20943-61-7

Upstream product

• 64-17-5 ethanol 
• 148705-22-0 isopropenyl α-oxo-1H-morpholine-1-acetate 
• 110-91-8 morpholine 
• 4755-77-5 Ethyl oxalyl chloride 
• 201230-82-2 carbon monoxide 
• 100-74-3 N-ethylmorpholine; 
• 95-92-1 oxalic acid diethyl ester 

Downstream Products

• 63833-44-3 morpholino(p-tolyl)methanone 
• 28911-34-4 2-morpholino-2-oxoacetic acid 

Relevant academic research and scientific papers

Pd/C-catalyzed synthesis of oxamates by oxidative cross double carbonylation of alcohols and tertiary amines through C-N bond cleavage

An efficient synthesis of oxamates by Pd/C-catalyzed oxidative cross double carbonylation of alcohols and unactivated tertiary amines has been demonstrated. The in situ oxidative C-N bond cleavage of tertiary amines was achieved using molecular oxygen as an environmentally benign oxidant providing a user-friendly approach to the synthesis of oxamates. The developed protocol showed excellent activity towards the cyclic as well as aliphatic tertiary amines and long-chain alcohols. This developed protocol system is advantageous, as it is phosphine ligand free, base free, and copper-free and the Pd/C catalyst is easily recyclable. The Pd/C catalyst was recycled up to five consecutive cycles.

IMIDAZO[1,2-A]PYRIDINYL DERIVATIVES AS IRAK4 INHIBITORS

This invention relates to Imidazo[1,2-a]pyridinyl Derivatives of formula (I′), or pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, capable of modulating the activity of IRAK4. The invention further provides a method of manufacturing compounds of the invention, and methods for their therapeutic use. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including inflammatory disease, autoimmune disease, cancer, cardiovascular disease, a disease of the central nervous system, disease of the skin, an ophthalmic disease and condition, and a bone disease.

Metal-, Photocatalyst-, and Light-Free Direct C-H Acylation and Carbamoylation of Heterocycles

Direct C-H acylations and carbamoylations of heterocycles can now be readily achieved without requiring any conventional metal, photocatalyst, electrocatalysis, or light activation, thus significantly improving on sustainability, costs, toxicity, waste, and simplicity of the operational procedure. These mild conditions are also suitable for gram-scale reactions and late-stage functionalizations of complex molecules, including pharmaceuticals, N,N-ligands, and light-sensitive molecules.

Synthesis of 2,3-allenylamides utilizing [1,2]-phospha-Brook rearrangement and their application to gold-catalyzed cycloisomerization providing 2-aminofuran derivatives

An efficient synthetic method for 2,3-allenylamides having an oxygen functionality at the 2-position, which are difficult to access by conventional methods, was newly developed by utilizing the [1,2]-phospha-Brook rearrangement under Br?nsted base catalysis. Further manipulation of the 2,3-allenylamides via gold-catalyzed cycloisomerization enables the formation of 2-aminofuran derivatives.

Room-Temperature Decarboxylative Couplings of α-Oxocarboxylates with Aryl Halides by Merging Photoredox with Palladium Catalysis

Enabled by merging iridium photoredox catalysis and palladium catalysis, α-oxocarboxylate salts can be decarboxylatively coupled with aryl halides to generate aromatic ketones and amides at room temperature. DFT calculations suggest that this reaction proceeds through a Pd0-PdII-PdIII pathway, in which the PdIII intermediate is responsible for reoxidizing IrII to complete the IrIII-IrIII-IrII photoredox cycle. Like a mergin': Enabled by merging iridium photoredox catalysis and palladium catalysis, palladium-catalyzed decarboxylative coupling of α-oxocarboxylates with aryl halides can proceed at room temperature. DFT calculations suggest that a Pd0-PdII-PdIII catalytic cycle is merged with an IrIII-IrIII-IrII photoredox cycle, in which PdIII is responsible for oxidizing IrII to complete the photoredox cycle.

NUCLEAR TRANSPORT MODULATORS AND USES THEREOF

The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.

Pd/C-catalyzed synthesis of oxamates by oxidative cross double carbonylation of amines and alcohols under Co-catalyst, base, dehydrating agent, and ligand-free conditions

This work reports a mild, efficient, and ligand-free Pd/C-catalyzed protocol for the oxidative cross double carbonylation of amines and alcohols. Notably, the reaction does not requires any base, co-catalyst, dehydrating agent, or ligand. Pd/C solves the problem of catalyst recovery, and the catalyst was recycled up to six times.

Total synthesis of (-)-goniotrionin

A stereoselective total synthesis of the reported structure of goniotrionin (4) has been accomplished. The key steps involved the opening of a chiral epoxide, a highly diastereoselective Mukaiyama aerobic oxidative cyclization, a selective 1,2-syn Mukaiyama aldol reaction, and a Noyori reduction.

Synthesis and first X-ray structures of cobalt(II) and cobalt(III) complexes bearing 2,4-dioxo-alkanoic acid dialkylamide ligands

The aerobic oxidation of 5-hydroxy pentenes to trans-tetrahydrofurans (THFs), the Mukaiyama oxidation, has in recent years emerged as a powerful tool in synthetic chemistry. In this report we describe the first crystal structures of 2,4-dioxo-alkanoic acid dialkylamide complexes for both Co(II) and Co(III) salts. The Co(II) structures show an unprecedented arrangement of atoms, with a central Co(II)(H2O)6 flanked by two Co(II) atoms each coordinated with three anionic chelating ligands. The dimeric Co(III) structures show two anionic chelating ligands and bridging hydroxyl groups.

Novel syntheses of oxamides, oxamates and oxalates from diisopropenyl oxalate

Diisopropenyl oxalate, obtained by catalytic addition of oxalic acid to propyne, is a useful reagent for the access to a variety of α-dicarbonyl compounds such as oxamides, oxamates and oxalates, under very mild conditions.