147497-32-3

Usage

Uses

Used in Pharmaceutical Industry:
6-BROMO-3,4-DIHYDRO-2H-ISOQUINOLIN-1-ONE is used as an intermediate in the synthesis of benzolactams, which are known as dopamine D3 receptor ligands. These ligands are essential for developing drugs that can modulate the activity of the dopamine D3 receptor, potentially leading to treatments for various neurological and psychiatric disorders.
6-BROMO-3,4-DIHYDRO-2H-ISOQUINOLIN-1-ONE is also used as an intermediate in the synthesis of new, selective 3-aminopyrazole-based MK2 inhibitors. These inhibitors have been proven to inhibit intracellular phosphorylation of hsp27 as well as LPS-induced TNFα release in cells. MK2 inhibitors hold promise in the development of therapeutic agents for inflammatory diseases and other conditions where the MK2 pathway is implicated.

InChI:InChI=1/C9H8BrNO/c10-7-1-2-8-6(5-7)3-4-11-9(8)12/h1-2,5H,3-4H2,(H,11,12)

Upstream product

• 7732-18-5 water 
• 1279816-33-9 methyl 3-bromophenethylcarbamate 
• 305447-65-8 methyl 4-(bromophen)ethylcarbamate 
• 58971-11-2 2-(3-bromophenyl)ethanamine 
• 75-75-2 methanesulfonic acid 
• 34598-49-7 5-Bromo-1-indanone 

Downstream Products

• 959755-58-9 (4-morpholin-4-yl-phenyl)-[5-(1-oxo-1,2,3,4-tetrahydro-isoquinolin-6-yl)-[1,2,4]triazolo[1,5-a]pyrazin-8-yl]-carbamic acid tert-butyl ester 
• 735351-82-3 2-benzyl-6-bromo-3,4-dihydroisoquinolin-1(2H)-one 
• 879887-26-0 6-formyl-1-oxo-1,2,3,4-tetrahydroisoquinoline 
• 226942-29-6 6-bromo-1,2,3,4-tetrahydroisoquinoline 
• 877868-87-6 6-iodo-3,4-dihydroisoquinolin-1(2H)-one 
• 1131223-07-8 6-bromo-3,4-dihydro-2-(2-(tetrahydro-2H-pyran-2-yloxy)ethyl)iso-quinolin-1-one 
• 376584-30-4 6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,4-dihydroisoquinolin-1(2H)-one 
• 1178884-85-9 6-bromo-2-(4-methoxy-benzyl)-3,4-dihydro-2H-isoquinolin-1-one 
• 879887-28-2 6-bromo-2-ethyl-3,4-dihydroisoquinolin-1(2H)-one 
• 1092550-63-4 C₁₈H₁₄FNO 
• 1092550-59-8 C₁₇H₁₂FNO 
• 1092550-65-6 C₁₇H₁₂ClNO 
• 215798-19-9 6-bromo-1,2,3,4-tetrahydroisoquinoline hydrochloride 
• 1567837-24-4 2,4-difluoro-N-(5-(5-(1-oxo-1,2,3,4-tetrahydroisoquinolin-6-yl)thiophen-2-yl)pyridin-3-yl)benzensulphonamide 

Relevant academic research and scientific papers

New Series of Potent Allosteric Inhibitors of Deoxyhypusine Synthase

Deoxyhypusine synthase (DHPS) is the primary enzyme responsible for the hypusine modification and, thereby, activation of the eukaryotic translation initiation factor 5A (eIF5A), which is key in regulating the protein translation processes associated with tumor proliferation. Although DHPS inhibitors could be a promising therapeutic option for treating cancer, only a few studies reported druglike compounds with this inhibition property. Thus, in this work, we designed and synthesized a new chemical series possessing fused ring scaffolds designed from high-throughput screening hit compounds, discovering a 5,6-dihydrothieno[2,3-c]pyridine derivative (26d) with potent inhibitory activity; furthermore, the X-ray crystallographic analysis of the DHPS complex with 26d demonstrated a distinct allosteric binding mode compared to a previously reported inhibitor. These findings could be significantly useful in the functional analysis of conformational changes in DHPS as well as the structure-based design of allosteric inhibitors.

COMPOUNDS FOR THE DEGRADATION OF STK4 AND TREATMENT OF HEMATOLOGIC MALIGNANCIES

The application relates to a compound of Formula (I) which modulate the amount of STK4, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease or disorder associated with the modulation of STK4.

Rational Design of Cell-Active Inhibitors of PARP10

Poly-ADP-ribose polymerases (PARPs 1-16) have emerged as major regulators of diverse cellular processes. PARPs can be subclassified based on their ability to catalyze poly-ADP-ribosylation (PARylation) or mono-ADP-ribosylation (MARylation). While much is

BENZAZEPINE DERIVATIVES

The present invention provides novel benzazepine compounds of Formula (1), or salts thereof, having vasopressin V1a and V2 antagonisms, and medical uses thereof. In the formula, R1 is optionally substituted C1-6 alkyl, etc.; L is -C(=O)-NH-, etc.; Ring A1 is a hydrocarbon ring, etc.; Ring A2 is a hydrocarbon ring, etc.; and each of Rings A1 and A2 may have at least one substituent.

Intramolecular Reductive Cyclization of o-Nitroarenes via Biradical Recombination

A visible-light-induced/thiourea-mediated intramolecular cyclization of o-nitroarenes under mild conditions is realized for the first time, which provides an efficient and environmentally friendly way to access pharmaceutical relevant quinazolinone derivatives. The reaction can be easily extended to gram level by using a continuous-flow setup with high efficiency. Mechanistic investigation including control experiments, transient fluorescence, UV-vis spectra, and DFT calculations suggests that the formation of active biradical intermediates via intramolecular single electron transfer (SET) is key stage in the catalytic cycle.

Metal-Free Synthesis of Polycyclic Quinazolinones Enabled by a (NH4)2S2O8-Promoted Intramolecular Oxidative Cyclization

An efficient metal-free, (NH4)2S2O8 mediated intramolecular oxidative cyclization for the construction of polycyclic heterocycles was disclosed. A series of polycyclic quinazolinone derivatives with good functional group tolerance were obtained in high yields. The natural products tryptanthrin and rutaecarpine, as well as their derivatives, were easily synthesized by this strategy. A preliminary mechanism study suggested the carbon-centered radical was involved in the catalytic cycle.

Light-Driven Intramolecular C?N Cross-Coupling via a Long-Lived Photoactive Photoisomer Complex

Reported herein is a visible-light-driven intramolecular C?N cross-coupling reaction under mild reaction conditions (metal- and photocatalyst-free, at room temperature) via a long-lived photoactive photoisomer complex. This strategy was used to rapidly prepare the N-substituted polycyclic quinazolinone derivatives with a broad substrate scope (>50 examples) and further exploited to synthesize the natural products tryptanthrin, rutaecarpine, and their analogues. The success of gram-scale synthesis and solar-driven transformation, as well as promising tumor-suppressing biological activity, proves the potential of this strategy for practical applications. Mechanistic investigations, including control experiments, DFT calculations, UV-vis spectroscopy, EPR, and X-ray single-crystal structure of the key intermediate, provides insight into the mechanism.

Histone histone deacetylase inhibitor and application thereof

The invention provides a histone histone deacetylase inhibitor and application thereof. Specifically, the invention provides a compound of formula (I) as shown in the specification, and a pharmaceutically acceptable salt of the compound, and in the formula, the groups are defined as shown in the specification. The invention further provides a preparation method of the compound. The compound of formula (I), which is provided by the invention, can be adopted to treat a series of diseases mediated by histone histone deacetylases by inhibiting histone histone deacetylases (HDACs), particularly type-I histone histone deacetylases (subtypes such as HDAC1 and HDAC3), particularly including tumor diseases such as solid tumor and leukemia, neurodegenerative diseases, and the like.

ISOQUINOLIN AND NAPHTHYDRIN COMPOUNDS

The present invention provides a compound of Formula I I wherein X is selected from the group consisting of CH and N; Q is selected from the group consisting of CH3 and H; R is selected from the group consisting of and; or a pharmaceutically acceptable salt thereof, compositions, methods to treat liver disease and NASH.

Heterocyclic Compounds and Methods of Use

This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.