90696-21-2

Upstream product

• 37614-59-8 4-(4-methoxyphenyl)prop-2-yn-1-ol 
• 4637-24-5 N,N-dimethyl-formamide dimethyl acetal 
• 768-60-5 4-methoxyphenylacetylen 
• 696-62-8 para-iodoanisole 
• 7515-17-5 methyl 3-(4-methoxyphenyl)propynoate 
• 100-66-3 methoxybenzene 
• 60512-57-4 1-(2,2-dibromovinyl)-4-methoxybenzene 
• 68-12-2 N,N-dimethyl-formamide 
• 624-67-9 Propargylic aldehyde 
• 107-19-7 propargyl alcohol 
• 62358-88-7 1-(3,3-diethoxyprop-1-yn-1-yl)-4-methoxybenzene 
• 123-11-5 4-methoxy-benzaldehyde 

Downstream Products

• 90718-42-6 [3-(4-Methoxy-phenyl)-prop-2-yn-(E)-ylidene]-trimethylsilanyl-amine 
• 647029-40-1 (4S)-4-benzyl-[(2R,3S)-3-hydroxy-5-(4-methoxyphenyl)-2-(3,4-methylenedioxybenzyl)-4-pentynoyl]-2-oxazolidinone 
• 647029-26-3 (4S)-4-benzyl-[(2R,3R)-3-hydroxy-5-(4-methoxyphenyl)-2-(3,4-methylenedioxybenzyl)-4-pentynoyl]-2-oxazolidinone 
• 647029-27-4 (4S)-4-benzyl-[(2S,3S)-3-hydroxy-5-(4-methoxyphenyl)-2-(3,4-methylenedioxybenzyl)-4-pentynoyl]-2-oxazolidinone 
• 90696-28-9 cis-3-isopropyl-4-((p-methoxyphenyl)ethynyl)-2-azetidinone 
• 5466-78-4 benzyl 4-methoxycinnamate 
• 1071813-79-0 C₁₀H₉N₃O₂ 
• 17171-17-4 4'-methoxy-3-methylbiphenyl 
• 1203668-62-5 (E)-1-methoxy-4-(4-nitrobut-3-en-1-ynyl)benzene 
• 1220193-93-0 (R)-2-(4-methoxyphenyl)-4-(nitromethyl)-4H-chromene-3-carbaldehyde 
• 1221590-69-7 C₂₀H₁₈O₃ 
• 1232144-20-5 (S)-methyl-3-(6-((tert-butyldimethylsilyloxy)methyl)-3-hydroxy-4-oxo-4H-pyran-2-yl)-3-(4-methoxyphenyl)propanoate 
• 1253522-12-1 (S)-N-(3-formyl-2-(4-methoxyphenyl)-4H-chromen-4-yl)-4-methylbenzenesulfonamide 
• 1254213-00-7 (R) ethyl 3-formy-4-hydroxy-7-methoxy-2-(4-methoxyphenyl)-4H-chromene-4-carboxylate 

Relevant academic research and scientific papers

Flexible Construction of Functionalized-Pyrroles under Palladium or Copper Catalysis in the Presence of BF3 ? Et2O

We have developed a flexible approach enabling the access to highly functionalized pyrroles under palladium or copper catalysis in the presence of BF3 ? Et2O. This catalytic methodology utilizes commercially available amines as react

NHC-catalyzed enantioselective C2-functionalization of 3-hydroxychromenonesviaα,β-unsaturated acyl azoliums

A novel synthetic method for enantioselective C2-functionalization of 3-hydroxychromenones promoted by N-heterocyclic carbenesviathe formation of α,β-unsaturated acyl azolium intermediates, which occurs with Coates-Claisen rearrangement is established. This synthetic strategy enabled the rapid assembly of enantiomerically enriched δ-hydroxychromenone-derived esters/amides under mild conditions with good to excellent yields and broad substrate scope.

Micelle-Mediated Trimerization of Ynals to Orthogonally Substituted 4H-Pyrans in Water: Downstream Rearrangement to Bioactive 2,8-dioxabicyclo[3.3.1]nona-3,6-diene Frameworks

An efficient trimerization of ynals to diversely substituted 4H-pyran constructs has been executed in water, under ambient conditions employing micellar catalysis. The method is in agreement with the ideas of green and sustainable chemistry. The locus of the micellar reaction site has been probed through proton NMR studies. A general acid-mediated downstream rearrangement of the derived 4H-pyrans to interesting 2,8-dioxabicyclo[3.3.1]nona-3,6-dienes has been observed.

Synthesis of Chiral Propargylamines, Chiral 1,2-Dihydronaphtho[2,1-b]furans and Naphtho[2,1-b]furans with C-Alkynyl N,N′-di-(tert-butoxycarbonyl)-aminals and β-Naphthols

Chiral phosphoric acid-catalyzed couplings of C-alkynyl N,N′-di-(tert-butoxycarbonyl)-aminals with β-naphthols led to chiral propargylamines in moderate to high yields with high to excellent enantioselectivity, in which the reactions underwent sequential chiral phosphoric acid-catalyzed in situ formation of N-(tert-butoxycarbonyl)-imines (N-Boc-imines) from the aminals, and 1,2-addition of β-naphthols to the N-Boc-imines. Chiral 1,2-dihydronaphtho[2,1-b]furans and naphtho[2,1-b]furans were prepared with satisfactory results when 10 mol% AgOAc and 20 mol% 2,6-lutidine or 1.2 equiv. of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) were added to the resulting chiral propargylamines solution, respectively.

Transition-metal-free and facile synthesis of 3-alkynylpyrrole-2,4-dicarboxylates from methylene isocyanides and propiolaldehyde

A transition-metal-free, facile and efficient method for the synthesis of 3-alkynylpyrrole-2,4-dicarboxylates from methylene isocyanides and propiolaldehyde with moderate to good yields has been developed. The direct transformation process and good tolerance of various substituents make it an alternative approach to previous protocols, and potential applications of these investigated compounds are expected with or without post-modifications.

Regiodivergent Hydration-Cyclization of Diynones under Gold Catalysis

Skipped diynones, efficiently prepared from biomass-derived ethyl lactate, undergo a tandem hydration-oxacyclization reaction under gold(I) catalysis. Reaction conditions have been developed for a switchable process that allows selective access to 4-pyrones or 3(2H)-furanones from the same starting diynones. Further application of this methodology in the total synthesis of polyporapyranone B was demonstrated.

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.

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.

Iron-Catalyzed Aerobic Oxidation of Alcohols: Lower Cost and Improved Selectivity

An aerobic oxidation reaction of alcohols toward aldehydes or ketones using catalytic amounts of Fe(NO3)3·9H2O, 4-OH-TEMPO, and NaCl has been developed. Compared with the former catalytic system with TEMPO developed in this group, the new protocol using 4-OH-TEMPO, which is much cheaper on an industrial scale, accomplished the transformation with a higher selectivity, especially for aliphatic alcohols toward aldehydes. α,β-Unsaturated alkynals or alkynones can be efficiently synthesized from propargyl alcohols, which has been much less studied in the literature.

Catalyst-Free Annulation of 2-Pyridylacetates and Ynals with Molecular Oxygen: An Access to 3-Acylated Indolizines

A catalyst and additive-free annulation of 2-pyridylacetates and ynals under molecular oxygen was the first developed, affording 3-acylated indolizines in good to excellent yields. Molecular oxygen was used as the source of the carbonyl oxygen atom in indolizines. This approach was compatible with a wide range of functional groups, and especially it has been successfully extended to unsaturated double bonds and triple bonds, which were difficult to prepare by previous methods in a single step.