1075-11-2Relevant articles and documents
Synthesis of Indole-Dihydroisoquinoline Sulfonyl Ureas via Three-Component Reactions
Pearson, Stuart E.,Fillery, Shaun M.,Goldberg, Kristin,Demeritt, Julie E.,Eden, Jonathan,Finlayson, Jonathan,Patel, Anil
, p. 4963 - 4981 (2018)
Isoquinolines activated with sulfamoyl chlorides were reacted with indoles in a 3-component reaction to generate a library of dihydroisoquinoline derivatives. Using a differential protecting group strategy, products could be further derivatised. Synthesis of isoquinoline starting materials using several different methods is also described.
PhenoFluor: Practical synthesis, new formulation, and deoxyfluorination of heteroaromatics
Fujimoto, Teppei,Becker, Fabian,Ritter, Tobias
supporting information, p. 1041 - 1044 (2014/11/07)
We report a practical synthesis method of the reagent PhenoFluor on decagram scale, provide a new formulation of PhenoFluor as a toluene solution, which should decrease challenges associated with the moisture sensitivity of the reagent, and expand the substrate scope of deoxyfluorination with PhenoFluor to heteroaromatics.
Pd-catalyzed nucleophilic fluorination of aryl bromides
Lee, Hong Geun,Milner, Phillip J.,Buchwald, Stephen L.
supporting information, p. 3792 - 3795 (2014/04/03)
On the basis of mechanism-driven reaction design, a Pd-catalyzed nucleophilic fluorination of aryl bromides and iodides has been developed. The method exhibits a broad substrate scope, especially with respect to nitrogen-containing heteroaryl bromides, and proceeds with minimal formation of the corresponding reduction products. A facilitated ligand modification process was shown to be critical to the success of the reaction.
CYCLOALKYLAMINE SUBSTITUTED ISOQUINOLONE DERIVATIVES
-
Page/Page column 44, (2008/12/06)
The invention relates to 6-substituted isoquinolone 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 composit
CYCLOALKYLAMINE SUBSTITUTED ISOQUINOLINE DERIVATIVES
-
Page/Page column 46, (2008/12/06)
The invention relates to 6-substituted isoquinoline 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.
CYCLOALKYLAMINE SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES
-
Page/Page column 48, (2008/12/06)
The invention relates to 6-substituted isoquinoline and isoquinolinone 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.
ISOQUINOLINE DERIVATIVES AS INHIBITORS OF RHO-KINASE
-
Page/Page column 43, (2008/06/13)
The invention relates to 6-piperidinyl-substituted isoquinoline 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.
PIPERIDINYL-SUBSTITUTED ISOQUINOLONE DERIVATIVES AS RHO-KINASE INHIBITORS
-
Page/Page column 35-36, (2008/06/13)
The invention relates to 6-piperidinyl-substituted isoquinolone derivatives of the formula (I) or isoquinoline derivatives of the formula (I′) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated pho
CYCLOHEXYLAMIN ISOQUINOLONE DERIVATIVES AS RHO-KINASE INHIBITORS
-
Page/Page column 34, (2010/11/25)
The invention relates to 6-cyclohexylamine-substituted isoquinolone derivatives of the formula (I) or isoquinoline 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.
Synthesis and SAR exploration of dinapsoline analogues
Sit, Sing-Yuen,Xie, Kai,Jacutin-Porte, Swanee,Boy, Kenneth M.,Seanz, James,Taber, Matthew T.,Gulwadi, Amit G.,Korpinen, Carolyn D.,Burris, Kevin D.,Molski, Thaddeus F.,Ryan, Elaine,Xu, Cen,Verdoorn, Todd,Johnson, Graham,Nichols, David E.,Mailman, Richard B.
, p. 715 - 734 (2007/10/03)
Dinapsoline is a full D1 dopamine receptor agonist that produces robust rotational activity in the unilateral 6-OHDA rat model. This compound is orally active, and shows a low tendency to cause tolerance in rat models. The active enantiomer was determined to have the S-(+) configuration, and the opposite enantiomer is essentially devoid of biological activity. Taken together, dinapsoline has significant metabolic and pharmacological advantages over previous D1 agonists. In an attempt to define the structure-activity relationships (SARs) and to map out the key elements surrounding the unique structure of dinapsoline, core analogues and substitution analogues of the parent tetracyclic condensed ring structure were prepared. Based on a recently developed synthesis of dinapsoline and its enantiomers, both core and substitution analogues on all four rings (A, B′, C and D ring) of dinapsoline were synthesized. It was found that affinity for both D1and D2 receptors was decreased by most substituents on the A, B′, and C rings, whereas D ring substitutions preserved much of the dopamine receptor binding activity.