- Tailored near-infrared contrast agents for image guided surgery
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The success of near-infrared (NIR) fluorescence to be employed for intraoperative imaging relies on the ability to develop a highly stable, NIR fluorescent, nontoxic, biocompatible, and highly excreted compound that retains a reactive functionality for co
- Njiojob, Costyl N.,Owens, Eric A.,Narayana, Lakshminarayana,Hyun, Hoon,Choi, Hak Soo,Henary, Maged
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- 4-Amino-1,8-naphthalimide-based fluorescent sensor with high selectivity and sensitivity for Zn2 + imaging in living cells
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A new 4-amino-1,8-naphthalimide-based fluorescent sensor with iminodiacetic acid as receptor, was synthesized and characterized. Under physiological pH conditions, it demonstrates high selectivity and sensitivity for sensing Zn 2 + with about 5
- Liu, Da-Ying,Qi, Jing,Liu, Xiao-Yan,He, Hua-Rui,Chen, Jia-Tong,Yang, Guang-Ming
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Read Online
- Study on a New Method for Synthesis of Mirabegron
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Mirabegron is a muscle relaxing drug for the treatment of overactive bladder. The existing synthetic methods for mirabegron produced intermediate product 4-(2-(phenethylamino)ethyl)aniline, which complicated the final product purification process. In this study, we designed a new synthetic route for mirabegron with low cost starting materials and a production of mirabegron at a 99.6% purity and a 61% overall yield. Particularly, this new synthetic route did not produce side product 4-(2-(phenethylamino)ethyl)aniline, which significantly simplified the product purification process.
- Xu, Guiqing,Mao, Shen,Mao, Longfei,Jiang, Yuqin,Zhou, Yong,Shen, Jiaxuan,Dong, Wenpei
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Read Online
- PYRAZOLE-OXAZOLIDINONE COMPOUND FOR ANTI-HEPATITIS B VIRUS
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The present invention discloses a pyrazole-oxazolidinone compound having anti-hepatitis B virus activity, which has the structure of formula (I), wherein each variable is as defined herein.
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Paragraph 0342-0344
(2019/06/07)
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- A process for preparing a broad pH fluorescent probe of the organic compound and use thereof (by machine translation)
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The present invention discloses a process for the preparation of a wide range of fluorescent probe in the pH of the organic compound, the organic compound can be produced according to the actual need to carry out any proportion of combination, and can be fixed in the hydrophilic high polymer further preparing and detecting water environment acidity and alkalinity of the product. The product can be realized to the pH value of the continuous measuring, thereby greatly improving the efficiency, sensitivity and repeatability. (by machine translation)
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Paragraph 0081; 0084; 0085
(2018/04/03)
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- Organic compound for detecting content of metal ions in water and application of organic compound
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The invention discloses an organic compound for detecting the content of metal ions. The compound adopts N-carbethoxy-N-methylpyridaniline as a metal ion complexing body, chromophore or fluorophore isintroduced into a molecule to generate a developing ind
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Paragraph 0027
(2018/09/14)
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- A method of preparing P ethylamine
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The invention discloses a preparation method of p-aminophenylethylamine, belonging to the technical field of organic synthesis. The technical scheme is as follows: the preparation method comprises the following steps: by using p-nitrophenylethanol as a raw material, carrying out catalytic hydrogenation to reduce the para-position nitro groups of the p-nitrophenylethanol into amino groups, carrying out Boc acid anhydride protection on the para-position nitro groups, carrying out substitution reaction on hydroxy groups with sulfonyl chloride compounds to obtain sulfonic acid compounds, aminating, and finally, removing Boc groups to obtain the p-aminophenylethylamine. The preparation process is simple and easy to implement, and has the advantages of cheap and accessible raw materials, higher reaction efficiency and favorable repetitiveness.
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- Selective Hydrogenation of Nitriles to Primary Amines Catalyzed by a Cobalt Pincer Complex
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The catalytic hydrogenation of nitriles to primary amines represents an atom-efficient and environmentally benign reduction methodology in organic chemistry. This has been accomplished in recent years mainly with precious-metal-based catalysts, with a single exception. Here we report the first homogeneous Co-catalyzed hydrogenation of nitriles to primary amines. Several (hetero)aromatic, benzylic, and aliphatic nitriles undergo hydrogenation to the corresponding primary amines in good to excellent yields under the reaction conditions.
- Mukherjee, Arup,Srimani, Dipankar,Chakraborty, Subrata,Ben-David, Yehoshoa,Milstein, David
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supporting information
p. 8888 - 8891
(2015/08/03)
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- Activation of electrophilicity of stable Y-delocalized carbamate cations in intramolecular aromatic substitution reaction: Evidence for formation of diprotonated carbamates leading to generation of isocyanates
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Although cations with three heteroatoms, such as monoprotonated guanidine and urea, are stabilized by Y-shaped conjugation and such Y-conjugated cations are sufficiently basic to be further protonated (or protosolvated) to dications in strongly acid media, only O-monoprotonated species have been detected in the case of carbamates even in magic acid. We found that the trifluoromethanesulfonic acid-catalyzed cyclization of arylethylcarbamates proceeds to afford dihydroisoquinolones in high yield. In strong acids, methyl carbamates are fully O-monoprotonated, and these monocations do not undergo cyclization even under heating. But, as the acidity of the reaction medium is further increased, the cyclization reaction of methyl phenethylcarbamates starts to proceed as a first-order reaction, with a linear relationship between rate and acidity. The sign and magnitude of the entropy of activation ΔS ? were found to be similar to those of other AAc1 reactions. These results strongly support the idea that further protonation of the O-protonated carbamates is involved in the cyclization, but the concentration of the dications is very low and suggests that the rate-determining step is dissociation of methanol from the diprotonated carbamate to generate protonated isocyanate, which reacts with the aromatic ring. Therefore, O-protonated carbamates are weak bases in sharp contrast to other Y-shaped monocations.
- Kurouchi, Hiroaki,Kawamoto, Kyoko,Sugimoto, Hiromichi,Nakamura, Satoshi,Otani, Yuko,Ohwada, Tomohiko
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p. 9313 - 9328,16
(2012/12/11)
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- Instantaneous SmI2/H2O/amine mediated reduction of nitroalkanes and α,β-unsaturated nitroalkenes
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A rapid method for efficient reduction of nitroalkanes and α,β-unsaturated nitroalkenes using SmI2/H2O/amine has been developed.
- Ankner, Tobias,Hilmersson, G?ran
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p. 5707 - 5710
(2008/02/10)
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- Indium Mediated Reduction of Nitro and Azide Groups in the Presence of HCl in Aqueous Media
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Indium mediated reduction of azide and nitro groups in the presence of HCl (1.5 equiv based on indium) at room temperature in aqueous THF successfully provided the corresponding amine in high to quantitative yields. Under the some reaction conditions, selective reduction of azide and nitro group in the presence of vinyl group could be accomplished.
- Lee, Jung Gyu,Choi, Kyung Il,Koh, Hun Yeong,Kim, Youseung,Kang, Yonghan,Cho, Yong Seo
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- Pd/C(en)-catalyzed chemoselective hydrogenation with retention of the N-Cbz protective group and its scope and limitations
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A chemoselective method for the hydrogenation of acetylene, olefin, azide, nitro and benzyl ester functionalities with retention of the aliphatic N-Cbz group was established. The chemoselectivity was accomplished by using a combination of 5% Pd/C-ethylenediamine [5% Pd/C(en)] and THF (or 1,4-dioxane) as a solvent, and the scope and limitations of this methodology were investigated. These results reinforce the utility of N-Cbz protective groups in synthetic chemistry, especially in peptide synthesis. (C) 2000 Elsevier Science Ltd.
- Hattori, Kazuyuki,Sajiki, Hironao,Hirota, Kosaku
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p. 8433 - 8441
(2007/10/03)
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- Studies of Reduction with Dimethoxyborane-Transition Metal Salt Systems. I. Reduction of Nitriles, Aldehydes and Ketones with Dimethoxyborane-Transition Metal Salt Systems
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The reduction of a variety of functional groups with new dimethoxyborane-transition metal salt systems was investigated.The dimethoxyborane-cobaltous chloride system reduced nitriles and aldehydes under mild conditions in good yields, and the dimethoxyborane-nickelous chloride system similarly reduced nitriles, aldehydes, olefin and ketones.The other functional groups tested were unaffected by these systems.Keywords reduction; nitrile; aldehyde; ketone; dimethoxyborane; transition metal salt; dimethoxyborane-cobaltous chloride system; dimethoxyborane-nickelous chloride system
- Nose, Atsuko,Kudo, Tadahiro
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p. 808 - 810
(2007/10/02)
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- SELECTIVE REDUCTION OF NITROARYLALKYLNITRILES WITH HYDRAZINE AND A METAL CATALYST
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The selectivity in the catalytic reduction of nitroalkylarylnitriles with hydrazine and metal catalysts was studied.
- Adger, Brian M,Young, Richard G
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p. 5219 - 5222
(2007/10/02)
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- Novel monoazo and disazo colorants from aminoalkylanilines and bis(aminoalkyl)anilines
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Water-insoluble azo dyestuffs of the formula STR1 and water-soluble acid addition salts thereof useful for coloring natural fibers, synthetic fiber-forming material and cellulosic materials as well as in the manufacture of paper, varnishes, inks, coatings and plastics in which A represents an azoic coupling radical derived from a coupling component selected from the group consisting of arylides of hydroxy-substituted carbocyclic aromatic carboxylic acids, 1-aryl-5-hydroxy-pyrazoles, 6-amino-1-naphthol-3-sulfonic acid, and compounds having an enolizable ketomethylene group of the formula STR2 R is hydrogen, lower-alkyl, lower-alkoxy or halogen; R2 is hydrogen, lower-alkyl, lower-alkoxy, halogen, aminomethyl or 2-aminoethyl with the proviso that A is other than β-naphthol when R2 is aminomethyl or 2-aminoethyl; R1 and R3 are the same or different and are each hydrogen, lower-alkyl, lower-alkoxy, halogen or aminomethyl with the proviso that at least one of R1 and R3 is aminomethyl when R2 is other than aminomethyl or 2-aminoethyl; and n represents an integer whose value is 1 or 2 and corresponds to the number of azo linkages, which dyestuffs are obtained by coupling a diazotized amine of the formula STR3 in which R, R1, R2 and R3 are as defined above with said coupling component.
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- Monoazo and diazo colorants from aminoalkylanilines and bis(aminoalkyl)anilines
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Water-insoluble azo dyestuffs of the formula STR1 AND WATER-SOLUBLE ACID ADDITION SALTS THEREOF USEFUL FOR COLORING NATURAL FIBERS, SYNTHETIC FIBER-FORMING MATERIAL AND CELLULOSIC MATERIALS AS WELL AS IN THE MANUFACTURE OF PAPER, VARNISHES, INKS, COATINGS AND PLASTICS IN WHICH A represents an azoic coupling radical derived from a coupling component selected from the group consisting of arylides of hydroxysubstituted carbocyclic aromatic carboxylic acids, 1-aryl-5-hydroxypyrazoles, 6-amino-1-naphthol-3-sulfonic acid, and compounds having an enolizable ketomethylene group of the formula STR2 R is hydrogen, lower-alkyl, lower-alkoxy or halogen; R2 is hydrogen, lower-alkyl, lower-alkoxy, halogen, aminomethyl or 2-aminoethyl with the proviso that A is other than β-naphthol when R2 is aminomethyl or 2-aminoethyl; R1 and R3 are the same or different and are each hydrogen, lower-alkyl, lower-alkoxy, halogen or aminomethyl with the proviso that at least one of R1 and R3 is aminomethyl when R2 is other than aminomethyl or 2-aminoethyl; and n represents an integer whose value is 1 or 2 and corresponds to the number of azo linkages, which dyestuffs are obtained by coupling a diazotized amine of the formula STR3 in which R, R1, R2 and R3 are as defined above with said coupling component.
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- Manufacture of aromatic amino compounds
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A process for producing an aromatic amine comprises heating an aromatic sulfonate and a metal amide in liquid ammonia in a closed reactor at a temperature of at least 40° C to produce a metal arylamide and reacting the resultant metal arylamide with water or lower aliphatic alcohol to produce an aromatic amine.
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