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【结 构 式】 
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【分子编号】65824 【品名】9-Iodominocycline 【CA登记号】 |
【 分 子 式 】C23H26IN3O7 【 分 子 量 】583.37993 【元素组成】C 47.35% H 4.49% I 21.75% N 7.2% O 19.2% |
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：(XIII)3) Iodination of minocycline (I) by treatment with N-iodosuccinimide in methanesulfonic acid gives compound (XIII) (4), which is converted to aldehyde (XIV) by palladium-catalyzed carbonylation with carbon monoxide gas in the presence of phosphine ligands and triethylsilane. Finally, aldehyde (XIV) is reductively aminated with neopentylamine (VIII) under catalytic hydrogenation conditions (5). Scheme 2.
| 【4】 Sheahan, P., Koza, D., Hawkins, P. et al. (Paratek Pharmaceuticals, Inc.; Tufts University). 9-Substituted minocycline compounds. CA 2415178, EP 1301467, EP 1679305, JP 2004502752, JP 2009029785, US 2003125348, US 6846939, WO 2002004406. |
| 【5】 Seyedi, F., Warchol, T., Grier, M. (Paratek Pharmaceuticals, Inc.). Methods for synthesizing substituted tetracycline compounds. WO 2009009042. |
| 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) | 65813 | Minocycline hydrochloride; [4S-(4alpha,4aalpha,5aalpha,12aalpha)]-4,7-Bis(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxonaphthacene-2-carboxamide monohydrochloride | 13614-98-7 | C23H27N3O7.HCl | 详情 | 详情 |
| (VIII) | 65819 | Neopentylamine; 2,2-dimethylpropan-1-amine | 5813-64-9 | C5H13N | 详情 | 详情 |
| (XIII) | 65824 | 9-Iodominocycline | C23H26IN3O7 | 详情 | 详情 | |
| (XIV) | 65825 | 9-Formylminocycline | C24H27N3O8 | 详情 | 详情 |
Extended Information