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【结 构 式】 
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【药物名称】NSC-619003, KRN-8602(diHCl), MX2, R-20X2(as de-morpholino analog) 【化学名称】3'-Deamino-3'-morpholino-13-deoxo-10-hydroxycarminomycin 【CA登记号】105026-50-4 【 分 子 式 】C30H35NO11 【 分 子 量 】585.61355 |
【开发单位】Kirin Brewery (Originator) 【药理作用】Antibiotics and Alkaloids, Antineoplastic Antibiotics, Brain Cancer Therapy, ONCOLYTIC DRUGS |
合成路线1
A fermentation broth of RMN-134-13 was filtered, adjusted at pH 3.4 and centrifuged. The liquid was passed through Diajon HP-20 and eluted with acetone-0.01 M HCl-KCl buffer. The luate was combined with the precipitate of the preceding centrifugation to which acetone and 28% aq. ammonia was added. After stirring for 3-4 h at 20 C the solution was adjusted at pH 7.2 with H2SO4, concentrated and extracted with CH3OH-CHCl3. After a cumbersome purification by HPLC, 13 deoxo-10-hydroxycarminomycin (oxaunomycin) (I) was obtained. Finally, the preceding compound was treated with diglycol dialdehyde (II) and sodium cyano-borohydride in CHCl3.
| 【1】 Otake, N.; Otuki, N.; Takeuchi, T.; U; Odagawa, A.; New morpholino anthrcyclines: MX, MX2 and MY5. J Antibiot 1987, 40, 7, 1058. |
| 【2】 Kawai, H.; Komeshima, N.; Mizobuchi, S.; Nakajima, S.; Odagawa, A.; Otake, N.; Tatsuta, K. (Microbial Chemistry Research Foundation); Anthracycline cpds. EP 0188293; JP 1986167696; JP 1987016495; US 4710564 . |
| 【3】 Prous, J.; Castaner, J.; MX2. Drugs Fut 1988, 13, 10, 923. |