933770-71-9Relevant articles and documents
HETEROCYCLIC AMIDES AS ROCK INHIBITORS
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Page/Page column 81, (2011/10/03)
The present invention relates to new kinase inhibitors of formula (I), more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
Investigation of oxacycle formation by base-promoted endo-mode ring-closing reaction of allenes
Kitagaki, Shinji,Kawamura, Takamasa,Shibata, Daisuke,Mukai, Chisato
experimental part, p. 11086 - 11095 (2009/04/11)
The base-promoted endo-mode ring closure of electron-withdrawing group-substituted allenes provided the following interesting results: (1) the endo-mode ring-closing reaction of 1-(benzyloxycarbonyl)-1-(ω-hydroxyalkyl)allenes smoothly proceeded during the
Studies of ring-closing mode of 4-hydroxy-2-vinylidenebutanoates: 5-exo-trig versus 5-endo-dig
Kitagaki, Shinji,Shibata, Daisuke,Mukai, Chisato
, p. 1735 - 1738 (2008/02/05)
The ring-closing mode of benzyl 4-hydroxy-2-vinylidenebutanoates (5-exo-trig vs 5-endo-dig) could precisely be controlled in a highly selective manner by the proper choice of conditions (solvent and base).
Asymmetric Hydroformylation of Heterocyclic Olefins Catalyzed by Chiral Phosphine-Phosphite-Rh(I) Complexes
Horiuchi, Toshihide,Ohta, Tetsuo,Shirakawa, Eiji,Nozaki, Kyoko,Takaya, Hidemasa
, p. 4285 - 4292 (2007/10/03)
Asymmetric hydroformylation of heterocyclic olefins catalyzed by phosphine-phosphite-Rh(I) complexes has been investigated. Hydroformylation of symmetrical heterocyclic olefins such as 2,5-dihydrofuran, 3-pyrroline derivatives, and 4,7-dihydro-1,3-dioxepin derivatives afforded the optically active aldehydes as single products in 64-76% ee. Unsymmetrical substrates such as 2,3-dihydrofuran and N-(tert-butoxycarbonyl)-2-pyrroline gave a mixture of regioisomers. From N-(tert-butoxycarbonyl)-2-pyrroline was obtained N-(tert-butoxycarbonyl)pyrrolidine-2-carbaldehyde in 97% ee. The hydroformylation products from 2,5-dihydrofuran and N-(tert-butoxycarbonyl)-3-pyrroline have the opposite configurations to those from 2,3-dihydrofuran and N-(tert-butoxycarbonyl)-2-pyrroline, respectively, with the same catalyst. The new phosphine-phosphite ligand (R,S)-3,3′-Me2-BINAPHOS [= (A)-2-(diphenylphosphino)-1,1′-binaphthalen-2′-yl (S)-3,3′-dimethyl-1,1′-binaphthalene-2,2′-diyl phosphite] was prepared and its hydridorhodium complex was characterized by NMR spectroscopy. Using (R,S)-3,3′-Me2-BINAPHOS as a ligand, the enantioselectivity was improved for some substrates. In addition, higher catalytic activity was observed with this ligand for most of the substrates employed.
Chemoenzymatic Approach to the Synthesis of the Antiviral Agents Penciclovir and Famciclovir in Isotopically Chiral Labelled Form
Sime, John T.,Barnes, Roger D.,Elson, Stephen W.,Jarvest, Richard L.,O'Toole, Kevin J.
, p. 1653 - 1658 (2007/10/02)
The antiviral agents penciclovir and famciclovir have been synthesised in isotopically chiral form.The synthesis of (+)-methyl 4-benzyloxy-2-(hydroxymethyl)butanoate 12a by use of enzymatic hydrolysis catalysed by the lipase from Candida cylindrac