227939-01-7

Usage

Uses

Used in Organic Synthesis:
(5-BROMOPYRIDIN-2-YL)METHYL-CARBAMIC ACID TERT-BUTYL ESTER is used as a protective group for amines, facilitating various chemical reactions by shielding the amine functionality from unwanted side reactions.
Used in Pharmaceutical Industry:
(5-BROMOPYRIDIN-2-YL)METHYL-CARBAMIC ACID TERT-BUTYL ESTER is used as a building block for the synthesis of biologically active compounds, leveraging its reactivity and stability to contribute to the development of new pharmaceutical agents.
Used in Chemical Reactions:
(5-BROMOPYRIDIN-2-YL)METHYL-CARBAMIC ACID TERT-BUTYL ESTER is used in nucleophilic substitution and palladium-catalyzed coupling reactions, taking advantage of the bromine atom for efficient synthetic transformations.
Used in Research and Development:
(5-BROMOPYRIDIN-2-YL)METHYL-CARBAMIC ACID TERT-BUTYL ESTER is utilized in the exploration of new synthetic pathways and methodologies, providing a stable and reactive platform for the advancement of organic chemistry.

InChI:InChI=1/C11H15BrN2O2/c1-11(2,3)16-10(15)14(4)9-6-5-8(12)7-13-9/h5-7H,1-4H3

Upstream product

• 624-28-2 2,5-dibromopyridine 
• 84539-30-0 5-bromo-N-methylpyridin-2-amine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1072-97-5 5-bromo-2-pyridylamine 
• 74-88-4 methyl iodide 
• 159451-66-8 tert-butyl N-(5-bromopyridin-2-yl)carbamate 

Downstream Products

• 1032758-87-4 methyl-[5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-pyridin-2-yl]-carbamic acid tert-butyl ester 
• 1235449-52-1 N-hydroxy-2-(methyl((2-(6-(methylamino)pyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)amino)pyrimidine-5-carboxamide 

Relevant academic research and scientific papers

Diaromatic vinyl derivative as well as preparation method and application thereof

The structural formula of the diaromatic vinyl derivative is shown I. In-flight R1 Document CH3 (Methyl) or CD3 (Deuterated methyl). R2 A group selected from C1 - 8 saturated alkoxy or alkylamino, substituted C2

Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS

Abdominal pain and abnormal bowel habits represent major symptoms for irritable bowel syndrome (IBS) patients that are not adequately managed. Although the etiology of IBS is not completely understood, many of the functions of the gastrointestinal (GI) tract are regulated by the enteric nervous system (ENS). Inflammation or stress-induced expression of growth factors or cytokines may lead to hyperinnervation of visceral afferent neurons in GI tract and contribute to the pathophysiology of IBS. Rearranged during transfection (RET) is a neuronal growth factor receptor tyrosine kinase critical for the development of the ENS as exemplified by Hirschsprung patients who carry RET loss-of-function mutations and lack normal colonic innervation leading to colonic obstruction. Similarly, RET signaling in the adult ENS maintains neuronal function by contributing to synaptic formation, signal transmission, and neuronal plasticity. Inhibition of RET in the ENS represents a novel therapeutic strategy for the normalization of neuronal function and the symptoms of IBS patients. Herein, we describe our screening effort and subsequent structure-activity relationships (SARs) in optimizing potency, selectivity, and mutagenicity of the series, which led to the discovery of a first-in-class, gut-restricted RET kinase inhibitor, 2-(4-(4-ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)acetamide (15, GSK3179106), as a clinical candidate for the treatment of IBS. GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET kinase inhibitor with a RET IC50 of 0.3 nM and is efficacious in vivo.

SELECTIVE INHIBITORS OF CLINICALLY IMPORTANT MUTANTS OF THE EGFR TYROSINE KINASE

The present invention provides compounds of Formula (I) or a subgeneric structure or species thereof, or a pharmaceutically acceptable salt, ester, solvate, and/or prodrug thereof, and methods and compositions for treating or ameliorating abnormal cell proliferative disorders, such as cancer, wherein A, R2, R3, R10, E1, E2, E3, Y, and Z are as defined herein.

Thiophene pyrimidines and preparation and its preparation method and application

The invention discloses a pyrantel compound and preparation, as well as a preparation method and application of the pyrantel compound and preparation, belonging to the technical field of chemical medicines and preparations thereof. According to the pyrantel compound or pharmaceutically acceptable salt thereof, HDAC (histone deacetylase)/PI3K (phosphatidylinositide 3-kinase) double-target inhibitor is used for selectively inhibiting tumor cell messenger core protein kinase target PI3K and epigenetic target HDAC which are synergized, and is capable of destroying the network of tumor cell messengers, thus exerting a great killing effect on various tumor cells. In multiple blood and entity heterogenic transplanted tumor animal models, the inhibitor can be used for intensively effectively inhibiting tumor growth and especially has a remarkable effect on various blood B-cell malignant tumors, and safety evaluation tests indicate that the inhibitor has high safety and security. The pyrantel compound and preparation can be used for effectively treating patients with later reoccurrence of lymphoma, myeloma and lymphatic leukemia or drug resistance.

THIAZOLOPYRIMIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE

Compounds of Formulas (Ia and Ib), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed

NOVEL HETEROARYL SUBSTITUTED BENZOTHIAZOLES

The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: [Chemical formula should be inserted here. Please see paper copy

Synthesis of [N-methyl- 11C]-3-[(6-dimethylamino)pyridin-3-yl]-2,5-dimethyl-N, N-dipropylpyrazolo[1,5-a]pyrimidine-7-amine: A potential PET ligand for in vivo imaging of CRF1 receptors

A convenient synthesis of [N-methyl- 11C]-3-[(6-dimethylamino)pyridin-3-yl]-2,5-dimethyl-N, N-dipropylpyrazolo[1,5-a]pyrimidine-7-amine (R121920), a highly selective CRF1 antagonist has been developed as a potential PET ligand. 3-[(6-methylamino)pyridin-3-yl]-2,5-dimethyl-N,N-dipropylpyrazolo [1,5-a]pyrimidine-7-amine (7), the precursor for radiolabelling was synthesized through a novel palladium catalyzed Suzuki coupling of aryl bromide 5 with heteroaryl boronate ester 4. The requisite boronate ester 4 was synthesized in four steps from 2-amino-4-bromopyridine in 50% overall yield. Although the synthesis of cold R121920 proceeded in 93% yield by sodium hexamethyl-disilazide (NaHMDS) mediated N-methylation of the desmethylamine 7 at -78°C, the attempted radiosynthesis under various conditions using conventional bases were not successful. However, the radiolabeling of [ 11C]R121920 was successfully carried out with [11C]MeOTf in acetone at -20°C in the absence of added basic reagents. The radiotracer was purified by RP-HPLC followed by RP-solid phase extraction. The yield of the reaction was 5% (at EOB) and the specific activity was > 1000 Ci/mmol (at EOB) with a radiochemical purity > 99%. Copyright