29768-03-4

Upstream product

• 109-04-6 2-bromo-pyridine 
• 107-19-7 propargyl alcohol 
• 51480-24-1 tetrahydropyranyloxypropargylmagnesium bromide 
• 109-09-1 2-chloropyridine 
• 5029-67-4 2-iodopyridine 
• 694-59-7 pyridine N-oxide 
• 1945-84-2 2-ethynylpyridine 
• 50-00-0 formaldehyd 
• 19070-80-5 n-<(trimethylsiloxy)methyl>phthalimide 
• 86521-05-3 2-(trimethylsilylethynyl)pyridine 
• 6175-54-8 hydroxy-1-propyne 

Downstream Products

• 82244-21-1 2-phenyl-3-(2-pyridyl)-2-propen-1-ol 
• 2859-68-9 3-(pyridin-2-yl)-propanol 
• 113985-52-7 (E)-3-(pyridin-2-yl)prop-2-en-1-ol 
• 82244-38-0 2-phenyl-3-(2-pyridyl)-2-propenal 
• 82244-29-9 2-Phenyl-3-piperidin-1-yl-indolizine 
• 133739-01-2 4-methoxy-4-[3-(3-(pyridin-2-yl)prop-2-yn-1-yloxy)phenyl]tetrahydropyran 
• 1254485-96-5 ethyl 5-formyl-2-phenyl-4-(pyridin-2-yl)furan-3-carboxylate 
• 1338920-67-4 C₁₇H₁₁NO₂ 
• 1599470-49-1 2-(3-(3-phenylprop-2-ynyloxy)prop-1-ynyl)pyridine 
• 1599470-55-9 2-(3-(3-(4-methoxyphenyl)prop-2-ynyloxy)prop-1-ynyl)pyridine 
• 767-61-3 1-methylindolizine 
• 24448-89-3 2-(3-hydroxypropyl)piperidine 
• 113985-43-6 2-(3-methoxyprop-1-yn-1-yl)pyridine 
• 76943-44-7 2,4,6-Trimethyl-benzenesulfonate1-amino-2-(3-hydroxy-prop-1-ynyl)-pyridinium; 

Relevant academic research and scientific papers

Carreira alkynylations with paraformaldehyde. A mild and convenient protocol for the hydroxymethylation of complex base-sensitive terminal acetylenes via alkynylzinc triflates

A new synthetic protocol for the hydroxymethylation of terminal acetylenes is described that involves stoichiometric Carreira alkynylation with solid paraformaldehyde (HO[CH2O]nH) in PhMe at 60 °C. Significantly, the method can be su

Palladium-catalyzed dearomative cyclocarbonylation of allyl alcohol for the synthesis of quinolizinones

An approach for the synthesis of quinolizinone with potential bioactivity has been developedviapalladium-catalytic dearomative cyclocarbonylation of allyl alcohol. Diverse quinolizinone compounds could be attained with good efficiencies. A feasible reaction pathway could be a successive procedure of allylation, dearomatization, CO insertion and the Heck reaction.

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.

BICYCLIC JAK INHIBITORS AND USES THEREOF

Provided herein are compounds of Formulas (I), (II), (III), and (IV) and subformulas thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I), (II), (III), or (IV) and methods of using the compounds, e.g., in the treatment of immune disorders, inflammatory disorders, and cancer.

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.

Preparation of monoalkylpiperidines via the mild hydrogenation of monoalkynylpyridines

Monoalkynylpyridines were prepared via a Sonogashira cross-coupling reaction between monoiodopyridines and alkynes. Mild hydrogenation of the obtained monoalkynylpyridines was then conducted to produce the corresponding monoalkylpiperidines in moderate to excellent yields. The hydrogenation reaction was carried out under H2 (1?atm) in the presence of 10?wt% Pd/C (5?eq) in either AcOH or MeOH at room temperature. The present mild method is therefore useful for the quick and easy preparation of monoalkylpiperidines.

METHOD FOR PRODUCING PIPERIDINE COMPOUND

PROBLEM TO BE SOLVED: To provide a method for producing a piperidine compound in an industrially convenient manner. SOLUTION: This invention relates to a method for producing a compound represented by general formula (I) or a salt thereof that includes the step of converting a pyridine compound having an alkynylene group in a side chain, by a contact hydrogenation reaction, into the compound represented by general formula (I) or a salt thereof (in the general formula (I), R1 is a hydrogen atom, a hydroxy group, or an optionally substituted alkyl group having carbon atoms of 1 or more and 20 or less). SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT

Sodium Phenoxide Mediated Hydroxymethylation of Alkynylsilanes with N-[(Trimethylsiloxy)methyl]phthalimide

The hydroxymethylation of alkynylsilanes with formaldehyde generated in situ from N-[(trimethylsiloxy)methyl]phthalimide proceeds in the presence of a stoichiometric amount of NaOPh. The reaction occurs at room temperature by using an operationally simple one-step procedure. A variety of alkynylsilanes possessing electron-donating, electron-withdrawing, and halogen groups (including heteroaryl-substituted alkynylsilanes) provide hydroxymethylated products.

Fused Selenazolinium Salt Derivatives with a Se-N+ Bond: Preparation and Properties

Convenient methods for the preparation of stable, fused selenazolinium salt systems with a Se-N+ bond have been developed. The mechanism for the formation of the selenazole cycle was investigated in detail by conducting multinuclear NMR experiments. The ability of these compounds to form stable inner salts was demonstrated. We have shown the glutathione peroxidase (GPx) like properties of selenazolopyridinium salts by oxidizing sulfur-containing natural amino acids, as well as aromatic and heteroaromatic aldehydes. The molecular structures of most of the compounds were confirmed by X-ray diffraction studies.

Selectivity in Garratt-Braverman cyclization of aryl-/heteroaryl- substituted unsymmetrical bis-propargyl systems: Formal synthesis of 7′-desmethylkealiiquinone

Unsymmetrical bis-propargyl ethers and sulfonamides containing various combinations of aryl/heteroaryl substituents at the acetylene termini were synthesized, and their reactivity under basic conditions was studied. Moderate to high (chemo)selectivity was