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【结 构 式】

【分子编号】48262

【品名】5-ethyl 3-methyl 4-(2-chlorophenyl)-2-methyl-6-[[2-(tritylamino)ethoxy]methyl]-1,4-dihydro-3,5-pyridinedicarboxylate

【CA登记号】

【 分 子 式 】C39H39ClN2O5

【 分 子 量 】651.20184

【元素组成】C 71.93% H 6.04% Cl 5.44% N 4.3% O 12.28%

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:(VIII)

The protection of ethanolamine (I) with trityl chloride (II) in isopropanol gives N-tritylethanolamine (III), which is condensed with ethyl 4-chloroacetoacetate (IV) by means of NaH in THF to yield ethyl 4-[2-(tritylamino)ethoxy]acetoacetate (V). The cyclization of (V) with 2-chlorobenzaldehyde (VI) and methyl 3-aminocrotonate (VII) in refluxing methanol affords the protected dihydropyridine (VIII), which, without isolation, is finally detritylated by a treatment with aqueous benzenesulfonic acid.

1 Furlan, B.; Copar, A.; Jeriha, A. (LEK Pharmaceutical and Chemical Co.); 3-Ethyl 5-methyl (+)2-[2-(N-tritylamino)ethoxymethyl]-4-(2-chloro-phenyl)-1,4-dihydro-6-methyl-6-methyl-3, 5-pyridinedicarboxylate. EP 0599220; US 5389654 .
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) 10259 Ethanol amine;Ethanolamine;2-Aminoethanol; 2-Amino-1-ethanol;2-Aminoethyl alcohol 141-43-5 C2H7NO 详情 详情
(II) 48259 1-(2-chloro-1,1-diphenylethyl)benzene C20H17Cl 详情 详情
(III) 48260 2-(tritylamino)-1-ethanol C21H21NO 详情 详情
(IV) 23541 ethyl 4-chloro-3-oxobutanoate;Ethyl 4-chloro-3-oxobutanoate;Ethyl 4-chloroacetoacetate 638-07-3 C6H9ClO3 详情 详情
(V) 48261 ethyl 3-oxo-4-[2-(tritylamino)ethoxy]butanoate C27H29NO4 详情 详情
(VI) 24114 2-chlorobenzaldehyde 89-98-5 C7H5ClO 详情 详情
(VII) 11372 Methyl (E)-3-amino-2-butenoate; Methyl 3-aminocrotonate C5H9NO2 详情 详情
(VIII) 48262 5-ethyl 3-methyl 4-(2-chlorophenyl)-2-methyl-6-[[2-(tritylamino)ethoxy]methyl]-1,4-dihydro-3,5-pyridinedicarboxylate C39H39ClN2O5 详情 详情

合成路线2

该中间体在本合成路线中的序号:(IV)

 

1 潘仙华,毛海舫.氨氯地平苯磺酸盐的制备方法:CN,Patent 1,927,837,2007.
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) 48261 ethyl 3-oxo-4-[2-(tritylamino)ethoxy]butanoate C27H29NO4 详情 详情
(II) 69572 (E)-ethyl 3-amino-4-(2-(tritylamino)ethoxy)but-2-enoate C27H30N2O3 详情 详情
(III) 44034 methyl (Z)-2-acetyl-3-(2-chlorophenyl)-2-propenoate C12H11ClO3 详情 详情
(IV) 48262 5-ethyl 3-methyl 4-(2-chlorophenyl)-2-methyl-6-[[2-(tritylamino)ethoxy]methyl]-1,4-dihydro-3,5-pyridinedicarboxylate C39H39ClN2O5 详情 详情
(V) 69570 Benzenesulfonic acid;Phenylsulfonic acid;Benzenemonosulfonic acid;Benzensulfonic acid;Benzenesulphonic acid; 98-11-3 C6H6O3S 详情 详情
Extended Information