145889-53-8

Upstream product

• 1247065-61-7 C₁₇H₂₁N₃O₃ 
• 141-78-6 ethyl acetate 
• 18942-49-9 Boc-D-Phe-OH 
• 105-36-2 ethyl bromoacetate 
• 145889-50-5 3-(2-tert-butoxycarbonylamino-1-oxo-3-phenylpropyl)-1,3-oxazolidin-2-one 
• 64-17-5 ethanol 
• 1071-46-1 hydrogen ethyl malonate 
• 13734-34-4 N-tert-butoxycarbonyl-L-phenylalanine 
• 4522-04-7 ethyl 3-phenyl-2-(N-tert-butoxycarbonyl)aminopropanoate 

Downstream Products

• 109667-69-8 (1'R,2'R)-N-<2,4-dihydroxy-4-oxo-1-(phenylmethyl)butyl>carbamic acid 1,1-dimethylethyl ester 
• 1271777-26-4 C₃₃H₄₈N₄O₇ 
• 1271777-32-2 C₂₃H₃₂N₄O₃ 
• 942120-45-8 tert-butyl N-[1-(6-oxo-1,6-dihydropyrimidin-4-yl)-2-phenylethyl]carbamate 
• 942120-47-0 1-(6-chloropyrimidin-4-yl)-2-phenylethan-1-amine 

Relevant academic research and scientific papers

Synthesis and docking studies of renin inhibitors containing ester and amide derivatives of (3S, 4S)-4-amino-hydroxy acids with S3-S3’ renin binding site

Seven novel potential renin inhibitors, having a structure based on the peptide fragment 8-13 of human angiotensinogen - a natural substrate for renin, have been designed and synthesized. All peptides were obtained by the carbodiimide method in solution and purified by chromatography on the SiO2 column. In P1-P3’ positions, they contain esters or N-alkyl amides of modified (3S, 4S)-4-amino-3-hydroxyacids. The achieved inhibitory activity IC50 was of 10-6-10-7M Inhibitory activity of the compounds was measured in vitro by high-performance liquid chromatography (HPLC) determination of lowering the concentration of substrate in the presence of renin and the potential rennin inhibitor. Their resistance to enzymatic degradation was assayed by the determination of stability against chymotrypsin activity. Their hydrophobicity evaluated as a Log P-value was calculated by a computer method. The theoretical binding affinity of thus obtained inhibitors was elaborated based on docking to the S3-S3’ pocket of the renin active site.

NOVEL MULTIFUNCTIONAL PEPTIDASE INHIBITORS, ESPECIALLY FOR MEDICAL USE

The invention relates to compounds of the general formula (1) or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formula (1) in medicine.

Novel multifunctional peptidase inhibitors, especially for medical use

The invention relates to compounds of the general formula (1) or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formula (1) in medicine.

Carbocyclic HIV protease inhibitors

The present invention is concerned with novel HIV protease Inhibitors of formula I as individual isomers, racemates, non-racemic mixtures or mixtures of diastereoisomers; wherein n, R1and R4are as described herein. The compounds of f

Facile synthesis of N-protected γ and δ-amino-β-keto-esters

The C-acylation of Meldrum's acid by protected amino acids, using isopropenyl chloroformate (IPCF) as the condensing agent, is described. The process is used to synthesize γ and δ-amino-β-keto-esters.

AN IMPROVED SYNTHESIS OF β-KETO ESTER UNITS IN DIDEMNINS, USING 2,2'-CARBONYL-BIS(3,5-DIOXO-4-METHYL-1,2,4-OXADIAZOLIDINE).

Activation of N-protected α-amino acids and O-protected α-hydroxy acids with 2,2'-carbonyl-bis(3,5-dioxo-4-methyl-1,2,4-oxadiazolidine) 6 provide a stable activated intermediate 7 suitable for the synthesis of β-keto ester 8.This activation was used in th