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Upstream product

• 6600-40-4 L-Norvaline 
• 75-36-5 acetyl chloride 
• 67-56-1 methanol 
• 27493-23-8 L-norvaline hydrochloride 
• 2013-12-9 D-norvaline 
• 498-18-0 norvaline 
• 501033-83-6 (2S,3R)-3-(tert-butoxycarbonylamino)hexane-1,2-diol 
• 220515-19-5 tert-butyl-(2S,3S)-1,2-dihydroxyhexan-3-ylcarbamate 
• 848613-42-3 2-aminopentanoic acid (hydrochloride) 
• 760-78-1 2-aminopentanoic acid 

Relevant academic research and scientific papers

PARP1 INHIBITORS

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

A class of nitrogen-containing heterocyclic butane framework of non-natural amino acid derivative and its synthesis method (by machine translation)

The invention belongs to the technical field of chemical synthesis, in particular discloses a containing azetidine skeleton of the synthesis method of the non-natural amino acid derivatives, its target product non-natural amino acid derivatives of the formula such as the specification of the Chinese (I), (II), (III), (IV) and (V) as shown in the, in the formula compound is a nitrogen-containing heterocyclic butane framework of non-naturalα-,β- Andγ- Amino acid derivatives, nitrogen atom are 2 - pyridine carboxylic acid protection; carboxyl methyl esterification; formula (I) in order to contain the azetidine framework of non-naturalα- Amino acid derivatives; (II) for the formula containing azetidine bridge ring skeleton of non-naturalα- Amino acid derivatives, wherein n=1 or 2; type (III) is a nitrogen-containing heterocyclic butane and ring skeleton of non-naturalα- Amino acid derivatives; formula (IV) is a nitrogen-containing heterocyclic butane bridge ring skeleton of non-naturalβ- Amino acid derivatives; type (V) is a nitrogen-containing heterocyclic butane and ring skeleton of non-naturalγ- Amino acid derivatives. The experiment of this invention result proves that: the compounds have potential hypolipidemic activity. (by machine translation)

Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate

Carboxamide pyrazinyloxy benzoxaboroles were investigated with the goal to identify a molecule with satisfactory antimalarial activity, physicochemical properties, pharmacokinetic profile, in vivo efficacy, and safety profile. This optimization effort discovered 46, which met our target candidate profile. Compound 46 had excellent activity against cultured Plasmodium falciparum, and in vivo against P. falciparum and P. berghei in infected mice. It exhibited good PK properties in mice, rats, and dogs. It was highly active against the other 11 P. falciparum strains, which are mostly resistant to chloroquine and pyrimethamine. The rapid parasite in vitro reduction and in vivo parasite clearance profile of 46 were similar to those of artemisinin and chloroquine, two rapid-acting antimalarials. It was nongenotoxic in an Ames assay, an in vitro micronucleus assay, and an in vivo rat micronucleus assay when dosed orally up to 2000 mg/kg. The combined properties of this novel benzoxaborole support its progression to preclinical development.

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.

Synthesis, crystal structure and biological activity screening of novel N-(α-bromoacyl)-α-amino esters containing valyl moiety

Three novel N-(α-bromoacyl)-α-amino esters: methyl 2-(2-bromo-3-methylbutanamido)pentanoate (1), methyl 2-(2-bromo-3-methylbutanamido)-2-phenylacetate (2) and methyl 2-(2-bromo-3-methylbutanamido)-3-phenylpropanoate (3) were synthesized. Single crystal X-

SYNTHESIS OF AN INTERMEDIATE OF AN ANTIVIRAL COMPOUND

Process for the preparation of a cyclopropylamide compound which is useful as a structural unit in a process for the preparation of a viral protease inhibitor.

Crucial role of β-elimination in determining regio- and chemoselectivity of the rhodium-catalyzed hydroformylation of N -allylpyrroles: A new approach to 5,6-dihydroindolizines

Rhodium-catalyzed hydroformylation of the chiral (S)-3-alkyl-3-pyrrol-1- ylprop-1-enes at 100 atmospheres total pressure and 25C led to the preferential formation of the branched 3-alkyl-2-methyl-3-pyrrol-1-ylpropanals. At 30 atmospheres and 125°C, the linear 4-alkyl-4-pyrrol-1-ylbutanals were obtained: these aldehydes are not the final products, but evolve into more stable 5,6-dihydroindolizines, with the same optical purity as the starting olefins, via a domino cyclization-dehydration process. According to the generally accepted mechanism for rhodium-catalyzed hydroformylation, the regioselectivity, and then the final chemoselectivity, can be rationalized by taking into account that while at room temperature no -elimination occurs, at high temperature the -elimination involves the branched rhodium-alkyl intermediate only.

QUINAZOLINEDIONE CHYMASE INHIBITORS

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

Mechanism-based inhibitors of serine proteases with high selectivity through optimization of S′ subsite binding

A series of mechanism-based inhibitors designed to interact with the S′ subsites of serine proteases was synthesized and their inhibitory activity toward the closely-related serine proteases human neutrophil elastase (HNE) and proteinase 3 (PR 3) was inve

PREPARATION AND USE OF BIPHENYL-4-YL-CARBONYLAMINO ACID DERIVATIVES FOR THE TREATMENT OF OBESITY

This invention relates to certain biphenyl-4-yl carbonylamino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.