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【结 构 式】

【药物名称】Coartem;Artemether;Lumefantrine

【化学名称】1-((Z)-9-(4-chlorobenzylidene)-2,7-dichloro-9H-fluoren-4-yl-2-(dibutylamino) ethanol

【CA登记号】82186-77-4

【 分 子 式 】C30H32Cl3NO

【 分 子 量 】527.15495

【开发单位】Novartis

【药理作用】  

合成路线1

 

1 Beutler U, Fuenfschilling PC, Steinkemper A. 2007. An improved manufacturing process for the antimalaria drug roartem. Part II. Organic Process Research & Development, 11(3): 341~345.
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) 67236 Fluorene;Diphenylenemethane;2,2'-Methylenebiphenyl;2,3-Benzindene;o-Biphenylenemethane;alpha-Diphenylenemethane-9H-fluorene 86-73-7 C13H10 详情 详情
(II) 67237 2,7-dichloro-9H-fluorene 7012-16-0 C13H8Cl2 详情 详情
(III) 67238 2-chloro-1-(2,7-dichloro-9H-fluoren-4-yl)ethanone   C15H9Cl3O 详情 详情
(IV) 67239 2-chloro-1-(2,7-dichloro-9H-fluoren-4-yl)ethanol   C15H11Cl3O 详情 详情
(V) 67240 2-(2,7-dichloro-9H-fluoren-4-yl)oxirane 53221-14-0 C15H10Cl2O 详情 详情
(VI) 67241 2-(dibutylamino)-1-(2,7-dichloro-9H-fluoren-4-yl)ethanol 69759-61-1 C23H29Cl2NO 详情 详情
(VII) 67242 (E)-2-(dibutylamino)-1-(2,7-dichloro-9-(4-chlorobenzylidene)-9H-fluoren-4-yl)ethanol   C30H32Cl3NO 详情 详情
(VIII) 67243 (Z)-2-(dibutylamino)-1-(2,7-dichloro-9-(4-chlorobenzylidene)-9H-fluoren-4-yl)ethanol 82186-77-4 C30H32Cl3NO 详情 详情

合成路线2

 

1 Rao DR, Kankan RN, Phull MS. 2006. Process for preparation of lumefantrine as antimalarial agent with improved method. CN 1865227.
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) 67236 Fluorene;Diphenylenemethane;2,2'-Methylenebiphenyl;2,3-Benzindene;o-Biphenylenemethane;alpha-Diphenylenemethane-9H-fluorene 86-73-7 C13H10 详情 详情
(II) 67237 2,7-dichloro-9H-fluorene 7012-16-0 C13H8Cl2 详情 详情
(III) 67238 2-chloro-1-(2,7-dichloro-9H-fluoren-4-yl)ethanone   C15H9Cl3O 详情 详情
(IV) 67240 2-(2,7-dichloro-9H-fluoren-4-yl)oxirane 53221-14-0 C15H10Cl2O 详情 详情
(V) 67244 (Z)-2-(2,7-dichloro-9-(4-chlorobenzylidene)-9H-fluoren-4-yl)oxirane   C22H13Cl3O 详情 详情
(VI) 67245 magnesium bromide dibutylamide   C8H18BrMgN 详情 详情

合成路线3

 

1 Murugesan B, Rafe M, Sathyananarayana S(Ranbaxy Laboratories Limited, India). 2007. A process for the preparation of dichlorofluorene as a key intermediate to lumefantrine. Indian Pat Appl, IN 2007DE00012.
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) 67236 Fluorene;Diphenylenemethane;2,2'-Methylenebiphenyl;2,3-Benzindene;o-Biphenylenemethane;alpha-Diphenylenemethane-9H-fluorene 86-73-7 C13H10 详情 详情
(III) 67237 2,7-dichloro-9H-fluorene 7012-16-0 C13H8Cl2 详情 详情
(IV) 67240 2-(2,7-dichloro-9H-fluoren-4-yl)oxirane 53221-14-0 C15H10Cl2O 详情 详情
(V) 33492 N,N-dibutylamine; N-butyl-1-butanamine 111-92-2 C8H19N 详情 详情
(VI) 67241 2-(dibutylamino)-1-(2,7-dichloro-9H-fluoren-4-yl)ethanol 69759-61-1 C23H29Cl2NO 详情 详情
(VII) 29029 4-chlorobenzaldehyde 104-88-1 C7H5ClO 详情 详情
(IX) 67246 sulfuryl dichloride 7791-25-5 Cl2O2S 详情 详情
Extended Information