1246453-63-3

Upstream product

• 2401-24-3 2-chloro-5-methoxyaniline 
• 1246453-61-1 (2-benzyloxy-ethyl)-(2-chloro-5-methoxyphenyl)amine 
• 30132-23-1 ethyl 3-bromo-2-oxocyclohexanecarboxylate 
• 85006-21-9 2-chloro-5-methoxyaniline hydrochloride 
• 1274863-78-3 2-benzyloxy-N-(2-chloro-5-methoxy-phenyl)acetamide 
• 19810-31-2 Benzyloxyacetyl chloride 
• 30379-55-6 benzyloxyacetic acid 
• 1246453-62-2 3-[(2-Benzyloxy-ethyl)-(2-chloro-5-methoxy-phenyl)-amino]-2-hydroxy-cyclohex-1-ene carboxylic acid ethyl ester 

Downstream Products

• 1246453-64-4 9-(2-benzyloxy-ethyl)-8-chloro-5-methoxy-2,3,4,9,-tetrahydro-1H-carbazole-4-carboxylic acid 
• 1246453-65-5 9-(2-benzyloxy-ethyl)-8-chloro-5-methoxy-2,3,4,9,-tetrahydro-1H-carbazole-4-carbonyl chloride 
• 1246453-66-6 9-(2-(benzyloxy)ethyl)-8-chloro-5-methoxy-2,3,4,9-tetrahydro-1H-carbazole-4-carboxylic acid diethylamide 
• 1246453-67-7 9-(2-(benzyloxy)ethyl)-5-methoxy-2,3,4,9-tetrahydro-1H-carbazole-4-carboxylic acid diethylamide 

Relevant academic research and scientific papers

Radiosynthesis of (R,S)-[18F]GE387: A Potential PET Radiotracer for Imaging Translocator Protein 18 kDa (TSPO) with Low Binding Sensitivity to the Human Gene Polymorphism rs6971

Translocator protein (TSPO) is a biomarker of neuroinflammation, which is a hallmark of many neurodegenerative diseases and has been exploited as a positron emission tomography (PET) target. Carbon-11-labelled PK11195 remains the most applied agent for imaging TSPO, despite its short-lived isotope and low brain permeability. Second-generation radiotracers show variance in affinity amongst subjects (low-, mixed-, and high-affinity binders) caused by the genetic polymorphism (rs6971) of the TSPO gene. To overcome these limitations, a new structural scaffold was explored based on the TSPO pharmacophore, and the analogue with a low-affinity binder/high-affinity binder (LAB/HAB) ratio similar (1.2 vs. 1.3) to that of (R)-[11C]PK11195 was investigated. The synthesis of the reference compound was accomplished in six steps and 9 % overall yield, and the precursor was prepared in eight steps and 8 % overall yield. The chiral separation of the reference and precursor compounds was performed using supercritical fluid chromatography with >95 % ee. The absolute configuration was determined by circular dichroism. Optimisation of reaction conditions for manual radiolabelling revealed acetonitrile as a preferred solvent at 100 °C. Automation of this radiolabelling method provided R and S enantiomers in respective 21.3±16.7 and 25.6±7.1 % decay-corrected yields and molar activities of 55.8±35.6 and 63.5±39.5 GBq μmol?1 (n=3). Injection of the racemic analogue into a healthy rat confirmed passage through the blood–brain barrier.

In vivo imaging method for cancer

The present invention provides a method useful in the diagnosis and monitoring of cancer wherein there is an abnormal expression of PBR. The method of the invention is particularly useful in evaluating the severity of the cancer, e.g. PBR expression corre

In vivo imaging method of mood disorders

The present invention provides a method useful in the diagnosis and/or monitoring of mood disorders wherein there is an abnormal expression of PBR. The method of the invention is useful in the differential diagnosis of said mood disorders and other condit

ENANTIOMERIC SEPARATION AND PURIFICATION OF 2,3,4,9-TETRAHYDRO-1H-CARBAZOLE-4-CARBOXYLIC ACID AMIDE DERIVATIVES

The present invention provides a method for the purification of cyclic indole compounds that provides advantages over previously-known methods. Using the method of the present invention allows for the facile preparation of a good quality solid form of the

MACROPHAGE IMAGING

The present invention concerns in vivo imaging and in particular in vivo imaging of activated macrophages. An indole-based in vivo imaging agent labelled with 18F is provided that binds with high affinity to translocator protein (TSPO). Other a

ZINC HALIDE MEDIATED CYCLIZATION PROCESS LEADING TO TRICYCLIC INDOLES

The present invention relates to a method for the production of tricyclic indole compounds comprising a cyclization step wherein this step is improved over known methods.

An improved, regioselective synthesis of the radiolabelling precursor for the translocator protein targeting positron emission tomography imaging radiotracer [18F]GE-180

[18F]GE-180 has been demonstrated to be a promising new positron emission tomography radiotracer for targeting translocator protein. PET imaging of TSPO will enable measurement of neuroinflammation and microglia activity in vivo. The synthetic route used in the initial discovery of GE-180, whilst enabling the rapid evaluation of the structure-activity relationships (SAR) in this molecular class, was not high yielding and not suitable for scale-up. Here we present an optimised route towards GE-180 and the radiolabelling precursor of [18F]GE-180 with significantly improved yields due to a strategy which improves the regioselectivity of the key indole formation step of the synthesis.

IN VIVO IMAGING METHOD OF MOOD DISORDERS

The present invention provides a method useful in the diagnosis and/or monitoring of mood disorders wherein there is an abnormal expression of PBR. The method of the invention is useful in the differential diagnosis of said mood disorders and other condit

ACTIVE ENANTIOMER

The present invention provides a PET tracer that has improved properties for imaging the peripheral benzodiazepine receptor (PBR) as compared with known such PET tracers. The present invention also provides a precursor compound useful in the preparation o