40274-29-1

Upstream product

• 80151-28-6 3-(4-fluoro-phenyl)-prop-2-yn-1-ol 
• 352-34-1 4-fluoro-1-iodobenzene 
• 227954-23-6 methanesulfonic acid 3-(4-fluorophenyl)prop-2-ynyl ester 
• 766-98-3 1-ethynyl-4-fluorobenzene 

Downstream Products

• 1174568-59-2 3-(4-fluoro-phenyl)-4H,6H-1,2,5,10b-tetraaza-benzo[e]azulene-5-carboxylic acid tert-butyl ester 
• 1243706-52-6 8-{4-[3-(4-fluorophenyl)prop-2-ynyloxy]phenyl}-1-propyl-1,7-dihydropurin-6-one 
• 1243706-63-9 8-{4-[3-(4-fluoro-phenyl)-prop-2-ynyloxy]-phenyl}-1-propyl-2-(3-trifluoromethyl-phenyl)-1,7-dihydro-purin-6-one 
• 1416161-18-6 C₁₉H₁₉FO₂Si 
• 1448667-81-9 (2S,4R)-1-(2,2-diphenylacetyl)-4-((3-(4-fluorophenyl)prop-2-yn-1-yl)(methyl)amino)piperidine-2-carboxylic acid 
• 1448668-24-3 C₃₁H₃₁FN₂O₃ 
• 1448667-80-8 (2S,4S)-1-(2,2-diphenylacetyl)-4-((3-(4-fluorophenyl)prop-2-yn-1-yl)(methyl)amino)piperidine-2-carboxylic acid 
• 1448668-23-2 C₃₁H₃₁FN₂O₃ 
• 1448679-56-8 C₂₀H₂₅FN₂O₄ 
• 1448678-97-4 (S)-1-(2,2-diphenylacetyl)-4-(3-[4-fluorophenyl]prop-2-yn-1-yl)piperazine-2-carboxylic acid 
• 1448679-57-9 C₂₉H₂₇FN₂O₃ 
• 1442681-21-1 C₁₉H₂₁FN₆O₃ 
• 1442680-64-9 C₃₅H₃₇FN₆O₅ 
• 1286746-18-6 (4-fluorophenyl)(8-methoxy-2H-chromen-3-yl)methanone 

Relevant academic research and scientific papers

RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.

Rhodium(i)-catalyzed Pauson-Khand-type reaction using formic acid as a CO surrogate: An alternative approach for indirect CO2 utilization

Formic acid is found to be an ideal CO surrogate for the rhodium(i)-catalyzed Pauson-Khand-type (PK-type) reaction of various substituted 1,6-enynes to afford bicyclic cyclopentenones in moderate to good yields. High TON value of up to 263 and good results in the gram-scale experiment were also obtained, demonstrating the efficacy of this methodology. In addition, heterocyclic molecules of pharmaceutical importance were also furnished via inter- or intra-molecular hetero-PK-type reactions, further broadening the application of current strategy. In this protocol, formic acid was utilized as a bridging molecule for the conversion of CO2 to CO, since formic acid is manufactured via catalytic hydrogenation of CO2 and releases CO in the presence of acetic anhydride readily. Therefore, this methodology represents a green and indirect approach for chemical valorization of CO2 in the preparation of value-added compounds.

Synthesis and antiviral activity of novel spirocyclic nucleosides

The synthesis of a number of spirocyclic ribonucleosides containing either a triazolic or azetidinic system is described, along with two analogous phosphonate derivatives of the former. These systems were constructed from the same β-d-psicofuranose starti

Design and synthesis of novel xanthine derivatives as potent and selective A2B adenosine receptor antagonists for the treatment of chronic inflammatory airway diseases

Adenosine induces bronchial hyperresponsiveness and inflammation in asthmatics through activation of A2B adenosine receptor (A2BAdoR). Selective antagonists have been shown to attenuate airway reactivity and improve inflammatory cond

HETEROCYCLIC COMPOUNDS AND METHODS OF THEIR USE

The present invention relates generally to compounds that are useful in antagonizing the angiotensin II type 2 (AT2) receptor. More particularly, the invention relates to substituted isoquinoline compounds and their use as AT2 receptor antagonists. Pharmaceutical compositions comprising the compounds and their use in modulating the AT2 receptor and therapies that require modulation of the AT2 receptor are described.

Synthesis and antiviral properties of spirocyclic [1,2,3]-Triazolooxazine nucleosides

An efficient synthesis of spirocyclic triazolooxazine nucleosides is described. This was achieved by the conversion of β-D-psicofuranose to the corresponding azido-derivative, followed by alkylation of the primary alcohol with a range of propargyl bromide

Synthesis of molecular frameworks containing two distinct heterocycles connected in a single molecule with enhanced three-dimensional shape diversity

Herein, we report the synthesis of fused-triazole scaffolds that are connected by pyrimidines, pyrazoles, or pyrazolopyrimidines through carbohydrate-derived stereodivergent linkers. Pyrimidine-, pyrazole-, or pyrazolopyrimidine-based carbohybrids were co

HETEROCYCLIC COMPOUNDS AND METHODS FOR THEIR USE

The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to piperidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.

Iron-catalyzed synthesis of functionalized 2H-chromenes via intramolecular alkyne-carbonyl metathesis

An iron-catalyzed intramolecular alkyne-aldehyde metathesis strategy of the alkynyl ether of salicylaldehyde derivatives has been developed which works under mild reaction conditions to produce the functionalized 2H-chromene derivatives. This protocol is compatible toward a wide range of functional groups, such as methoxy, fluoro, chloro, bromo, and phenyl groups. This method provides an atom-economical and environmentally friendly approach for the synthesis of a series of substituted 2H-chromenes.

NOVEL HETEROCYCLIC COMPOUNDS

The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relat