2620-11-3

Upstream product

• 598-72-1 2-Bromopropionic acid 
• 100-61-8 N-methylaniline 
• 7148-74-5 2-Bromopropionyl chloride 
• 563-76-8 α-bromopropionyl bromide 

Downstream Products

• 46988-26-5 N-Methyl-2--propionanilid 
• 5827-78-1 N-methyl-N-phenylpropanamide 
• 647018-70-0 (1-{tert-butyl-[1-(methyl-phenyl-carbamoyl)-ethoxy]-amino}-2,2-dimethyl-propyl)-phosphonic acid diethyl ester 
• 251346-03-9 2-iodo-N-methyl-N-phenylpropanamide 
• 5455-67-4 N-methyl-N-phenyl-α-hydroxypropanamide 
• 802256-19-5 N-Methyl-2--propionsaeure-anilid 
• 1522362-26-0 4-(4-(tert-butyl)phenyl)-N,2-dimethyl-4-oxo-N-phenylbutanamide 
• 1228378-14-0 2-azido-N-methyl-N-phenylpropanamide 
• 1616976-38-5 2-(chloro-λ⁵-azaneyl)-N-methyl-N-phenylpropanamide hydrochloride 
• 1616976-39-6 N-methyl-N-phenyl-2-[(2-phenylquinolin-4-yl)amino]propanamide 
• 1616976-40-9 N-methyl-N-phenyl-2-[(2-phenylquinolin-4-yl)oxy]propanamide 
• 1616976-41-0 N-methyl-N-phenyl-2-(quinolin-4-yloxy)propanamide 
• 1616976-42-1 N-methyl-N-phenyl-2-[(2-phenylpyridin-4-yl)oxy]propanamide 
• 1616976-48-7 N-methyl-N-phenyl-2-{[2-(pyridin-2-yl)quinolin-4-yl]oxy}propanamide 

Relevant academic research and scientific papers

Enantioconvergent Cu-Catalyzed Radical C-N Coupling of Racemic Secondary Alkyl Halides to Access α-Chiral Primary Amines

α-Chiral alkyl primary amines are virtually universal synthetic precursors for all other α-chiral N-containing compounds ubiquitous in biological, pharmaceutical, and material sciences. The enantioselective amination of common alkyl halides with ammonia is appealing for potential rapid access to α-chiral primary amines, but has hitherto remained rare due to the multifaceted difficulties in using ammonia and the underdeveloped C(sp3)-N coupling. Here we demonstrate sulfoximines as excellent ammonia surrogates for enantioconvergent radical C-N coupling with diverse racemic secondary alkyl halides (>60 examples) by copper catalysis under mild thermal conditions. The reaction efficiently provides highly enantioenrichedN-alkyl sulfoximines (up to 99% yield and >99% ee) featuring secondary benzyl, propargyl, α-carbonyl alkyl, and α-cyano alkyl stereocenters. In addition, we have converted the masked α-chiral primary amines thus obtained to various synthetic building blocks, ligands, and drugs possessing α-chiral N-functionalities, such as carbamate, carboxylamide, secondary and tertiary amine, and oxazoline, with commonly seen α-substitution patterns. These results shine light on the potential of enantioconvergent radical cross-coupling as a general chiral carbon-heteroatom formation strategy.

Visible-Light-Driven Aryl Migration and Cyclization of α-Azido Amides

This paper reports two new visible-light-promoted radical reactions of α-azido amides. By catalysis of [Ir(ppy)2(dtbbpy)]PF6 with i-Pr2NEt as the reducing agent, N-aryl α-azido tertiary amides were first converted to the corresponding aminyl radicals through reduction of the azido group; the aminyl radicals then underwent N-to-N aryl migration to give α-anilinyl-functionalized amides. α-Azido secondary amides, on the other hand, reacted with the solvent ethanol and i-Pr2NEt to afford the imidazolinone products.

A copper(II)-mediated radical cross-dehydrogenative coupling/sulfinic acid elimination approach to 2-quinolones

A new cyclisation procedure to prepare 4-carboxy-quinolin-2-ones via a one-pot Cu(II)-mediated radical cross-dehydrogenative coupling/sulfinic acid elimination of linear anilides is described. Extensions to more complex substrates are also reported as are

Nickel-Catalyzed Asymmetric C-Alkylation of Nitroalkanes: Synthesis of Enantioenriched β-Nitroamides

A general catalytic method for asymmetric C-alkylation of nitroalkanes using nickel catalysis is described. This method enables the formation of highly enantioenriched β-nitroamides from readily available α-bromoamides using mild reaction conditions that are compatible with a wide range of functional groups. When combined with subsequent reactions, this method allows access to highly enantioenriched products with nitrogen-bearing fully substituted carbon centers.

INDANE DERIVATIVES USEFUL AS MODULATORS OF MGLUR7

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, X, Y, Z, D, R1, R2, R3, R4, R12, R15nd R16 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use as modulators of mGluR7.

Electrochemical dehydrogenative cyclization of 1,3-dicarbonyl compounds

The intramolecular C(sp3)-H/C(sp2)-H cross-coupling of 1,3-dicarbonyl compounds has been achieved through Cp2Fe-catalyzed electrochemical oxidation. The key to the success of these dehydrogenative cyclization reactions is

Transfer Hydro-dehalogenation of Organic Halides Catalyzed by Ruthenium(II) Complex

A simple and efficient Ru(II)-catalyzed transfer hydro-dehalogenation of organic halides using 2-propanol solvent as the hydride source was reported. This methodology is applicable for hydro-dehalogenation of a variety of aromatic halides and α-haloesters and amides without additional ligand, and quantitative yields were achieved in many cases. The potential synthetic application of this method was demonstrated by efficient gram-scale transformation with catalyst loading as low as 0.5 mol %.

Synthesis and microbicidal activity of substituted 1,2,3-triazoles having amide and hydroxy functionality

A series of 1,4-disubstituted 1,2,3-triazoles was designed and synthesized from hydroxy terminal alkynes and 2-azido-N-substituted Nphenylpropanamides. All the synthesized substituted triazoles were characterized by spectral techniques (FT-IR, 1H NMR, 13C

A Direct C-H/Ar-H Coupling Approach to Oxindoles, Thio-oxindoles, 3,4-Dihydro-1 H-quinolin-2-ones, and 1,2,3,4-Tetrahydroquinolines

A copper(II)-catalysed approach to oxindoles, thio-oxindoles, 3,4-dihydro-1H-quinolin-2-ones, and 1,2,3,4-tetrahydroquinolines via formal C-H, Ar-H coupling is described. In a new variant, copper(II) 2-ethylhexanoate has been identified as an inexpensive and efficient catalyst for this transformation, which utilises atmospheric oxygen as the re-oxidant. Copper(II) 2-ethylhexanoate: The synthesis of oxindoles, thio-oxindoles, 3,4-dihydro-1H-quinolin-2-ones, and 1,2,3,4-tetrahydroquinolines from linear precursors by direct C-H, Ar-H coupling by using a single copper catalyst is reported (see scheme; DIPEA=diisopropylethylamine, EWG=electron-withdrawing group). The cyclisations are simple to perform, run open to the air, are moisture insensitive, and use an inexpensive catalyst.

A novel synthetic approach to (±)-desoxynoreseroline

(±)-Desoxynoreseroline (3), the basic ring structure of the pharmacologically active alkaloid physostigmine (1), was synthesized starting from 3-allyl-1,3-dimethyloxindole (9). The latter was prepared from the corresponding 2H-azirin-3-amine 6 by a BFsub