75001-09-1Relevant articles and documents
Preparation method of precursor raw material Pht-AEEA-AEEA for somatostatin side chain
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Paragraph 0047; 0057-0059; 0083; 0093-0095; 0119; 0129-0131, (2021/10/05)
The preparation method comprises the following steps: in the reaction kettle, adding AEEA phthalic AEEA anhydride, toluene, opening stirring, heating and refluxing, separating the 100 ml water Pht through a water separator, ending the reaction, and lowering the temperature to room temperature. Post-treatment: addition of saturated NaHCO3 The solution was washed 1h. The method is scientific and reasonable in structure, safe and convenient to use, and safe and convenient to use; the product is prepared by using @timetime@ petroleum ether 1:20, AEEA-AEEA ethyl ester as a raw material, PA-AEEA - ethyl ester preparation third and deamination, and then PA ethyl ester is prepared by using the solid phase method AEEA AEEA . 4th-Pht-AEEA Ethyl AEEA -ethyl ester.
Preparation method of [2-[1-(Fmoc-amino)ethoxy]ethoxy]acetic acid
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, (2019/09/17)
The invention provides a preparation method of [2-[1-(Fmoc-amino)ethoxy]ethoxy]acetic acid. The preparation method comprises steps as follows: amino protection is performed on diglycolamine by use ofphthalic anhydride, an obtained intermediate and halo-acetic acid or halo-acetate are subjected to a reaction, deprotection or deprotection and hydrolysis are performed, a product reacts with a Fmoc-based amino protection reagent, and [2-[1-(Fmoc-amino)ethoxy]ethoxy]acetic acid is obtained. In the preparation method, phthalic anhydride and diglycolamine are taken as initial raw materials, short time is required by an amino protection reaction, an obtained intermediate compound has good stability, can be preserved for a long time and does not react with water, water-soluble impurities (such asthe raw material diglycolamine, a byproduct phthalic acid and the like) can be separated through extraction, so that an amino protection product with high purity is obtained, and the purity and the yield of the target product are also improved.
Synthesis of novel amphiphilic spin probes with the paramagnetic doxyl group in the polar region
Pajk, Stane,Pe?ar, Slavko
scheme or table, p. 659 - 665 (2009/04/07)
The use of ESR and specially designed spin probes has led to major breakthroughs in understanding the complexity of biological membranes. Research has been focused mainly on molecular events within the?lipid bilayer, and few probes have been designed for studying events in the extracellular space near the membrane surface. We have prepared a series of amphiphilic spin probes in which an ethylene glycol type hydrophilic spacer was introduced between a hydrophobic anchor and the doxyl group, placing the latter above the membrane in the extracellular space. Furthermore, the 2pπ orbital, containing the unpaired electron of the nitroxide group, would be orientated perpendicular to the membrane surface, making it more useful for ESR investigations of structural and dynamic properties close to the membrane surface in different situations of the cell life.
Synthesis of two optically active calcium channel antagonists labelled with carbon-11 for in vivo cardiac PET imaging
Dolle, Frederic,Hinnen, Francoise,Valette, Heric,Fuseau, Chantal,Duval, Raphael,Peglion, Jean-Louis,Crouzel, Christian
, p. 749 - 764 (2007/10/03)
(±)-S11568 (1, 3-ethyl-5-methyl-(±)-2-[(2-(2-aminoethoxy)ethoxy)methyl]-4-(2,3 -dichlorophenyl)-6-methyl-1,4-dihydropyridine-3,5- dicarboxylate), has an in vitro profile of high potency and of high selectivity for the low-voltage dependent L-type calcium channel. In in vitro binding studies, it displaced specifically bound (-)-[3H]PN 200-110 (isradipine (2), the reference molecule for in vitro studies) from cardiac and vascular smooth muscle preparations with potencies of 5.6 and 51 nM, respectively. It also appears as a pure pharmacological antagonist acting at a single channel L-type and free of any interaction at the benzothiazepine binding site such as amlodipine (3). Both enantiomers of S11568 have in vitro activities, the dextro isomer S12967 ((±)-1) being 6 to 18-fold less potent than the levo one S12968 ((-)-1). Two couples of optically active labelling precursors of S11568, ((-)-10/(+)-10 and (-)-14/(+)-14) have been synthesized using a modified Hantzsch's dihydropyridine synthesis. In both cases, the enantiomers were separated by preparative chiral HPLC. They both have been independently labelled with carbon-11, using [11C]diazomethane or [11C]iodomethane to give multimilliCurie quantities of (-)-1 (S12968) and (+)-1 (S12967) with high specific activities (500-1000 mCi/μmol, 18.5-37.0 GBq/μmol). Both enantiomers appear suitable for PET experiments: their myocardial concentration increases after a bolus injection to reach a maximum in 2 min and then remains on a plateau with a slight downslope while the blood concentration falls rapidly. Myocardial uptake was threefold higher than lung uptake, leading to a good contrast on PET images. The present preliminary biological results obtained in Beagle dogs showed that both enantiomers have similar myocardisk kinetics and in vivo affinity for the left ventricular myocardium.
THE SYNTHESIS OF GLYCOLIPIDS CONTAINING A HYDROPHILIC SPACER-GROUP
Slama, James,Rando, Robert R.
, p. 213 - 222 (2007/10/02)
Cholesterol-containing glycolipids incorporating a new hydrophilic specer-group, 8-amino-3,6-dioxaoctanoic acid, were synthesized.This spacer group eliminates many of the problems inherent in the use of hydrophobic or charged, spacer arms.
