The title compound was prepared from chloroacetic acid and elongated to dipeptides, which cyclized spontaneously upon Fmoc-deprotection to form N-allylated 2,5-diketopiperazines.
The title compound was prepared from chloroacetic acid and elongated to dipeptides, which cyclized spontaneously upon Fmoc-deprotection to form N-allylated 2,5-diketopiperazines.
Synthesis of macrocyclic analogues of the neuroprotective agent glycyl-l-prolyl-l-glutamic acid (GPE)
作者:Paul W. R. Harris、Margaret A. Brimble
DOI:10.1039/b605293b
日期:——
The syntheses of seven macrocyclic analogues of the neuroprotective tripeptide glycyl-L-prolyl-L-glutamic acid (GPE) 1 are described. Macrocycles 6 and 7 mimic the cis conformer of GPE whereas macrocycles 2–5, 8, and 9 mimic the trans conformer of GPE. The macrocyclic peptides of well-defined geometry were prepared via Grubbs ring closing metathesis of an appropriate diene precursor. In turn each of the diene precursors were prepared from the readily available allyl-substituted amino acid building blocks 12, 13, 14, 27, 36 and 51.
[EN] AN ENANTIOSELECTIVE PROCESS FOR THE SYNTHESIS OF (2S,4R)-4-HYDROXYPIPECOLIC ACID<br/>[FR] PROCÉDÉ ÉNANTIOSÉLECTIF DE SYNTHÈSE D'ACIDE (2S,4R)-4-HYDROXYPIPÉCOLIQUE
申请人:COUNCIL SCIENT IND RES
公开号:WO2016120890A1
公开(公告)日:2016-08-04
The present invention relates to an improved process for synthesis of 4-hydroxy pipecolic acid. The present invention relates to an improved enantioselective process for the synthesis of (2S,4R)-4-hydroxypipecolic acid via Co(III) (salen)-catalyzed two stereocentered Hydrolytic Kinetic Resolution (HKR) of racemic 1,3-azido epoxide with good yields and high optical purity without any protecting groups. 10 31
The invention provides nanoparticles, methods for making nanoparticles, and methods for using nanoparticles. An important attribute of a drug delivery system is its ability to allow for spatial and temporal regulated drug release, thereby minimizing side effects and improving therapeutic efficacy of conventional pharmaceuticals. Iron oxide nanoparticles (NPs), specifically Fe304 nanoparticles, possess many appropriate qualities that make them a viable choice for drug delivery.
The novel compound 1,4-diisopropyl-2,5-diketopiperazine can be hydrolytically cleaved to prepare N-isopropylglycine, which can be reacted with formaldehyde and phosphorous acid to produce N-isopropyl-Nphosphonomethylglycine. The latter compound can be dealkylated in the presence of base to produce N-phosphonomethylglycine, a well known herbicide.