A kind of peganumine A alkaloid structure simplification and its application
A technology of simplified substances and alkaloids, applied in the field of medicine, can solve the problems of further improvement of anti-tumor activity, limited sources of alkaloids, and high difficulty of total synthesis, and achieve simple chemical synthesis routes, easy synthesis methods, and excellent druggability Effect
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Embodiment 1
[0038] Synthesis of compound I-1
[0039]
[0040] The first step, the preparation of intermediate 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-1-carboxylic acid (compound 3)
[0041] According to the method reported in the literature (Organic Letters, 2014, 16, 4194-4197), in 50 ml of water, add tryptamine, compound 1 (1.0 g, 6.24 mM) and glyoxylic acid, compound 2 (0.47 g, 6.3 mM ), stirring and reacting at room temperature for 2 hours, a white precipitate was obtained, which was filtered by suction and dried in vacuo to obtain compound 3, 1.05 g of a white solid, with a yield of 77.8%.
[0042] The second step, the preparation of intermediate 6,7-dimethoxy-3,4-dihydroisoquinoline (compound 5)
[0043]
[0044] In 2 ml DMSO, add 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline, compound 4 (0.1 g, 0.52 mM) and 2-iodobenzoic acid (IBX, 0.15 g, 0.52 mM), react in DMSO at room temperature for 1 hour. After the reaction was complete, add saturated NaCl to wash with water, extra...
Embodiment 2
[0049] It was prepared according to the method steps of Example 1, the raw material of the first step was changed to compound 6, and the second and third steps were prepared according to the method of Example 1.
[0050]
[0051] Compound I-2 was obtained as a white solid 28 mg, with a yield of 27%.
Embodiment 3
[0053] It was prepared according to the method steps of Example 1, the raw material of the first step was changed to compound 8, and the second and third steps were prepared according to the method of Example 1.
[0054]
[0055] Compound I-3 was obtained as a white solid 45 mg with a yield of 45%.
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