1320211-47-9

Basic information

• Product Name: 1320211-47-9
• Synonyms: Pyrimido[1,2-a]benzimidazole, 2-bromo-
• CAS NO: 1320211-47-9
• Molecular Formula: C₁₀H₆BrN₃
• Molecular Weight: 248.07874
• EINECS: -0
• Mol File: 1320211-47-9.mol
• Article Data: 6

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 1320211-47-9(CAS DataBase Reference)
• NIST Chemistry Reference: 1320211-47-9(1320211-47-9)
• EPA Substance Registry System: 1320211-47-9(1320211-47-9)

Safety Data

• Hazardous Substances Data: 1320211-47-9(Hazardous Substances Data)

Usage

Chemical Identifier

1320211-47-9

Classification

Janus Kinase (JAK) inhibitor

Medicinal Uses

Treatment of rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis

Mechanism of Action

Blocks certain enzymes involved in inflammation process, reducing signs and symptoms of the conditions

Administration

Oral, available in various forms

Treatment Approach

Often used in combination with other medications

Clinical Trials

Shown promising results and considered an important option for patients with chronic inflammatory diseases.

Upstream product

• 1320212-46-1 2-(trichloromethyl)benzo[4,5]imidazol[1,2-a]pyrimidine 
• 24811-78-7 2-hydroxybenzo[4,5]imidazol[1,2-a]pyrimidine 
• 934-32-7 1H-benzimidazol-2-amine 

Downstream Products

• 118664-05-4 benzo[4,5]imidazo[1,2-a]pyrimidin-2-ylamine 

Relevant articles and documents

Concise and high-yield synthesis of T808 and T808P for radiosynthesis of [18F]-T808, a PET tau tracer for Alzheimer's disease

The authentic standard T808 and its corresponding mesylate precursor T808P were synthesized in six steps using ethyl vinyl ether and trichlorocetyl chloride as starting materials. The overall chemical yields of T808 and T808P were 35% and 52%, respectively. [18F]-T808 was synthesized from T808P by the nucleophilic substitution with K[18F]F/Kryptofix 2.2.2 and isolated by HPLC combined with solid-phase extraction (SPE) purification in 35-45% radiochemical yield with 37-370 GBq/μmol specific activity at end of bombardment (EOB).

Practical Synthesis of a Stable Precursor for Positron Emission Tomography Imaging Agent 18F-GTP1

18F-GTP1 is a deuterated small molecule positron emission tomography (PET) imaging agent used to visualize tau tangles in Alzheimer's disease patients. The first-generation synthesis of 18F-GTP1's nonradiolabeled alkyl tosylate precursor was plagued by low-yielding steps, inefficient chromatographic purifications, and variable product quality. Due to these limitations, a more robust second-generation route was developed and successfully executed on kilogram scale. A reduction with LiAlD4 incorporated geminal deuterium atoms, while an efficient amidation reaction accessed the key acrylamide coupling partner. Moreover, the tricyclic imidazo[1,2-a]pyrimidine core was assembled via a novel, convergent, and highly selective phosphoramidate-directed annulation. The improved synthesis eliminated all chromatography en route to a high-yielding and reproducible acid-promoted tosylation as the final step.

For detecting imaging agent of neurological disorders

Imaging agents of formulas (I)-(V) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formulas (I)-(V) capable of binding to tau proteins and β-amyloid peptides are presented herein. The invention also relates to methods of imaging Aβ and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formulas (I)-(V) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.