53856-93-2Relevant articles and documents
Radiochemical Synthesis and Evaluation of 13N-Labeled 5-Aminolevulinic Acid for PET Imaging of Gliomas
Pippin, Adam B.,Voll, Ronald J.,Li, Yuancheng,Wu, Hui,Mao, Hui,Goodman, Mark M.
, p. 1236 - 1240 (2017)
The endogenous amino acid, 5-aminolevulinic acid (5-ALA), has received significant attention as an imaging agent, including ongoing clinical trials for image-guided tumor resection due to its selective uptake and subsequent accumulation of the fluorescent protoporphyrin IX in tumor cells. Based on the widely reported selectivity of 5-ALA, a new positron emission tomography imaging probe was developed by reacting methyl 5-bromolevulinate with [13N] ammonia. The radiotracer, [13N] 5-ALA, was produced in high radiochemical yield (65%) in 10 min and could be purified using only solid phase cartridges. In vivo testing in rats bearing intracranial 9L glioblastoma showed peak tumor uptake occurred within 10 min of radiotracer administration. Immunohistochemical staining and fluorescent imaging was used to confirm the tumor location and accumulation of the tracer seen from the PET images. The quick synthesis and rapid tumor specific uptake of [13N] 5-ALA makes it a potential novel clinical applicable radiotracer for detecting and monitoring tumors noninvasively.
Synthesis and characterization of altaicadispirolactone
Zhang, Yan,Wu, Linbo,Li, Feng,Li, Bo-Geng
, p. 2729 - 2733 (2005)
Altaicadispirolactone was synthesized via a simple route. In this route, levulinic acid was used as a starting material, and bromination followed by hydrolysis and BF3·OEt2-catalyzed cyclization were carried out. A single-crystal ORTEP drawing has been created and more detailed crystallographic data of the compound has been obtained from X-ray analysis. Copyright Taylor & Francis, Inc.
N-(1H-IMIDAZOL-2-YL)BENZAMIDE COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME AS ACTIVE INGREDIENT
-
Page/Page column 43; 45; 152; 159, (2021/04/10)
N-(1H-imidazol-2-yl)benzamide compound of formula (I), or a pharmaceutically acceptable salt, a prodrug, a solvate, or a stereoisomer thereof which is a novel compound exhibiting excellent inhibitory activity against IRAK-4, can be used without side effects for efficient prevention and treatment of diseases mediated by IRAK-4 receptors, particularly autoimmune diseases or lymphomas.
DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES
-
Page/Page column 61-62, (2020/01/24)
The application describes dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.
Method for manufacturing methyl 5-bromolevulinate and manufacturing method 5-aminolevulinic acid heyl ester hydrochloride using the same
-
Paragraph 0019-0021, (2019/02/28)
The present invention relates to a method of preparing methyl 5-bromolevulinate, capable of improving the yield of a final product while having stability of a product, and a method of preparing 5-aminoalkylenic acid hexyl ester hydrochloride using the same. To this end, the method of preparing methyl 5-bromolevulinate comprises: a first reaction step of mixing levulinic acid, methanol and bromine in a container and making the mixture react; a second reaction step of mixing a first product of the first reaction step, a first reactant not reacting in the first reaction step, ultrapure water and chloroform solution, and making the mixture react; an extraction step of extracting a chloroform solution layer from a first mixture formed after the second reaction step; a third reaction step of mixing the chloroform solution layer extracted in the extraction step, ethyl ether, and sodium bicarbonate saturated aqueous solution and stirring the mixture; a purification step of separating an aqueous solution layer from a second mixture formed after the third reaction step; a fourth reaction step of mixing a remaining mixture after the aqueous solution layer is separated from the second mixture with N-Hexane, and making the mixture react; a precipitation step of precipitating methyl 5-bromolevulinate in a solid state from a third mixture while quenching the third mixture formed after the fourth reaction step; and a filtering step of filtering the methyl 5-bromolevulinate in the solid state from a fourth mixture formed after the precipitation step by using a filtration device.COPYRIGHT KIPO 2019
