- A novel homochiral metal-organic framework with an expanded open cage based on (: R)-3,3′-bis(6-carboxy-2-naphthyl)-2,2′-dihydroxy-1,1′-binaphthyl: synthesis, X-ray structure and efficient HPLC enantiomer separation
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A new homochiral metal-organic framework (MOF) with an expanded open cage based on the (R)-3,3′-bis(6-carboxy-2-naphthyl)-2,2′-dihydroxy-1,1′-binaphthyl ligand was synthesized and utilized as a novel chiral stationary phase for high-performance liquid chromatography. Twelve racemates including sec-alcohols, sulfoxides, epoxides, lactone, 1,3-dioxolan-2-one, and oxazolidinone were used as analytes for evaluating the separation properties of the chiral-MOF-packed column. Experimentally, the homochiral MOF offered good molecular recognition ability, which suggests good prospects for the application of chiral MOFs as stationary phases for enantioseparation.
- Tanaka, Koichi,Kawakita, Tomohiro,Morawiak, Maja,Urbanczyk-Lipkowska, Zofia
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p. 487 - 493
(2019/01/21)
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- PYRAZOLO-TRIAZINE AND/OR PYRAZOLO-PYRIMIDINE DERIVATIVES AS SELECTIVE INHIBITOR OF CYCLIN DEPENDENT KINASE
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The present invention relates to pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[l,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.
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Page/Page column 50; 57-58
(2019/11/04)
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- A practical and enantiospecific synthesis of (-)-(R)- and (+)-(S)-piperidin-3-ols
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A highly enantiospecific, azide-free synthesis of (-)-(R)- and (+)-(S)-piperidin-3-ol in excellent yield was developed. The key step of the synthesis involves the enantiospecific ring openings of enantiomerically pure (R)- and (S)-2-(oxiran-2-ylmethyl)-1H-isoindole-1,3(2H)-diones with the diethyl malonate anion and subsequent decarboxylation.
- Babu, Meruva Suresh,Raghunadh, Akula,Ramulu, Konda,Dahanukar, Vilas H.,Syam Kumar, Unniaran K.,Dubey, P. Kumar
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p. 1507 - 1515
(2015/02/19)
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- 2-Methyltetrahydrofuran as a suitable green solvent for phthalimide functionalization promoted by supported KF
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An efficient chemoselective nitrogen functionalization of phthalimides by using KF-Alumina in 2-methyltetrahydrofuran, a solvent obtained from renewal sources, is described.
- Pace, Vittorio,Hoyos, Pilar,Fernandez, Maria,Sinisterra, Jose V.,Alcantara, Andres R.
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supporting information; experimental part
p. 1380 - 1382
(2010/09/05)
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- 1-Amido-3-(2-hydroxyphenoxy)-2-propanol derivatives and a process for preparing 2-amidomethyl-1,4-benzodioxane derivatives
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An 1-amido-3-(2-hydroxyphenoxy)-2-propanol derivative represented by the following formula (1), wherein cycle A may have further 1 to 4 substituents, and said substituent means a substituent selected from the group consisting of saturated or unsaturated C
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Page/Page column 5
(2008/06/13)
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- ACYCLIC 1,3-DIAMINES AND USES THEREFOR
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This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted -acyclic diamines according to Formula (I): or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a combination thereof, wherein: the R groups are as defined herein. The present invention also relates to a pharmaceutical composition and a method of treatment using the compound of Formula (I).
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Page/Page column 112-113
(2010/10/20)
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- Novel series of highly potent non-peptide growth hormone secretagogues with improved bioavailability
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The discovery and the SAR of acylproline derivatives as highly potent growth hormone secretagogues (GHSs) with good oral bioavailability are described. One representative compound, N-[3-(2,2-dimethylpropylamino)-2-hydroxypropyl]-2(R)-[1-(2,2-dimethylpropionyl)pyrrolidine-2(S)- carbonylamino]-3-naphthalen-2-ylpropionamide (4e), showed potent GHS activity (ED50=1 nM) and good oral bioavailability (BA=33.2%). Moreover, the optically pure N-[3-(2,2-dimethylpropylamino)-2(S)-hydroypropyl]-2(R)-[1-(2,2-dimethylpropionyl)pyrrolidine-2(S)-carbonylamino]-3-naphthalen-2- ylpropionamide ((2S)-4e) showed a good metabolic stability against in vitro clearance (human liver microsome) with potent GHS activity.
- Ishige, Hirohide,Ishiyama, Nobuo,Mimura, Mitsuo,Hayashida, Mitsuo,Okuno, Tadashi,Ukai, Kiyoharu,Kiyofuji, Takeshi,Yoneda, Yasuo,Tauchi, Shinji,Aoyama, Akinori,Inoguchi, Kiyoshi
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p. 561 - 566
(2007/10/03)
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- Novel amide derivatives as growth hormone secretagogues
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Disclosed are the novel compounds as growth hormone secretagogues represented by the structural Formula I: wherein R1 is, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, substitu
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Page/Page column 23
(2010/02/15)
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- PROCESS FOR PREPARATION OF OPTICALLY ACTIVE 1-SUBSTITUTED AMINO-2,3-EPOXYPROPANES, INTERMEDIATES FOR THE SYNTHESIS THEREOF AND PROCESS FOR PREPARATION OF THE INTERMEDIATES
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The present invention provides an industrial process for effectively and advantageously preparing optically active 1-substituted amino-2,3-epoxypropanes useful as intermediates for preparing agricultural chemicals and medical products from optically activ
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Page/Page column 24
(2008/06/13)
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- Process for preparing glycidylphthalimide
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A process for preparing glycidylphtalimide or its optically active compound by reacting a phthalimide alkali metal salt with an epihalohydrin or an optically active epihalohydrin in an alcohol solvent; or by reacting phthalimide with an epihalohydrin or an optically active epihalohydrin in the presence of an alkali metal carbonate, an alkali metal hydrogencarbonate or a quaternary ammonium salt to obtain a N-(3-halogeno-2-hydroxypropyl)phthalimide and then by cyclizing the product with an alkali metal alkoxide.
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- The preparation and alkylation of a butanedione-derived chiral glycine equivalent and its use for the synthesis of α-amino acids and α,α-disubstituted amino acids
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A benzyloxycarbonyl protected glycine equivalent 2 has been prepared in enantiopure form and has been used in the synthesis of both α-substituted amino acids and α,α-disubstituted amino acids. The process involved deprotonation to form the corresponding enolates which underwent stereoselective alkylation with various electrophiles and upon hydrolysis gave the corresponding amino acid derivatives as enantiomerically pure products.
- Harding, Christopher I.,Dixon, Darren J.,Ley, Steven V.
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p. 7679 - 7692
(2007/10/03)
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- Studies on quinazolines. 6. Asymmetric synthesis of (S)-(+)- and (R)-(-)-3-[[4-(2-methoxyphenyl)piperazin-1-yl]methyl]-5-methylthio-2,3- dihydroimidazo[1,2-c]quinazolines
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The titled compounds have been synthesized in five steps from commercially available (R)-(+) and (S)-(-)-glycidol. The overall yield was about 29% with ee>98.5%. Copyright
- Gutcait, Alexander,Wang, Kuang-Chao,Liu, Hsiu-Wen,Chern, Ji-Wang
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p. 1641 - 1648
(2007/10/03)
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