118460-23-4

Upstream product

• 186581-53-3 diazomethane 
• 42492-62-6 (S)-N-benzyl-N-metylvaline 
• 4070-48-8 L-Valine methyl ester 
• 100-39-0 benzyl bromide 
• 40216-62-4 N-benzyl-L-valine methyl ester 
• 74-88-4 methyl iodide 
• 50-00-0 formaldehyd 
• 100-52-7 benzaldehyde 
• 15363-84-5 (S)-2-(benzylamino)-3-methylbutanoic acid 
• 6306-52-1 L-valine methylester hydrochloride 
• 72-18-4 L-valine 

Downstream Products

• 1403983-89-0 2-[benzyl(methyl)amino]-3-methyl-1,1-diphenylbutan-1-ol 
• 35016-37-6 N-methyl-L-valine methyl ester 

Relevant academic research and scientific papers

Preparation of the optically pure N-methyl amino ester method and product

The invention belongs to the field of organic synthesis of amino acids and discloses a method for preparing optically pure N-methyl amino-acid ester. The method comprises the following steps of carrying out esterification reaction on amino acid as a starting raw material and aldehyde to form an imine intermediate, carrying out reductive amination in the presence of palladium carbon, and carrying out hydrogenation and debenzylation to finally synthesize optically pure N-methyl amino-acid ester. The method has the advantages of simplicity in method, mild reaction conditions and good adaptability and side chains of D-type or L-type amino acid do not need to be protected.

THERAPEUTIC COMPOUNDS AS INHIBITORS OF THE OREXIN-1 RECEPTOR

The present invention relates to compounds that are inhibitors of the orexin-1 receptor. The compounds have the structural formula I defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with orexin-1 receptor activity.

Synthesis of enantiomerically enriched indolines and tetrahydroisoquinolines from (S)-amino acid-derived chiral carbocations: An easy access to (3S,4R)-demethoxy-3-isopropyl diclofensine

Enantiomerically enriched indolines and tetrahydroisoquinolines were synthesized within 5 min to 2 h in high yields from easily accessible (S)-amino acid derived chiral carbocations. The diastereoselective Friedel-Crafts reaction is promoted by a Lewis acid (AlCl3) offering trans-diastereoselectivity. The rate of the reaction and diastereoselectivity of the product are significantly influenced by steric hindrance of the amino acids substituents and aryl groups. The methodology can be applied for the synthesis of the enantiomerically enriched bioactive scaffold (3S,4R)-demethoxy-3-isopropyl diclofensine. This journal is

Nucleophilic Ring-Opening Reactions of Morpholin-2-ones. A Resolution of dl-(Secondary-alkyl)amines

The alcoholysis of morpholin-2-ones yielded an equilibrium mixture of morpholin-2-one and the corresponding hydroxy ester.The equilibrium constants for the methanolysis of several sustituted morpholin-2-ones were determined.Treatment of optically active morpholin-2-ones with (secondary-alkyl)amines resulted in stereoselective ring opening to afford hydroxy amides with up to 30percent de.Hydrolysis of one such hydroxy amide regenerated the optically active (secondary-alkyl)amine and the morpholin-2-one.