- Simplified syntheses of the water-soluble chiral shift reagents Sm-(R)-pdta and Sm-(S)-pdta
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The chiral shift reagents Sm-(R)-pdta and Sm-(S)-pdta, which are based on (R)- or (S)-1,2-diaminopropane-N,N,N′,N′-tetraacetic acid were synthesized from easily accessible compounds in three simple steps, which makes the method suitable for laboratory-scale production. In addition, a new and efficient method for the preparation of pure anhydrous (R)- or (S)-1,2-diaminopropane-N,N,N′,N′-tetraacetic acid was developed.
- Hrubá, Lucie,Budě?ínsky, Milo?,Pícha, Jan,Jirá?ek, Ji?í,Vaněk, Václav
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- Dexrazoxane preparation method
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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.
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Paragraph 0016; 0018; 0020; 0022
(2019/07/04)
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- Novel Method for Producing 4,4-(1-Methyl-1,2-Ethanediyl)-BIS-(2,6-Piperazinedione)
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A method for preparing compounds of the formula (I) by the cyclization of tetraacetic acid alkyl esters of the formula (II) in the presence of ammonia and formamide as well as to the compounds of the formula (II), which are used in this method.
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Page/Page column 5
(2010/06/22)
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