24613-06-7Relevant articles and documents
Preparation method of dexrazoxane
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Paragraph 0026-0028, (2021/11/14)
The invention aims to provide a simple and efficient preparation method of dexrazoxane. According to the present invention, 1, 2-propane diamine is adopted as an initial raw material, splitting is performed to obtain hydrochloride of (S)-1, 2-propane diamine, the hydrochloride and bromoacetate are subjected to condensation to prepare (S)-1, 2-diaminopropane-tetraacetate, amide is adopted as an ammonia source, and dexrazoxane is finally prepared. The method has advantages of high yield, mild reaction conditions, easy operation and less environmental pollution, and is beneficial to large-scale industrial production.
Dexrazoxane preparation method
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Paragraph 0016; 0019; 0020; 0023, (2019/07/04)
The invention belongs to the field of drug synthesis, and provides a completely-new dexrazoxane preparation method, which comprises: carrying out a reaction on (S)-1,2-propanediamine ditartrate splitby using inexpensive and easily-available (+/-)-1,2-propanediamine as a starting raw material and using D-(-)-tartaric acid as a splitting agent and potassium chloride to obtain (S)-1,2-propanediaminedihydrochloride, carrying out condensation on the (S)-1,2-propanediamine dihydrochloride and chloroacetic acid to prepare (S)-N,N,N',N'-1,2-propanediaminetetraacetic acid, and finally carrying out cyclization to obtain dexrazoxane, wherein the total yield is 38.3%. According to the present invention, the route has advantages of simple reaction step, convenient post-treatment, no requirement of column chromatography separation, good product quality and the like.
Synthesis of chiral carbosilane dendrimers with L-cysteine and N-acetyl-L-cysteine on their surface and their application as chiral selectors for enantiomer separation by capillary electrophoresis
Quintana, Sara,García, María ángeles,Marina, María Luisa,Gómez, Rafael,de la Mata, F. Javier,Ortega, Paula
, p. 1797 - 1802 (2017/11/16)
The synthesis of chiral carbosilane dendrimers functionalized with cysteine and N-acetylcysteine groups is presented. These dendrimers were obtained through thiol–ene addition reactions and their application as chiral selectors in capillary electrophoresis was investigated. Four drugs used as model compounds were analyzed under different experimental conditions observing that the use of a first generation dendrimer containing 4 terminal N-acetyl-L-cysteine groups enabled the enantiomeric discrimination of razoxane with a discrimination power similar to that obtained with other powerful chiral selectors such as cyclodextrins.