226085-17-2

Usage

Uses

Used in Pharmaceutical Industry:
TERT-BUTYL 3-BROMO-1H-PYRROLO[2,3-B]PYRIDINE-1-CARBOXYLATE is used as a building block for the synthesis of various biologically active molecules, contributing to the development of new pharmaceuticals and medicinal chemistry research. Its unique structure allows for the creation of compounds with potential therapeutic applications.
Used in Drug Development:
In the drug development process, TERT-BUTYL 3-BROMO-1H-PYRROLO[2,3-B]PYRIDINE-1-CARBOXYLATE serves as a drug candidate for the treatment of certain diseases. Its potential efficacy and unique properties make it a promising option for further research and development into new therapeutic agents.
Used in Medicinal Chemistry Research:
TERT-BUTYL 3-BROMO-1H-PYRROLO[2,3-B]PYRIDINE-1-CARBOXYLATE is utilized in medicinal chemistry research to explore its properties and interactions with biological targets. This research aids in understanding its potential as a therapeutic agent and contributes to the advancement of pharmaceutical science.

Upstream product

• 138343-77-8 1-(tert-butoxycarbonyl)-1H-pyrrolo<2,3-b>pyridine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 74420-15-8 3-bromo-1H-pyrrolo[2,3-b]pyridine 

Downstream Products

• 866545-87-1 3-(3,4-dimethoxy-phenyl)-1H-pyrrolo[2,3-b]pyridine 
• 942070-47-5 2-methyl-2-propanyl 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrrolo[2,3-b]pyridine-1-carboxylate 

Relevant academic research and scientific papers

INDOLE COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS

Provided herein are compounds of formula (V) that bind to BF3 of an androgen receptor (AR), which can modulate the AR for the treatment of Kennedy's disease.

Discovery of novel and orally bioavailable CDK 4/6 inhibitors with high kinome selectivity, low toxicity and long-acting stability for the treatment of multiple myeloma

Multiple myeloma (MM) ranks second in malignant hematopoietic cancers, and the most common anti-MM drugs easily generate resistance. CDK4/6 have been validated to play determinant roles in MM, but no remarkable progress has been obtained from clinical trials of CDK4/6 inhibitors for MM. To discover novel CDK6 inhibitors with better potency and high druggability, structure-based virtual screening was conducted to identify compound 10. Further chemical optimization afforded a better derivative, compound 32, which exhibited strong inhibition of CDK4/6 and showed high selectivity over 360+ kinases, including homologous CDKs. The in vivo evaluation demonstrated that compound 32 possessed low toxicity (LD50 > 10,000 mg/kg), favorable bioavailability (F% = 51%), high metabolic stability (t1/2 > 24 h) and strong anti-MM potency. In summary, we discovered a novel CDK4/6 inhibitor bearing favorable drug-like properties and offered a great candidate for MM preclinical studies.

Five-membered heterocyclic oxo carboxylic acid compound and medical application thereof

The invention relates to a five-membered heterocyclic oxo carboxylic acid compound and a medical application thereof. Specifically, the invention relates to a compound, a pharmaceutical salt, a prodrug, a hydrate, a solvate or a crystal form as shown in a formula (I), and also relates to a preparation method of the compound, a pharmaceutical composition containing the compound and an application of the pharmaceutical composition as a secretion regulator of interferon type I, especially as an STING agonist in preparation of medicines for preventing and/or treating I-type interferon related diseases.

Azaindole pyrimidinamine heterocyclic compound as well as preparation method and application thereof

The invention discloses an azaindole pyrimidinamine heterocyclic compound as well as a preparation method and application thereof. The compound is shown as a formula (S). The compound provided by the invention can inhibit malignant proliferation of cancers, has good treatment effect, low toxicity and good drug metabolism characteristics, is not easy to generate drug resistance, and can be used for preparing drugs for treating cancers or tumor-related diseases. The cancers or tumor-related diseases include multiple myeloma, leukemia, breast cancer, prostate cancer, lung cancer, liver cancer, gastric cancer, bone cancer, brain cancer, head and neck cancer, intestinal cancer, pancreatic cancer, bladder cancer, testicular cancer, ovarian cancer and endometrial cancer.

TYK2 INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

Synthesis of Differentially Protected Azatryptophan Analogs via Pd2(dba)3/XPhos Catalyzed Negishi Coupling of N-Ts Azaindole Halides with Zinc Derivative from Fmoc-Protected tert-Butyl (R)-2-Amino-3-iodopropanoate

Unnatural amino acids play an important role in peptide based drug discovery. Herein, we report a class of differentially protected azatryptophan derivatives synthesized from N-tosyl-3-haloazaindoles 1 and Fmoc-protected tert-butyl iodoalanine 2 via a Neg

Selective Halogenation Using an Aniline Catalyst

Electrophilic halogenation is used to produce a wide variety of halogenated compounds. Previously reported methods have been developed mainly using a reagent-based approach. Unfortunately, a suitable "catalytic" process for halogen transfer reactions has yet to be achieved. In this study, arylamines have been found to generate an N-halo arylamine intermediate, which acts as a highly reactive but selective catalytic electrophilic halogen source. A wide variety of heteroaromatic and aromatic compounds are halogenated using commercially available N-halosuccinimides, for example, NCS, NBS, and NIS, with good to excellent yields and with very high selectivity. In the case of unactivated double bonds, allylic chlorides are obtained under chlorination conditions, whereas bromocyclization occurs for polyolefin. The reactivity of the catalyst can be tuned by varying the electronic properties of the arene moiety of catalyst.

ANTIBACTERIAL CONDENSED THIAZOLES

Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk - is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (-0-), thioether (-S-) or amino (-NR)- link, wherein R is hydrogen, -CN or C1-C3 alky!; X is -C(=O)NR6-, or -C(=O)O- wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is -N= or -CH= Z2 is -N= or -C(R1)=; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2JaIkOXy or (C1-C2)alkylthio, nitro, or nitrile (-CN); R2 is a group Q1 -[Alk1]q-Q2 -, wherein q is 0 or 1; AIkl is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (-O-), thioether (-S-) or amino (-NR)- link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 5 or 6 ring atoms or an optionally substituted divalent bicyclic carbocyclic or heterocyclic radical having 9 or 10 ring atoms; Q1 is hydrogen, an optional substituent or an optionally substituted carbocyclic or heterocyclic radical having 3-7 ring atoms

PDE4B inhibitors

Compounds are described that are active on PDE4. Also described are crystal structures of PDE4B determined using X-ray crystallography, the use of PDE4B crystals and strucural information for identifying molecular scaffolds, for developing ligands that bind to and modulate PDE4B, and for identifying improved ligands based on known ligands.

Synthesis of 3-aryl- and 3-heteroaryl-7-azaindoles

The synthesis of 1-protected 3-trimethylstannyl-7-azaindoles and their coupling with aryl and heteroaryl halides is described.