole derivative compounds of the following formula: wherein R1 to R4 and Z have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminobenzoxazole derivative compounds.
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- 4-unsubstituted dihydroisoquinolinone derivatives and combinatorial libraries thereof
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The present invention relates to novel dihydroisoquinolinone (DHQ) derivative compounds of the following formula: wherein R1to R7, X, Y, Z, b, c and d have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing DHQ derivative compounds.
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- 2-aminopyridine derivatives and combinatorial libraries thereof
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The present invention relates to novel 2-aminopyridine derivative compounds of the following formula: wherein R1to R5have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminopyridine derivative compounds.
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- Process for the preparation of cyclopropylamine
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Cyclopropylamine is prepared from butyrolactone by a process comprising: (a) reacting butyrolactone with hydrogen chloride, thereby yielding chlorobutyric acid, (b) esterifying said chlorobutyric acid with a primary or secondary alcohol having 4-8 carbon atoms, (c) cyclizing the ester with an alkali metal alcoholate of a primary alcohol having 1-3 carbon atoms to give a mixture of cyclopropanecarboxylic acid esters, (d) converting the cyclopropanecarboxylic acid ester mixture into cyclopropanecarboxylic acid amide by reacting the ester mixture with ammonia, and (e) reacting said cyclopropanecarboxylic acid amide with hypohalite ion in a basic medium, thereby forming cyclopropylamine.
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- Thiazoline derivatives
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Object: To provide compounds useful as inhibitors of blood platelet aggregation for intravenous administration. Constitution: A thiazoline derivative represented by the formula: STR1 ?wherein R1 is a hydroxyl group, an alkoxy group, a cycloalkoxy group or a group represented by the formula: R4 NH-- (wherein R4 is a cycloalkyl group), R2 is an alkyl group, a cycloalkyl group or a phenylalkyl group, R3 is a hydrogen atom or an alkyl group, and n is an integer of 2 to 9! or a salt thereof.
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- Preparation process of aminoacetamide derivative
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Disclosed herein are novel processes for preparing aminoacetamide derivatives, wherein: (1) a secondary amine is reacted with a 2-haloacetamide in the presence or absence of at least one solvent selected from water, lower alcohols, aromatic solvents and acetic acid esters; (2) an N-benzylideneamine derivative is reacted with dimethyl sulfate or diethyl sulfate to form a secondary amine, and this secondary amine is then reacted with a 2-haloacetamide; and (3) a primary amine is reacted with benzaldehyde to form an N-benzylideneamine derivative, this product is then reacted with dimethyl sulfate or diethyl sulfate to form a secondary amine, and this secondary amine is further reacted with a 2-haloacetamide. The 2-aminoacetamide derivatives are useful as intermediates for the preparation of novel antibiotics.
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- Anti-tumor platinum(II) complexes and process for the preparation thereof
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The present invention relates to anti-tumor platinum complexes represented by the general formula I: STR1 wherein A is selected from the group consisting of ammine and mondentate primary alkyl- and cycloalkylamines having 1-3 carbon atoms such as methyl, ethyl, n-propyl-, isopropyl- and cyclopropylamines, or the two amine groups may be combined to be a bidentate diamine of the chelating form AA such as ethylenediamine, 1,2-diaminocyclohexane, and 2-hydroxy-1,3-diaminopropane, and X is either vinylene(--CH=CH--) or ethylene (--CH2 --CH2 --) when it is bound to two sulfur atoms in a cyclic form or represents two methyl groups separately bound to each sulfur atom.
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- 3-benzyl-1,2,4-triazolo[4,3-α] pyrazines
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3-benzyl-1,2,4-triazolo [4,3-α] pyrazines are prepared. They are useful as anticonvulsants.
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- 3-amino-5-methyl-1H-pyrazole-4-carboxylic acids and esters thereof as anticonvulsants, muscle relaxants and anxiolytics
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A novel method of controlling epilepsy, muscle tension, muscular spasticity, and anxiety in living animal bodies by administering compounds of the formula: STR1 wherein: R1 is hydrogen, loweralkyl or a pharmaceutically acceptable cation; R2 and R3, same or different, are hydrogen, loweralkyl, aryl, cycloalkyl, loweralkenyl, 1-adamantyl, heterocyclicaminoalkyl, diloweralkylaminoloweralkyl, or R2 with R3 and adjacent nitrogen may form a heterocyclic ring structure; and the pharmaceutical acceptable acid salts, and tautomeric isomers thereof; and novel pharmaceutical compositions therefor are disclosed.
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- Very Soluble and Photostable Perylene Fluorescent Dyes
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The synthesis of perylene dyes 2 with two terminal alkyl groups is described.Long-chain alkyl groups do not increase, but diminish solubility.Cycloalkyl substituents give a minimum of solubility with medium sized rings and a maximum with the cyclotetradecyl derivative (2p).Very high solubility in organic solvents is attained by substitution with secondary alkyl residues having two long chains.One of them, the dye with the 1-hexylheptyl substituent (2v), exhibits a solubility of more than 100g/l in most solvents, a fluorescent quantum yield of about 100 percent, and a very high photostability, thus making it suitable for special applications.
- Demming, Stefan,Langhals, Heinz
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p. 225 - 230
(2007/10/02)
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- Phenyloxoalkyl piperidines and the pharmaceutical compositions containing them
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This invention relates to novel piperidines substituted on the nitrogen atom with a (phenyloxo alkyl) group as well as the processes for their production.
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- Preparation of esters of phosphorus acids
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Esters of phosphorus acids are prepared by an improved process whereby aromatic alcohols and phosphorus halides are reacted at specified temperatures in the presence of amine catalysts thereby providing high yields of substantially pure esters and allowing preparation of selected halogen-containing mono- and di-esters of phosphorus acids wherein halogen is directly bonded to phosphorus having substantially no side reactant contamination. The phosphorus esters are useful as intermediates in the preparation of plasticizers, oil additives and functional fluids.
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