868561-17-5

Usage

Uses

Used in Pharmaceutical Industry:
7-Bromo-1H-indole, N-BOC protected is used as a key intermediate in the synthesis of various pharmaceuticals for its ability to be incorporated into the molecular structures of drugs, enhancing their properties and effectiveness.
Used in Chemical Industry:
In the chemical industry, 7-Bromo-1H-indole, N-BOC protected is utilized as a reagent or building block in the production of a range of organic compounds, including those with potential applications in material science, agrochemicals, and other specialized fields.
The specific applications and industries may vary based on the innovative uses of 7-Bromo-1H-indole, N-BOC protected in research and development, as it can be tailored for specific reactions and syntheses due to its unique structural features.

InChI:InChI=1/C13H14BrNO2/c1-13(2,3)17-12(16)15-8-7-9-5-4-6-10(14)11(9)15/h4-8H,1-3H3

Upstream product

• 577-19-5 2-nitrophenyl bromide 
• 51417-51-7 7-bromo-1H-indole 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 100874-07-5 7-bromo-2-phenyl-1H-indole 

Relevant academic research and scientific papers

Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7

CDK7 has emerged as an exciting target in oncology due to its roles in two important processes that are misregulated in cancer cells: cell cycle and transcription. This report describes the discovery of SY-5609, a highly potent (sub-nM CDK7 Kd) and selective, orally available inhibitor of CDK7 that entered the clinic in 2020 (ClinicalTrials.gov Identifier: NCT04247126). Structure-based design was leveraged to obtain high selectivity (>4000-times the closest off target) and slow off-rate binding kinetics desirable for potent cellular activity. Finally, incorporation of a phosphine oxide as an atypical hydrogen bond acceptor helped provide the required potency and metabolic stability. The development candidate SY-5609 displays potent inhibition of CDK7 in cells and demonstrates strong efficacy in mouse xenograft models when dosed as low as 2 mg/kg.

Pyridopyrimidinone compound and application thereof

The invention provides a pyridopyrimidinone compound with a structure as shown in a general formula (II) and application thereof. Researches prove that the compound provided by the invention can effectively inhibit KRAS G12C mutation. KRAS mutation accounts for a large proportion in tumors, no approved drug is obtained for treatment at present, and the compound provided by the invention has the potential to become a therapeutic drug for malignant tumors (especially non-small cell lung cancer (NSCLC) and colorectal cancer) carrying KRAS G12C mutation, and has a great application value.

INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7)

The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

Formal Total Synthesis of Diazonamide A by Indole Oxidative Rearrangement

A short formal total synthesis of the marine natural product diazonamide A is described. The route is based on indole oxidative rearrangement, and a number of options were investigated involving migration of tyrosine or oxazole fragments upon oxidation of open chain or macrocyclic precursors. The final route proceeds from 7-bromoindole by sequential palladium-catalysed couplings of an oxazole fragment at C-2, followed by a tyrosine fragment at C-3. With the key 2,3-disubstituted indole readily in hand, formation of a macrocyclic lactam set the stage for the crucial oxidative rearrangement to a 3,3-disubstituted oxindole. Notwithstanding the concomitant formation of the unwanted indoxyl isomer, the synthesis successfully delivered, after deprotection, the key oxindole intermediate, thereby completing a formal total synthesis of diazonamide A.

THERAPEUTIC COMPOUNDS AND USES THEREOF

The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

2-SULFONYLAMINO-4-HETEROARYL BUTYRAMIDE ANTAGONISTS OF CCR10

This invention relates to a compound of formula (I) and the pharmaceutically acceptable salts thereof wherein R1, R2, R4. Ar and Het are as defined herein. The invention also relates to methods of using the compound of for