17745-40-3

Upstream product

• 67-56-1 methanol 
• 201230-82-2 carbon monoxide 
• 87241-55-2 4-propionylphenol trifluoromethanesulfonate 
• 4219-55-0 4-propionylbenzoic acid 
• 112513-57-2 4-(2-Nitro-propionyl)-benzoic acid methyl ester 
• 96056-29-0 1--2-propanol 
• 74-88-4 methyl iodide 
• 3609-53-8 methyl 4-acetylbenzoate 
• 70-70-2 4-hydroxypropiophenone 
• 245679-66-7 N-cyclohexyl-4-(methoxycarbonyl)benzamide 
• 925-90-6 ethylmagnesium bromide 
• 811-49-4 ethyllithium 
• 923-34-2 Triethylindium 
• 135738-30-6 ethylcerium dichloride 

Downstream Products

• 58764-22-0 methyl 4-(2-bromopropanoyl)benzoate 
• 33036-62-3 4-Bromo-1-butanol 
• 142721-21-9 Methyl 4-[[2-(2,4-Diamino-5-methylpyrido[2,3-d]-pyrimidin-6-yl)-1-ethyl]ethenyl]benzoate 
• 1186680-40-9 4-((E)-1-benzyloxycarbonylmethylpropenyl)benzoic acid methyl ester 
• 81631-63-2 p-(methoxycarbonyl)-n-propylbenzene 
• 1196046-98-6 methyl 4-(1-aminopropyl)benzoate hydrochloride 
• 142721-20-8 methyl 4-<2-(2,4-diamino-6-pteridinyl)-1-ethylethenyl>benzoate 

Relevant academic research and scientific papers

Photoredox/nickel-catalyzed hydroacylation of ethylene with aromatic acids

We report a general, practical and scalable hydroacylation reaction of ethylene with aromatic carboxylic acids with the synergistic combination of nickel and photoredox catalysis. Under ambient temperature and pressure, feedstock chemicals such as ethylene can be converted into high-value-added aromatic ketones in moderate to good yields (up to 92%) with reaction time of 2-6 hours.

Palladium-catalyzed room temperature acylative cross-coupling of activated amides with trialkylboranes

A highly efficient acylative cross-coupling of trialkylboranes with activated amides has been effected at room temperature to give the corresponding alkyl ketones in good to excellent yields by using 1,3-bis(2,6-diisopropyl)phenylimidazolylidene and 3-chloropyridine co-supported palladium chloride, the PEPPSI catalyst, in the presence of K2CO3 in methyl tert-butyl ether. The scope and limitations of the protocol were investigated, showing good tolerance of acyl, cyano, and ester functional groups in the amide counterpart while halo group competed via the classical Suzuki coupling. The trialkylboranes generated in situ by hydroboration of olefins with BH3 or 9-BBN performed similarly to those separately prepared, making this protocol more practical.

DMF as carbon source: Rh-catalyzed α-methylation of ketones

An unprecedented Rh-catalyzed direct methylation of ketones with N,N-dimethylformamide (DMF) is disclosed. The reaction shows a broad substrate scope, tolerating both aryl and alkyl ketones with various substituents. Mechanistic studies suggest that DMF delivers a methylene fragment followed by a hydride in the methylation process.

Chemoselective synthesis of ketones and ketimines by addition of organometallic reagents to secondary amides

The development of efficient and selective transformations is crucial in synthetic chemistry as it opens new possibilities in the total synthesis of complex molecules. Applying such reactions to the synthesis of ketones is of great importance, as this motif serves as a synthetic handle for the elaboration of numerous organic functionalities. In this context, we report a general and chemoselective method based on an activation/addition sequence on secondary amides allowing the controlled isolation of structurally diverse ketones and ketimines. The generation of a highly electrophilic imidoyl triflate intermediate was found to be pivotal in the observed exceptional functional group tolerance, allowing the facile addition of readily available Grignard and diorganozinc reagents to amides, and avoiding commonly observed over-addition or reduction side reactions. The methodology has been applied to the formal synthesis of analogues of the antineoplastic agent Bexarotene and to the rapid and efficient synthesis of unsymmetrical diketones in a one-pot procedure. Macmillan Publishers Limited. All rights reserved.

Efficient synthesis of alkyl aryl ketones & ketals via palladium-catalyzed regioselective arylation of vinyl ethers

The combination of Pd(OAc)2 with 1,3-bis(diphenylphosphino) propane (dppp) in ethylene glycol constitutes a high-performance catalytic system for highly regioselective arylation of a range of electron-rich vinyl ethers by aryl bromides to provide, upon hydrolysis, alkyl aryl ketones and cyclic ketals in good yields with up to 3.75 × 105 TON and 15625 h-1 TOF.

PROTEASE INHIBITORS

Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one

PROTEASE INHIBITORS

Compounds of the formula II, wherein R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3/

Cysteine Protease Inhibitors

Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; Rq is trifluoromethyl and Rq′ is H or Rq and Rq′ define keto; Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)piperazin-1-yl-thiazol-4-yl- moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.

PROTEASE INHIBITORS

Compounds of the formula (II): wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or fluoro; R4 is C1-C6alkyl; E is a bond or thiazolyl, optionally substituted with methyl or fluoro; n is 0 or 1; or a pharmaceutically acceptable salt, N-oxide or hydrate thereof; have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsinK, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.