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【结 构 式】

【分子编号】36409

【品名】(1R,2R)-2-amino-1-[4-(methylsulfonyl)phenyl]-1,3-propanediol

【CA登记号】51458-28-7

【 分 子 式 】C10H15NO4S

【 分 子 量 】245.29944

【元素组成】C 48.96% H 6.16% N 5.71% O 26.09% S 13.07%

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:(I)

The D-(threo)-1-p-substituted-phenyl-2-dichloroacetamido-3-fluoro-1-propanol derivatives were prepared according to the following reaction sequence: The amino group of (I) was protected with phthalicanhydride (II), followed by substitution of the primary hydroxy group with diethylamine - sulfur-trifluoride to (III), deprotection with hydrazine to the amine (IV) and acetylation with methyldichloro-acetate (B) to the target compounds.

1 Kwung-ping Fu; SCH-24893 and SCH-25298. Drugs Fut 1982, 7, 3, 172.
2 Nagabhushan, T.L.; et al.; EP 0800820 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(A) 11900 2-Benzofuran-1,3-dione;1,2-Benzenedicarboxylic Anhydride;1,2-BENZENE DICARBOXYLIC ACID ANHYDRIDE;1,2-BENZENEDICARBONIC ACID, ANHYDRIDE;1,3-DIOXOPHTHALAN;1,3-ISOBENZOFURANDIONE;o-phthalic anhydride; Phthalic anhydride 85-44-9 C8H4O3 详情 详情
(B) 36413 methyl 2,2-dichloroacetate 116-54-1 C3H4Cl2O2 详情 详情
(I) 36409 (1R,2R)-2-amino-1-[4-(methylsulfonyl)phenyl]-1,3-propanediol 51458-28-7 C10H15NO4S 详情 详情
(II) 36410 2-[(1R,2R)-2-hydroxy-1-(hydroxymethyl)-2-[4-(methylsulfonyl)phenyl]ethyl]-1H-isoindole-1,3(2H)-dione C18H17NO6S 详情 详情
(III) 36411 2-[(1S,2R)-1-(fluoromethyl)-2-hydroxy-2-[4-(methylsulfonyl)phenyl]ethyl]-1H-isoindole-1,3(2H)-dione C18H16FNO5S 详情 详情
(IV) 36412 (1R,2S)-2-amino-3-fluoro-1-[4-(methylsulfonyl)phenyl]-1-propanol C10H14FNO3S 详情 详情
Extended Information