10047-10-6

Upstream product

• 67-56-1 methanol 
• 760-78-1 2-aminopentanoic acid 
• 848613-42-3 2-aminopentanoic acid (hydrochloride) 

Downstream Products

• 144232-17-7 2-((S)-2-Benzyloxycarbonylamino-4-methyl-pentanoylamino)-pentanoic acid methyl ester 
• 296282-25-2 2-(2-amino-benzoylamino)-pentanoic acid methyl ester 
• 1370228-79-7 (RS)-methyl 2-((N-(tert-butoxycarbonyl)-N-(3-phenoxybenzyl)sulfamoyl)amino)-pentanoate 
• 296282-02-5 2-[2-(2-amino-benzoylamino)-benzoylamino]-pentanoic acid methyl ester 
• 124094-91-3 2-{[1-Phenyl-meth-(E)-ylidene]-amino}-pentanoic acid methyl ester 
• 137132-13-9 N- norvaline methyl ester 
• 4146-04-7 DL-2-amino-1-pentanol 

Relevant academic research and scientific papers

New 2-(2'-phenyl-9'-benzyl-8'-azapurin-6'-ylamino)-carboxylic acid methylesters as ligands for A1 adenosine receptors.

Synthesis of a series of new 2-phenyl-9-benzyl-8-azaadenines bearing on N6 an alkyl or aralkyl chain having a carbonyloxymethyl group on the carbon bound to N6 were reported. The ester group could assure to the molecule a better water-solubility than the 8-azaadenines 2, 6 and 9 substituted with lipophilic groups synthesised in the past. Compounds synthesised demonstrated only little capability of binding A1 adenosine receptors.

PARP1 INHIBITORS

The present invention relates to azaquinolone compounds of Formula (I), and their use in medicine. Formula (I)

Regiodivergent Enantioselective γ-Additions of Oxazolones to 2,3-Butadienoates Catalyzed by Phosphines: Synthesis of α,α-Disubstituted α-Amino Acids and N,O-Acetal Derivatives

Phosphine-catalyzed regiodivergent enantioselective C-2- and C-4-selective γ-additions of oxazolones to 2,3-butadienoates have been developed. The C-4-selective γ-addition of oxazolones occurred in a highly enantioselective manner when 2-aryl-4-alkyloxazol-5-(4H)-ones were employed as pronucleophiles. With the employment of 2-alkyl-4-aryloxazol-5-(4H)-ones as the donor, C-2-selective γ-addition of oxazolones took place in a highly enantioselective manner. The C-4-selective adducts provided rapid access to optically enriched α,α-disubstituted α-amino acid derivatives, and the C-2-selective products led to facile synthesis of chiral N,O-acetals and γ-lactols. Theoretical studies via DFT calculations suggested that the origin of the observed regioselectivity was due to the distortion energy that resulted from the interaction between the nucleophilic oxazolide and the electrophilic phosphonium intermediate.

QUINAZOLINEDIONE CHYMASE INHIBITORS

Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving Chymase.

Resolution of non-protein amino acids via the microbial protease-catalyzed enantioselective hydrolysis of their N-unprotected esters

In the Aspergillus oryzae protease-catalyzed ester hydrolysis, substitution of N-unprotected amino acid esters for the corresponding N-protected amino acid esters resulted in a large enhancement of the hydrolysis rate, while the enantioselectivity was deteriorated strikingly when the substrates employed were the conventional methyl esters. This difficulty was overcome by employing esters bearing a longer alkyl chain such as the isobutyl ester. Utilizing this ester, amino acids carrying an aromatic side chain were resolved with excellent enantioselectivities (E=50 to >200). With amino acids bearing an aliphatic side chain also, good results in terms of the hydrolysis rate and enantioselectivity were obtained by employing such an ester as the isobutyl ester. Moreover, the enantioselectivity proved to be enhanced further by conducting the reaction at low temperature. This procedure was applicable to the case where the enantioselectivity was not high enough even by the use of the isobutyl ester.