【结 构 式】 |
【分子编号】51378 【品名】 【CA登记号】 |
【 分 子 式 】C9H12Br2ClN2O5P 【 分 子 量 】454.439222 【元素组成】C 23.79% H 2.66% Br 35.17% Cl 7.8% N 6.16% O 17.6% P 6.82% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号:(V)Reduction of 5-nitro-2-furaldehyde (I) with NaBH4 provided the corresponding alcohol (II). The phosphoramidic dichloride (IV) was prepared by treatment of bis(2-bromoethyl)amine (III) with phosphorus oxychloride in the presence of triethylamine at -40 C. Condensation of acid chloride (IV) with the lithium alkoxide of (II) at -78 C produced the intermediate (V), which was treated in situ with gaseous ammonia at -20 C, yielding the title phosphorodiamidate.
【1】 Joswig, C.; Marakovits, J.T.; Liu, J.; Mulcahy, R.T.; Borch, R.F.; Schmidt, J.P.; Gipp, J.J.; Synthesis and evaluation of nitroheterocyclic phosphoramidates as hypoxia-selective alkylating agents. J Med Chem 2000, 43, 11, 2258. |
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