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【结 构 式】

【分子编号】52394

【品名】[5-(2,3-bis{[(1,1-dimethylethyl)(dimethyl)silyl]oxy}propyl)-2-[(6-{2-[5-(3-hydroxypropyl)-3-methylidenetetrahydro-2-furanyl]ethyl}-4-methyl-3-methylidenetetrahydro-2H-pyran-2-yl)methyl]-4-(methyloxy)tetrahydro-3-furanyl]methyl 4-methylbenzenesulfonate

【CA登记号】

【 分 子 式 】C46H80O10SSi2

【 分 子 量 】881.3722

【元素组成】C 62.69% H 9.15% O 18.15% S 3.64% Si 6.37%

与该中间体有关的原料药合成路线共 2 条

合成路线1

该中间体在本合成路线中的序号:(XXXI)

Alcohol (XXIX) was converted to the corresponding tosylate (XXX) employing p-toluenesulfonyl chloride and pyridine. Replacement of the pivaloyl protecting group of (XXX) for a mono-methoxytrityl group, yielding (XXXII), was effected by reductive cleavage of the pivaloyl ester of (XXX) and then treatment of alcohol (XXXI) with methoxytrityl chloride. Displacement of the tosylate group of (XXXII) by NaI in refluxing acetone provided the alkyl iodide (XXXIII).

1 Littlefield, B.A.; Zheng, W.; Seletsky, B.M.; Yu, M.J.; Palme, M.H.; Towle, M.J. (Eisai Co., Ltd.); Macrocyclic analogs and methods of their use and preparation. US 6214865; WO 9965894 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(XXIX) 52392 3-{5-[2-(6-{[5-(2,3-bis{[(1,1-dimethylethyl)(dimethyl)silyl]oxy}propyl)-3-(hydroxymethyl)-4-(methyloxy)tetrahydro-2-furanyl]methyl}-4-methyl-5-methylidenetetrahydro-2H-pyran-2-yl)ethyl]-4-methylidenetetrahydro-2-furanyl}propyl 2,2-dimethylpropanoate C44H82O9Si2 详情 详情
(XXX) 52393 3-{(2S,5S)-5-[2-((2S,4R,6R)-6-{[(2S,3R,4R,5R)-5-((2S)-2,3-bis{[tert-butyl(dimethyl)silyl]oxy}propyl)-4-methoxy-3-({[(4-methylphenyl)sulfonyl]oxy}methyl)tetrahydro-2-furanyl]methyl}-4-methyl-5-methylenetetrahydro-2H-pyran-2-yl)ethyl]-4-methylenetetrahydro-2-furanyl}propyl 2,2-dimethylpropanoate C51H88O11SSi2 详情 详情
(XXXI) 52394 [5-(2,3-bis{[(1,1-dimethylethyl)(dimethyl)silyl]oxy}propyl)-2-[(6-{2-[5-(3-hydroxypropyl)-3-methylidenetetrahydro-2-furanyl]ethyl}-4-methyl-3-methylidenetetrahydro-2H-pyran-2-yl)methyl]-4-(methyloxy)tetrahydro-3-furanyl]methyl 4-methylbenzenesulfonate C46H80O10SSi2 详情 详情
(XXXII) 52395   C66H96O11SSi2 详情 详情
(XXXIII) 52396   C59H89IO8Si2 详情 详情

合成路线2

该中间体在本合成路线中的序号:(XXXI)

Alcohol (XXIX) was converted to the corresponding tosylate (XXX) employing p-toluenesulfonyl chloride and pyridine. Replacement of the pivaloyl protecting group of (XXX) for a mono-methoxytrityl group, yielding (XXXII), was effected by reductive cleavage of the pivaloyl ester of (XXX) and then treatment of alcohol (XXXI) with methoxytrityl chloride. Displacement of the tosylate group of (XXXII) by NaI in refluxing acetone provided the alkyl iodide (XXXIII).

1 Littlefield, B.A.; Zheng, W.; Seletsky, B.M.; Yu, M.J.; Palme, M.H.; Towle, M.J. (Eisai Co., Ltd.); Macrocyclic analogs and methods of their use and preparation. US 6214865; WO 9965894 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(XXIX) 52392 3-{5-[2-(6-{[5-(2,3-bis{[(1,1-dimethylethyl)(dimethyl)silyl]oxy}propyl)-3-(hydroxymethyl)-4-(methyloxy)tetrahydro-2-furanyl]methyl}-4-methyl-5-methylidenetetrahydro-2H-pyran-2-yl)ethyl]-4-methylidenetetrahydro-2-furanyl}propyl 2,2-dimethylpropanoate C44H82O9Si2 详情 详情
(XXX) 52393 3-{(2S,5S)-5-[2-((2S,4R,6R)-6-{[(2S,3R,4R,5R)-5-((2S)-2,3-bis{[tert-butyl(dimethyl)silyl]oxy}propyl)-4-methoxy-3-({[(4-methylphenyl)sulfonyl]oxy}methyl)tetrahydro-2-furanyl]methyl}-4-methyl-5-methylenetetrahydro-2H-pyran-2-yl)ethyl]-4-methylenetetrahydro-2-furanyl}propyl 2,2-dimethylpropanoate C51H88O11SSi2 详情 详情
(XXXI) 52394 [5-(2,3-bis{[(1,1-dimethylethyl)(dimethyl)silyl]oxy}propyl)-2-[(6-{2-[5-(3-hydroxypropyl)-3-methylidenetetrahydro-2-furanyl]ethyl}-4-methyl-3-methylidenetetrahydro-2H-pyran-2-yl)methyl]-4-(methyloxy)tetrahydro-3-furanyl]methyl 4-methylbenzenesulfonate C46H80O10SSi2 详情 详情
(XXXII) 52395   C66H96O11SSi2 详情 详情
(XXXIII) 52396   C59H89IO8Si2 详情 详情
Extended Information