42807-92-1

Upstream product

• 24164-05-4 methyl N-(tertbutoxycarbonyl)-N-methyl-L-isoleucinate 
• 610800-47-0 (2S,3S)-methyl 3-methyl-2-(4-nitrophenylsulphonamido)pentanoate 
• 18598-74-8 methyl L-isoleucinate hydrochloride 
• 610800-53-8 N-methyl-N-4-nitrophenylsulfonyl-L-isoleucine methyl ester 
• 67-56-1 methanol 
• 4125-98-8 N-methyl-L-isoleucine 
• 1426066-77-4 methyl N-methyl-N-benzyl-2-amino-3-methylpentanoate 
• 5619-06-7 1-methoxy-3-methyl-1-oxopentan-2-aminium chloride 

Relevant academic research and scientific papers

Asymmetric Total Synthesis of Nannocystin A

Nannocystin A is a novel 21-membered macrolactone isolated from myxobacterium Nanocystis sp. It is a potent elongation factor 1 inhibitor and inhibits cancer cell line growth at nanomolar concentrations. In this work, a concise asymmetric total synthesis of nannocystin A has been developed, which features Sharpless epoxidation, Stille coupling, and final macrolactamization.

NITROXOLINE PRODRUG AND USE THEREOF

Provided are a nitroxoline prodrug and a use thereof. Specifically, provided are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, a composition containing the compound, and a use thereof in the preparation of anti-infective and antitumor drugs, and definitions of groups in formula (I) are as stated in the specification. The compound represented by formula (I) has better pharmacokinetic parameters such as solubility, blood medicine concentration, or half-life period than nitroxoline. The compound represented by formula (I) can reduce the frequency of drug administration, and has potential for application in other fields other than the field of urinary tracts.

PRODRUG OF NITROXOLINE AND USE THEREOF

The present invention relates to the prodrug of nitroxoline and use thereof. Specifically, the present invention relates to a compound of formula (I) or the pharmaceutically acceptable salt thereof, a preparation method thereof, a pharmaceutical composition comprising the same, as well as a use thereof in anti-infective and anti-tumor drugs. The compound of formula (I) has better pharmacokinetic parameters such as water solubility, blood concentration or half-life relative to nitroxoline. The compound of formula (I) can reduce the number of administrations, and has the possibility of being applied in other fields than the urinary tract field. The definition of each group in formula (I) is as defined in the description.

Simple and efficient Fmoc removal in ionic liquid

A mild method for an efficient removal of the fluorenylmethoxycarbonyl (Fmoc) group in ionic liquid was developed. The combination of a weak base such as triethylamine and [Bmim][BF4] makes the entire system more efficient for the cleavage at room temperature of various amines and amino acid methyl esters in short reaction times. The procedure works well even in the case of N-Fmoc amino acids bearing acid-sensitive protecting groups and of N-alkylated amino acid methyl esters. The solvent-free condition provides a complementary method for Fmoc deprotection in solution phase peptide synthesis and modern organic synthesis.

"One-pot" methylation of N-nosyl-α-amino acid methyl esters with diazomethane and their coupling to prepare N-methyl dipeptides

N-Nosyl-α-amino acid methyl esters are methylated quantitatively with diazomethane. After proper deprotection of the amino function by treatment with the reagent system mercaptoacetic acid/sodium methoxide, the obtained N-methyl amino acid methyl esters are coupled with N-Fmoe amino acid chlorides to afford the corresponding dipeptides. The obtained products do not show any detectable extent of racemization by 1H NMR and HPLC.