Tag: 200-300

Synthesis of cortistatins A, J, K and L was written by Flyer, Alec N.;Si, Chong;Myers, Andrew G.. And the article was included in Nature Chemistry in 2010.Product Details of 75476-83-4 The following contents are mentioned in the article:

The cortistatins are a recently identified class of marine natural products characterized by an unusual steroidal skeleton, which have been found to inhibit differentially the proliferation of various mammalian cells in culture by an unknown mechanism. We describe a comprehensive route for the synthesis of cortistatins from a common precursor, azide I, which in turn is assembled from two fragments of similar structural complexity. Cortistatins A and J, and for the first time K and L, have been synthesized in parallel processes from like intermediates prepared from a single compound With the identification of facile laboratory transformations linking intermediates in the cortistatin L synthetic series with corresponding intermediates to cortistatins A and J, we have been led to speculate that somewhat related paths might occur in nature, offering potential sequencing and chem. detail for cortistatin biosynthetic pathways. The antiproliferative activity of the cortistatins was tested against HUVECs. This study involved multiple reactions and reactants, such as 7-Iodoisoquinoline (cas: 75476-83-4Product Details of 75476-83-4).

7-Iodoisoquinoline (cas: 75476-83-4) belongs to isoquinoline derivatives. Quinoline and isoquinoline skeletons are among the most attractive frameworks with a wide range of biological and pharmacological activities. Other industrial applications include their use as corrosion inhibitors, preservatives, and as solvents for resins and terpenes.Product Details of 75476-83-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

The Dimeric Form of 1,3-Diaminoisoquinoline Derivative Rescued the Mis-splicing of Atp2a1 and Clcn1 Genes in Myotonic Dystrophy Type 1 Mouse Model was written by Matsumoto, Jun;Nakamori, Masayuki;Okamoto, Tatsumasa;Murata, Asako;Dohno, Chikara;Nakatani, Kazuhiko. And the article was included in Chemistry – A European Journal in 2020.Reference of 1215767-89-7 The following contents are mentioned in the article:

Expanded CUG repeat RNA in the dystrophia myotonia protein kinase (DMPK) gene causes myotonic dystrophy type 1 (DM1) and sequesters RNA processing proteins, such as the splicing factor muscleblind-like 1 protein (MBNL1). Sequestration of splicing factors results in the mis-splicing of some pre-mRNAs. Small mols. that rescue the mis-splicing in the DM1 cells have drawn attention as potential drugs to treat DM1. Herein we report a new mol. JM642 consisted of two 1,3-diaminoisoquinoline chromophores having an auxiliary aromatic unit at the C5 position. JM642 alternates the splicing pattern of the pre-mRNA of the Ldb3 gene in the DM1 cell model and Clcn1 and Atp2a1 genes in the DM1 mouse model. In vitro binding anal. by surface plasmon resonance (SPR) assay to the r(CUG) repeat and disruption of ribonuclear foci in the DM1 cell model suggested the binding of JM642 to the expanded r(CUG) repeat in vivo, eventually rescue the mis-splicing. This study involved multiple reactions and reactants, such as 5-Bromo-1,3-dichloroisoquinoline (cas: 1215767-89-7Reference of 1215767-89-7).

5-Bromo-1,3-dichloroisoquinoline (cas: 1215767-89-7) belongs to isoquinoline derivatives. Although isoquinoline derivatives can be synthesized by several methods, relatively few direct methods deliver the unsubstituted isoquinoline. Other industrial applications include their use as corrosion inhibitors, preservatives, and as solvents for resins and terpenes.Reference of 1215767-89-7

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Synthesis of isoquinolines from indenes was written by Miller, R. Bryan;Frincke, James M.. And the article was included in Journal of Organic Chemistry in 1980.Reference of 75476-83-4 The following contents are mentioned in the article:

A general procedure for the preparation of Me, di-Me, NO₂, Br, iodo, and di-MeO-substituted isoquinolines from the appropriately substituted indenes is described. Ozonolysis of the indenes followed by reductive workup gives intermediate homophthalaldehydes, which are treated with NH₄OH to give the isoquinolines. This “one-pot”, three-step reaction sequence was applied to the formation of all of the mono-C-methyl-substituted isoquinolines in a regiospecific manner. The procedure is applicable to both electron-withdrawing and electron-donating substituents on the indene system. In this manner the 6- and 7-nitro-, -bromo-, and -iodoisoquinolines were prepared This study involved multiple reactions and reactants, such as 7-Iodoisoquinoline (cas: 75476-83-4Reference of 75476-83-4).

7-Iodoisoquinoline (cas: 75476-83-4) belongs to isoquinoline derivatives. Quinoline is a catabolite of tryptophan, the basic structure of some antihypertensive drugs, such as the peripheral vasodilators prazosin and doxazosin. The Pomeranz–Fritsch reaction provides a method for the preparation of isoquinoline. This reaction uses a benzaldehyde and aminoacetoaldehyde diethyl acetal, which in an acid medium react to form isoquinoline.Reference of 75476-83-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Regioselective Bromination of Fused Heterocyclic N-Oxides was written by Wengryniuk, Sarah E.;Weickgenannt, Andreas;Reiher, Christopher;Strotman, Neil A.;Chen, Ke;Eastgate, Martin D.;Baran, Phil S.. And the article was included in Organic Letters in 2013.SDS of cas: 1421517-86-3 The following contents are mentioned in the article:

A mild method for the regioselective C2-bromination of fused azine N-oxides is presented, employing tosic anhydride as the activator and tetra-n-butylammonium bromide as the nucleophilic bromide source. The C2-brominated compounds, e.g. I [X = H, 4-OMe, 6-OMe, etc.], are produced in moderate to excellent yields and with excellent regioselectivity in most cases. The potential extension of this method to other halogens, effecting C2-chlorination with Ts₂O/TBACl is also presented. Finally, this method could be incorporated into a viable one-pot oxidation/bromination process, using methyltrioxorhenium/urea hydropgen peroxide as the oxidant. This study involved multiple reactions and reactants, such as 1-Bromo-4-fluoroisoquinoline (cas: 1421517-86-3SDS of cas: 1421517-86-3).

1-Bromo-4-fluoroisoquinoline (cas: 1421517-86-3) belongs to isoquinoline derivatives. Quinoline and isoquinoline skeletons are among the most attractive frameworks with a wide range of biological and pharmacological activities. Other industrial applications include their use as corrosion inhibitors, preservatives, and as solvents for resins and terpenes.SDS of cas: 1421517-86-3

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Efficient and stereoselective installation of isoquinoline: formal total synthesis of cortistatin A was written by Yamashita, Shuji;Kitajima, Kazuki;Iso, Kentaro;Hirama, Masahiro. And the article was included in Tetrahedron Letters in 2009.Synthetic Route of C9H6IN The following contents are mentioned in the article:

The highly stereoselective attachment of isoquinoline onto the steroidal framework of cortistatin A (I) was achieved. The synthetic strategy featured a Ce-mediated nucleophilic addition of an isoquinoline unit to the sterically congested ketone followed by formation of the Ph thiocarbamate, and subsequent stereoselective radical reduction The new method resulted in a formal total synthesis of cortistatin A. This study involved multiple reactions and reactants, such as 7-Iodoisoquinoline (cas: 75476-83-4Synthetic Route of C9H6IN).

7-Iodoisoquinoline (cas: 75476-83-4) belongs to isoquinoline derivatives. Quinoline and isoquinoline skeletons are among the most attractive frameworks with a wide range of biological and pharmacological activities. Lewis acid activation and nucleophilic attack can produce multiple regioisomers in quinolines and pyridines; isoquinolines generally only undergo attack at the 1-position.Synthetic Route of C9H6IN

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Synthesis and structure of 3-isoquinolinols was written by Simchen, Gerhard;Haefner, Manfred. And the article was included in Justus Liebigs Annalen der Chemie in 1975.Related Products of 55086-31-2 The following contents are mentioned in the article:

The isoquinolinols I (X = Cl, Br, or iodine; R = H, Cl, Br, Me, or OMe; R1 = H, Me, or OMe) were prepared by cyclization of 3,4,6-RR1(NC)C6H2CH2COCl in the presence of anhydrous HX. Hydrogenation of I over Pd/C gave I (X = H). The lactam-lactim tautomerism of these compounds was discussed. This study involved multiple reactions and reactants, such as 1-Chloro-6-methoxyisoquinolin-3(2H)-one (cas: 55086-31-2Related Products of 55086-31-2).

1-Chloro-6-methoxyisoquinolin-3(2H)-one (cas: 55086-31-2) belongs to isoquinoline derivatives. Although isoquinoline derivatives can be synthesized by several methods, relatively few direct methods deliver the unsubstituted isoquinoline. The Pomeranz–Fritsch reaction provides a method for the preparation of isoquinoline. This reaction uses a benzaldehyde and aminoacetoaldehyde diethyl acetal, which in an acid medium react to form isoquinoline.Related Products of 55086-31-2

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Product class 5: isoquinolines was written by Alvarez, M.;Joule, J. A.. And the article was included in Science of Synthesis in 2005.Formula: C9H6IN The following contents are mentioned in the article:

A review primarily covering methods of preparation of isoquinolines via cyclization, ring transformations or substituent modification. Isoquinoline 2-oxides and isoquinolinium salts are also included. This study involved multiple reactions and reactants, such as 7-Iodoisoquinoline (cas: 75476-83-4Formula: C9H6IN).

7-Iodoisoquinoline (cas: 75476-83-4) belongs to isoquinoline derivatives. The isoquinoline structure occurs in a considerable number of alkaloids in widely separated plant families. The Pomeranz–Fritsch reaction provides a method for the preparation of isoquinoline. This reaction uses a benzaldehyde and aminoacetoaldehyde diethyl acetal, which in an acid medium react to form isoquinoline.Formula: C9H6IN

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On March 15, 2004, Grubbs, Russell A.; Lewis, Mechelle M.; Owens-Vance, Connie; Gay, Elaine A.; Jassen, Amy K.; Mailman, Richard B.; Nichols, David E. published an article.HPLC of Formula: 58142-46-4 The title of the article was 8,9-Dihydroxy-1,2,3,11b-tetrahydrochromeno[4,3,2,-de]isoquinoline (dinoxyline), a high affinity and potent agonist at all dopamine receptor isoforms. And the article contained the following:

The synthesis and preliminary pharmacol. evaluation of 8,9-dihydroxy-1,2,3,11b-tetrahydrochromeno[4,3,2,-de]isoquinoline (5, now named dinoxyline) is described. This mol. was designed as a potential bioisostere that would conserve the essential elements of our β-phenyldopamine D1 pharmacophore (i.e., position and orientation of the nitrogen, hydroxyls, and Ph rings). Previously, we have rigidified these elements using alkyl bridges, as exemplified in the dopamine D1 full agonist mols. dihydrexidine (1) and dinapsoline (2). This approach has been modified and we now show that it is possible to tether these elements using an ether linkage. Preliminary pharmacol. has revealed that 5 is a potent full D1 agonist (K0.5 <10 nM; EC50=30 nM), but also has high affinity for brain D2-like and cloned D2 and D3 receptors. Interestingly, whereas 1 and 2 and their analogs have only moderate affinity for the human D4 receptor, 5 also has high affinity for this isoform. Moreover, although N-alkylation of 1 and 2 increases D2 affinity, the N-allyl (15) and N-Pr (17) derivatives of 5 had decreased D2 affinity. Therefore, 5 may be engaging different amino acid residues than do 1 and 2 when they bind to the D2 receptor. This is the first example of a ligand with high affinity at all dopamine receptors, yet with functional characteristics similar to dopamine. These rigid ligands also will be useful tools to determine specific residues of the receptor transmembrane domains that are critical for agonist ligand selectivity for the D4 receptor. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).HPLC of Formula: 58142-46-4

The Article related to dinoxyline analog preparation dopamine receptor agonist, Pharmacology: Structure-Activity and other aspects.HPLC of Formula: 58142-46-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On August 8, 2001, Peglion, Jean-louis; Dessinges, Aimee; Poitevin, Christophe; Vilaine, Jean-paul; Villeneuve, Nicole; Thollon, Catherine; Bourguignon, Marie-pierre published a patent.Formula: C9H5BrN2O2 The title of the patent was Preparation of N-piperidinyl(alkyl)isoquinolinesulfonamides and analogs for treatment of vascular disease. And the patent contained the following:

RSO2NR1Z1ZZ2R2 [I; R = (un)substituted (hetero)aryl; R1 = H or alkyl; R2 = (un)substituted 2- or 3-indenyl or -benzofuranyl; Z = (4-hydroxy)piperidine-4,1-diyl; Z1 = bond or alkylene; Z2 = (un)substituted alk(en)ylene] were prepared Thus, Et 4-piperidinecarboxylate was converted in 5 steps to title compound II. Data for biol. activity of 1 prepared I were given. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Formula: C9H5BrN2O2

The Article related to piperidinylalkylisoquinolinesulfonamide preparation vascular disease treatment, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Formula: C9H5BrN2O2

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On April 9, 2004, D’Orchymont, Hugues; Van Hijfte, Luc; Zimmermann, Andre published a patent.Reference of 4-Bromo-5-nitroisoquinoline The title of the patent was Preparation of indazolecarboxamides as CDK1, CDK2, and CDK4 inhibitors for treating CDK-related diseases, in particular cancer. And the patent contained the following:

Title compounds I [R1 = H, halo, NH2, NHR2, NHCOR2, NO2, CN, CH2NH2, CH2NHR2, (un)substituted Ph, heteroaryl; Ar = (un)substituted Ph, heteroaryl; R2 = Ph, heteroaryl, (un)substituted alkyl (substituent = Ph or heteroaryl); n = 0, 1, 2, or 3; PG = protecting group selected from trimethylsilylethoxymethyl, mesitylenesulfonyl; their free bases, addition salts with acids, solvates and hydrates; with the exclusion of certain compounds] were prepared as cyclin-dependent kinase (CDK)-1, CDK2, and CDK4 inhibitors for treating cdk-related diseases, in particular cancer. For instance, reacting indazole-3-carboxylic acid with N-phenyl-1,4-phenylenediamine in the presence of DCC gave 58% II. I displayed IC50 values < 20 μM for the inhibition of CDK2, CDK1, and CDK4 in a test for measuring the enzymic activity of CDK2/Cyclin A, CDK1/Cyclin B, and CDK4/Cyclin D1, resp. I are useful for treating cancers, autoimmune diseases, inflammations, cardiovascular diseases, viral and fungal infections, hematol. diseases, and degenerative diseases of muscular system. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Reference of 4-Bromo-5-nitroisoquinoline

The Article related to indazolecarboxamide preparation cdk1 cdk2 cdk4 inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Reference of 4-Bromo-5-nitroisoquinoline

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem