Synthesis of tetrahydroisoquinolines through TiCl4-mediated cyclization and Et3SiH reduction
A versatile and efficient telescoped reaction sequence for the synthesis of tetrahydroisoquinolines (THIQs) is reported that uses TiCl4 to promote cyclization of a benzylaminoacetal derivative and Et3SiH for reduction of the intermediate 4-hydroxy-THIQ. This method is complimentary to the classical Pomeranz-Fritsch and related reactions since it tolerates electron-withdrawing substituents and allows access to 8-substituted THIQs.
Shi, Zeyu,Xiao, Qiong,Yin, Dali
supporting information
p. 729 - 732
(2019/10/02)
Ultrasound assisted one-pot synthesis of benzo-fused indole-4,9-dinones from 1,4-naphthoquinone and α-aminoacetals
A one-pot synthesis of benzo[f]indole-4,9-diones from 1,4-naphthoquinone with α-aminoacetals has been developed. This method provides a straightforward synthesis of benzo[f]indole-4,9-diones via intramolecular nucleophilic attack of aminoquinones to aldehydes under mild reaction conditions. The detailed mechanism was also investigated.
Luu, Quang H.,Guerra, Jorge D.,Casta?eda, Cecilio M.,Martinez, Manuel A.,Saunders, Jong,Garcia, Benjamin A.,Gonzales, Brenda V.,Aidunuthula, Anushritha R.,Mito, Shizue
supporting information
p. 2253 - 2256
(2016/05/10)
ARYL CARBOXAMIDE DERIVATIVES AS SODIUM CHANNEL INHIBITORS FOR TREATMENT OF PAIN
The present invention provides compounds that are inhibitors of voltage-gated sodium channels (Nav), in particular Nav 1.7, and are therefore useful for the treatment of diseases treatable by inhibition of these channels, in particular, chronic pain disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
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Page/Page column 76
(2011/09/19)
New substituted isoquinoline and isoquinolinone derivatives
The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
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Page/Page column 14
(2010/04/23)
SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES
The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
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Page/Page column 51-52
(2008/12/06)
CYCLOALKYLAMINE SUBSTITUTED ISOQUINOLONE AND ISOQUINOLINONE DERIVATIVES
The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula 1 useful for the treatment and prevention of diseases associated with Rho-kinase and Rho- kinase mediated phosphorylation of myosin light chain phosphatase, and composition containing such compound
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Page/Page column 40-41
(2008/12/06)
Multisubstrate inhibitors of dopamine β-hydroxylase. 2. Structure-activity relationships at the phenethylamine binding site