- Switchable synthesis of cyclic carbamates by carbon dioxide fixation at atmospheric pressure
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The base-promoted switchable synthesis of five- and six-membered cyclic carbamates using atmospheric pressure carbon dioxide as the C1 source was developed. The chemoselectivity of products was simply controlled by changing bases and solvents. The reaction proceeds effectively under mild conditions, affording valuable cyclic carbamates. Experimental results and DFT studies revealed the reaction mechanism.
- Toda, Yasunori,Shishido, Minoru,Aoki, Tatsuya,Sukegawa, Kimiya,Suga, Hiroyuki
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supporting information
p. 6672 - 6675
(2021/07/13)
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- Synthesis of Novel Hybrid 4 H -Pyran-lipoic and 4 H -Pyran-azetidine Derivatives
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In this study, a molecular hybridization strategy was used to design and synthesize two novel series of hybrid compounds: 4 H -pyran-lipoic and 4 H -pyran-azetidine, employing ammonium hydroxide and involving the participation of aldehydes, malononitrile, and compounds derived from β-ketoesters to obtain the products with good yields.
- Hernández-Borja, Fernando,Contreras, Leticia,López, Julio,Alcaraz, Yolanda,Cruz, David,Estrada-Soto, Samuel,Delgado, Francisco,Vázquez, Miguel A.
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p. 1020 - 1026
(2017/11/29)
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- 2 - (2, 4, 5 - SUBSTITUTED -ANILINO) PYRIMIDINE DERIVATIVES AS EGFR MODULATORS USEFUL FOR TREATING CANCER
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The present invention relates to certain 2-(2,4,5-substituted-anilino) pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.
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Page/Page column 96
(2013/03/26)
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- Synthesis and biological evaluation of novel azetidine derivatives as dopamine antagonist
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In this study, azetidine derivatives were evaluated for their potency as dopaminergic antagonist. The study comprised derivatives substituted in 3-position with amide moiety. Further, the phenyl moiety of amide was modified at 2, 3, or 4-position. The substituted compounds were biologically evaluated for their affinity for D2 and D4 receptors. The most potent D2 and D4 antagonist among these compounds appeared to be the N-(1-benzhydryl-azetidin-3yl)-2-bromo-benzamide and N-(1-benzhydryl-azetidin-3yl)-4-bromo-benzamide, respectively. Various docking interactions of CPPMA with the D4 receptor and the same for compound 5 i.e., N-(1-benzhydryl-azetidin-3yl)-4-bromo-benzamide were found to have good correlation with observed biological activity.
- Metkar, Shashikant D.,Bhatia, Manish S.,Desai, Uday V.
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p. 5982 - 5989
(2013/11/06)
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- DMAP-catalyzed synthesis of 2-oxazolidinones from corresponding halohydrins using KOCN/DMF
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We report facile and simple synthesis of a variety of 2-oxazolidinones from the corresponding halohydrins by reaction with KOCN in DMF catalyzed by DMAP. DMAP and temperature play key roles in enriching the yield of 2-oxazolidinones. A few examples in this Letter are applicable to pharmaceutically important processes.
- Chinnam Naidu,Ravi Babu,Gangaiah,Mukkanti,Madhusudhan
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experimental part
p. 1226 - 1229
(2010/04/23)
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- Syntheses and pharmacokinetic studies of prodrug esters for the development of oral carbapenem, L-084
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We discovered an orally active carbapenem, L-084, through pharmacokinetic studies on various prodrug esters of (1R,5S,6S)-6-[(R)-1-hydroxyethyl]-1-methyl- 2-[1-(1,3-thiazolin-2-yl)azetidin-3-yl]thio-1-carbapen-2-em-3-carboxylic acid (LJC11,036). L-084 showed a strong antimicrobial activity against Gram-positive and Gram-negative bacteria and exhibited the highest intestinal absorption among synthesized prodrugs of LJC11,036. Japan Antibiotics Research Association.
- Isoda, Takeshi,Ushirogochi, Hideki,Satoh, Koichi,Takasaki, Tsuyoshi,Yamamura, Itsuki,Sato, Chisato,Mihira, Ado,Abe, Takao,Tamai, Satoshi,Yamamoto, Shigeki,Kumagai, Toshio,Nagao, Yoshimitsu
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p. 241 - 247
(2007/10/03)
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- Cathepsin cysteine protease inhibitors
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This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of Cathepsins K and L. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
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- Derivatives of 1-(disubstituted phenoxy)-3-amino-2-hydroxypropanes
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N-Diphenylmethyl and o-biphenylenemethyl derivatives of 1-(disubstituted phenoxy)-3-amino-2-hydroxypropane and their salts are useful for combatting cerebrovascular insufficiency and producing psychostimulation in humans and other animals. The compounds, of which 1-(2-methoxy-4-allylphenoxy)-2-hydroxy-3-diphenylmethylamino-propane is a typical embodiment, can be prepared by a number of synthetic routes.
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