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【结 构 式】 
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【药物名称】 【化学名称】2-(2-Aminoethyl)-5-[2-(dimethylamino9ethylamino]indazolo[4,3-gh]isoquinolin-6(2H)-one 【CA登记号】 【 分 子 式 】C19H22N6O 【 分 子 量 】350.42679 |
【开发单位】Roche (Originator), University of Vermont (Originator) 【药理作用】ONCOLYTIC DRUGS |
合成路线1
The cyclization of 9-fluoro-6-(tosyloxy)-5,10-dihydrobenzo[g]isoquinoline-5,10-dione (I) with 2-aminoethylhydrazine (II) gives 2-(2-aminoethyl)-5-(tosyloxy)indazolo[4,3-gh] isoquinolin-6(2H)-one (III), which is finally condensed with N,N-dimethylethylene-1,2-diamine (IV) to afford the title compound.
| 【1】 Gallagher, C.E.; Maresch, M.J.; Krapcho, A.P.; et al.; 6,9-Disubstituted benz[g]isoquinoline-5,10-diones, key intermediates for the synthesis of antitumor 2,5-disubstituted-indazolo[4,3-gh]isoquinoline-6(2H)-ones (9-aza-anthrapyrazoles). 25th Natl Med Chem Symp (June 18, Univ. Michigan, Ann Arbor) 1996, Abst. 15. |
| 【2】 Menta, E.; et al.; Synthesis and antitumor evalution of 2, 5-disubstituted-indazolo[4, 3-gh]isoquinoline-6(2H)-ones (9-aza-anthrapyrazoles). 211th ACS Natl Meet (March 24-28, New Orleans) 1996, Abst MEDI 076. |
| 【3】 Krapcho, A.P.; Menta, E.; Antitumor aza-anthrapyrazoles. Drugs Fut 1997, 22, 6, 641. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 41185 | 9-fluoro-5,10-dioxo-5,10-dihydrobenzo[g]isoquinolin-6-yl 4-methylbenzenesulfonate | C20H12FNO5S | 详情 | 详情 | |
| (II) | 41188 | 2-hydrazinoethylamine; 2-hydrazino-1-ethanamine | C2H9N3 | 详情 | 详情 | |
| (III) | 41189 | 2-(2-aminoethyl)-6-oxo-2,6-dihydroindazolo[4,3-gh]isoquinolin-5-yl 4-methylbenzenesulfonate | C22H18N4O4S | 详情 | 详情 | |
| (IV) | 14481 | (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carbothioic S-acid | C21H26F2O4S | 详情 | 详情 |
Extended Information