1394175-04-2

Upstream product

• 127095-97-0 (2S)-2-[(tert-butoxycarbonyl)amino]-3-(3,4-dimethoxyphenyl)propanoic acid 
• 24424-99-5 di-tert-butyl dicarbonate 
• 59-92-7 levodopa 
• 105779-71-3 (S)-(-)-[2-(3,4-dimethoxyphenyl)-1-hydroxymethylethyl]carbamic acid tert-butyl ester 
• 32161-30-1 (S)-3,4-dimethoxyphenylalanine 
• 138908-56-2 (S)-(+)-2-tert-butoxycarbonylamino-3-(3,4-dimethoxyphenyl)propionic acid methyl ester 
• 30033-24-0 (2S)-3-(3,4-dihydroxyphenyl)-2-[(tert-butoxy)carbonylamino]propanoic acid 

Downstream Products

• 1394175-05-3 [rac-2-(3,4-dimethoxyphenyl)-1-(1H-imidazol-2-yl)ethyl]carbamic acid tert-butyl ester 
• 1394175-08-6 rac-8-(3,4-dimethoxybenzyl)-7,8-dihydroimidazo[1,2-a]pyrazin-6-one 

Relevant academic research and scientific papers

Probing α-Amino Aldehydes as Weakly Acidic Pronucleophiles: Direct Access to Quaternary α-Amino Aldehydes by an Enantioselective Michael Addition Catalyzed by Br?nsted Bases

The high tendency of α-amino aldehydes to undergo 1,2-additions and their relatively low stability under basic conditions have largely prevented their use as pronucleophiles in the realm of asymmetric catalysis, particularly for the production of quaternary α-amino aldehydes. Herein, it is demonstrated that the chemistry of α-amino aldehydes may be expanded beyond these limits by documenting the first direct α-alkylation of α-branched α-amino aldehydes with nitroolefins. The reaction produces densely functionalized products bearing up to two, quaternary and tertiary, vicinal stereocenters with high diastereo- and enantioselectivity. DFT modeling leads to the proposal that intramolecular hydrogen bonding between the NH group and the carbonyl oxygen atom in the starting α-amino aldehyde is key for reaction stereocontrol.

Nitrogen (oxygen) heterocyclic pentane - 2 - one (thione) compound, pharmaceutical composition, preparation method and use thereof

The invention belongs to the field of pharmacology, and relates to aza (oxa)-cyclopentane-2- ketone (thione) compounds shown in the formula I, medicine compositions thereof, a preparation method, applications in preparation of medicines treating diabetes and glucolipid metabolism, and especially applications in preparation of medicines treating II-type diabetes.

NOVEL INDOLE AND PYRROLOPYRIDINE AMIDES

The present invention relates to indole and pyrrolopyridine amide derivatives of formula (I) wherein R1, R 2, R 3, U, V, W, X, Y, Z and ring A are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.