Sophoridine derivative with nitrogen mustard as well as preparation method and application of sophoridine derivative
A definition and compound technology, applied in the field of medicinal chemistry, can solve the problems of limited anti-tumor activity of sophoridine, inability to be widely used, and strong water solubility.
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Embodiment 1
[0037] Example 1: 4-((3aR,3a1S,10aS)-2-toluenesulfonyl dodecahydropyridin[3,2,1-ij][1,6]naphthyridin-1-yl)butylbis(2 Preparation of -chloroethyl)butyl carbamate
[0038]
[0039] Step 1: Preparation of Sophoridine
[0040]
[0041] Weigh 1.0g of sophoridine, place it in 20mL of 5N potassium hydroxide aqueous solution, heat and reflux for 12h, after the reaction is completed, cool to room temperature, add 5N hydrochloric acid solution, control the pH to be less than 6, and precipitate a large amount of white solid, filter, and after the filtrate is concentrated, residual The substance was fully dissolved with methanol, and the inorganic salt was removed by filtration to obtain a methanol solution of sophoridine. After being spin-dried, the crude product of sophoridine was obtained, and then recrystallized with methanol to separate out the pure product of sophoridine. 13 C NMR (101MHz, CDCl 3 )δ 177.13, 67.62, 58.99, 53.08, 48.78, 41.72, 35.94, 34.64, 33.47, 28.38, 26.46...
Embodiment 2
[0055] Example 2: 4-((3aR,3a1S,10aS)-2-((3,4-dimethylphenyl)sulfonyl)dodecahydropyridine[3,2,1-ij][1,6] Preparation of naphthyridin-1-yl)butylbis(2-chloroethyl)butylcarbamate
[0056]
[0057] 13 C NMR (101MHz, CDCl 3 )δ159.28,139.48,136.26,134.69,131.22,131.12,125.91,66.82,66.08,60.86,53.08,48.91,47.01,41.63,40.87,36.03,31.39,29.69,28.30,26.29,24.09,23.33,23.13,20.55,19.62 .HRMS: calcd for C 28 h 43 Cl 2 N 3 O 4 S:587.2153,found:587.2153.
Embodiment 3
[0058] Example 3: 4-((3aR,3a1S,10aS)-2-((4-chlorophenyl)sulfonyl)dodecahydropyridin[3,2,1-ij][1,6]naphthyridine-1 Preparation of -yl)butyl bis(2-chloroethyl)butyl carbamate
[0059]
[0060] 13 C NMR (101MHz, CDCl 3 )δ159.28, 140.36, 139.69, 130.44, 129.52, 66.82, 66.08, 60.86, 53.08, 48.91, 47.01, 41.63, 40.87, 36.03, 31.39, 29.69, 28.30, 26.29, 24.09 for CMS. HR, 23.3 26 h 38 Cl 3 N 3 O 4 S:593.3212,found:593.3212.
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