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【结 构 式】 
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【分子编号】40487 【品名】(1R,4S,5R,6S)-5,6-dihydroxy-2-azabicyclo[2.2.1]heptan-3-one 【CA登记号】 |
【 分 子 式 】C6H9NO3 【 分 子 量 】143.1424 【元素组成】C 50.35% H 6.34% N 9.79% O 33.53% |
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：(VIII)Reaction of 5,6-dihydroxy-2-azabicyclo[2.2.1]heptan-3-one (VIII) with 2,2-dimethoxypropane (A) and TsOH in acetone gives the acetonide (IX), which is treated with ethylamine at 140 C, followed by optical resolution with di-O-benzoyl-D-tartaric acid, yielding the chiral cyclopentanecarboxamide (IV).
| 【1】 Martín, L.; Leeson, P.A.; Castañer, J.; Sorbera, L.A.; AMP-579. Drugs Fut 2000, 25, 9, 900. |
| 【2】 Spada, A.P.; Fink, C.A.; Myers, M.R. (Aventis Pharma SA); Cpds. having antihypertensive, cardioprotective, a. EP 0758897; EP 1006115; JP 1997512020; US 5561134; WO 9528160 . |
| 【3】 Spada, A.P.; Fink, C.A.; Myers, M.R. (Aventis Pharma SA); Cpds. having antihypertensive and anti-ischemic pr. EP 0550631; JP 1993508864; US 5217982; US 5364862; WO 9205177 . |
| 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) | 10722 | 1-Methoxy-1-methylethyl methyl ether; 2,2-Dimethoxypropane | 77-76-9 | C5H12O2 | 详情 | 详情 |
| (IV) | 23850 | (3aR,4S,6R,6aS)-6-amino-N-ethyl-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxole-4-carboxamide | C11H20N2O3 | 详情 | 详情 | |
| (VIII) | 40487 | (1R,4S,5R,6S)-5,6-dihydroxy-2-azabicyclo[2.2.1]heptan-3-one | C6H9NO3 | 详情 | 详情 | |
| (IX) | 40488 | (1S,2R,6S,7R)-4,4-dimethyl-3,5-dioxa-8-azatricyclo[5.2.1.0(2,6)]decan-9-one | C9H13NO3 | 详情 | 详情 |
Extended Information