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米加司他盐酸盐
Tier C · 观察 / 贸易Migalastat Hydrochloride
Amicus Therapeutics Inc
原研
2016
首批上市
-
到期年（公开口径）
$0.52B ▲
峰值销售
化学药
类型
靶点：α-Gal A
商品名：Galafold、Amigal
适应症（已批准）：法布里病
各地区研发/上市状态
美国
批准上市
2018-08-10
欧盟
批准上市
2016-05-25
中国
-
日本
批准上市
2018-03-23
合成路线与中间体5 routes
原研路线 × 1优化路线（非专利）× 4工艺路线 × 0
路线按「原研路线 → 优化路线 / 工艺路线（非专利）」排序。每条路线附本站自绘的路线流程图（中间体 → 原料药）与中间体表（编号 / CAS / 英文名），可直接用于供应商开发与询价。流程图由本站依据已授权的结构化数据自行渲染，未使用任何第三方路线图。
原研Route 1步骤 15 · 总收率 80 mg
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| MIGA-001 | 350255-13-9 | (3aR,5S,6S,6aR)-5-((S)-2,2-dimethyl-1,3-dioxolan-4-yl)-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxol-6-ol |
| MIGA-002 | 26597-73-9 | (3aR,5R,6aS)-5-((S)-2,2-dimethyl-1,3-dioxolan-4-yl)-2,2-dimethyldihydrofuro[2,3-d][1,3]dioxol-6(3aH)-one |
| MIGA-003 | 1260634-96-5 | (3aR,6aR)-5-(2,2-dimethyl-1,3-dioxolan-4-yl)-2,2-dimethyl-3a,6a-dihydrofuro[2,3-d][1,3]dioxol-6-yl acetate |
| MIGA-004 | 26775-14-4 | (3aR,5S,6R,6aR)-5-((R)-2,2-dimethyl-1,3-dioxolan-4-yl)-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxol-6-yl acetate |
| MIGA-005 | 19131-06-7 | (3aR,5S,6R,6aR)-5-((R)-2,2-dimethyl-1,3-dioxolan-4-yl)-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxol-6-yl 4-methylbenzenesulfonate |
| MIGA-006 | 38166-65-3 | (3aR,5S,6S,6aR)-5-((R)-2,2-dimethyl-1,3-dioxolan-4-yl)-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxol-6-yl acetate |
| MIGA-007 | 109680-96-8 | (3aR,5S,6S,6aR)-5-((R)-1,2-dihydroxyethyl)-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxol-6-yl acetate |
| MIGA-008 | 864442-71-7 | - |
| MIGA-009 | 109680-98-0 | - |
| MIGA-010 | 109680-99-1 | - |
| MIGA-011 | 109681-01-8 | - |
| MIGA-012 | - | (3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)piperidin-1-ium-2-sulfonate |
| MIGA-013 | 107537-94-0 | (3R,4S,5S,6R)-6-(hydroxymethyl)piperidine-2,3,4,5-tetraol |
优化Route 2步骤 8 · 总收率 39 mg
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| MIGA-014 | 95715-87-0 | tert-butyl (R)-4-formyl-2,2-dimethyloxazolidine-3-carboxylate |
| MIGA-015 | 114301-35-8 | (R)-tert-butyl 4-((R)-1-hydroxyallyl)-2,2-dimethyloxazolidine-3-carboxylate |
| MIGA-016 | 89985-72-8 | tert-butyl ((4R,5R)-2,2-dimethyl-4-vinyl-1,3-dioxan-5-yl)carbamate |
| MIGA-017 | 556-56-9 | 3-iodoprop-1-ene |
| MIGA-018 | 577969-74-5 | tert-butyl allyl((4R,5R)-2,2-dimethyl-4-vinyl-1,3-dioxan-5-yl)carbamate |
| MIGA-019 | 577969-73-4 | (4aR,8aR)-tert-butyl 2,2-dimethyl-6,8a-dihydro-4H-[1,3]dioxino[5,4-b]pyridine-5(4aH)-carboxylate |
| MIGA-020 | 577969-76-7 | (5R,6R)-tert-butyl 5-hydroxy-6-(hydroxymethyl)-5,6-dihydropyridine-1(2H)-carboxylate |
| MIGA-021 | 577969-77-8 | (4aR,6aR,7aR,7bS)-tert-butyl 2,2-dimethyltetrahydro-4H-[1,3]dioxino[5,4-b]oxireno[2,3-d]pyridine-5(4aH)-carboxylate |
优化Route 3步骤 4 · 总收率 10.5 mg
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| MIGA-022 | 106192-66-9 | (2R,3R,4S,5R)-2-azido-6-methylenetetrahydro-2H-pyran-3,4,5-triyl triacetate |
| MIGA-023 | - | (3R,4R,5R,6R)-2-(acetoxymethyl)-6-azido-2-methoxytetrahydro-2H-pyran-3,4,5-triyl triacetate |
| MIGA-024 | - | (3R,4R,5R,6R)-6-azido-2-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3,4,5-triol |
| MIGA-025 | 135395-59-4 | (2R,3R,4S,5R)-2-(hydroxymethyl)piperidine-3,4,5-triol |
优化Route 4步骤 5 · 总收率 1.35 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| MIGA-026 | 41847-60-3 | (3R,4R,5S)-2-(hydroxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetraol |
| MIGA-027 | 151377-80-9 | ((3a'R,4S,6'S,6a'R)-2,2,2',2'-tetramethyldihydro-3a'H-spiro[[1,3]dioxolane-4,4'-furo[3,4-d][1,3]dioxol]-6'-yl)methanol |
| MIGA-028 | 1314231-77-0 | ((3a'R,4S,6'S,6a'R)-2,2,2',2'-tetramethyldihydro-3a'H-spiro[[1,3]dioxolane-4,4'-furo[3,4-d][1,3]dioxol]-6'-yl)methyl trifluoromethanesulfonate |
| MIGA-029 | 151252-15-2 | (3a'R,4S,6'S,6a'R)-6'-(azidomethyl)-2,2,2',2'-tetramethyldihydro-3a'H-spiro[[1,3]dioxolane-4,4'-furo[3,4-d][1,3]dioxole] |
| MIGA-030 | 1314231-78-1 | (2R,3R,4S,5S)-5-(azidomethyl)-2-(hydroxymethyl)tetrahydrofuran-2,3,4-triol |
优化Route 5步骤 11 · 总收率 158 mg
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| MIGA-031 | 147959-19-1 | (S)-tert-butyl 2,2-dimethyl-4-(2-oxoethyl)oxazolidine-3-carboxylate |
| MIGA-032 | 1704372-29-1 | (R)-tert-butyl 4-((R,E)-4-ethoxy-1-hydroxy-4-oxobut-2-en-1-yl)-2,2-dimethyloxazolidine-3-carboxylate |
| MIGA-033 | 1704372-31-5 | (R)-tert-butyl 4-((R,E)-1-(benzyloxy)-4-ethoxy-4-oxobut-2-en-1-yl)-2,2-dimethyloxazolidine-3-carboxylate |
| MIGA-034 | 1704372-34-8 | (R)-tert-butyl 4-((1S,2R,3R)-1-(benzyloxy)-4-ethoxy-2,3-dihydroxy-4-oxobutyl)-2,2-dimethyloxazolidine-3-carboxylate |
| MIGA-035 | 1704372-37-1 | (R)-tert-butyl 4-((S)-(benzyloxy)((4S,5R)-5-(ethoxycarbonyl)-2,2-dimethyl-1,3-dioxolan-4-yl)methyl)-2,2-dimethyloxazolidine-3-carboxylate |
| MIGA-036 | 1704372-38-2 | (R)-tert-butyl 4-((S)-(benzyloxy)((4S,5S)-5-(hydroxymethyl)-2,2-dimethyl-1,3-dioxolan-4-yl)methyl)-2,2-dimethyloxazolidine-3-carboxylate |
| MIGA-037 | 1704372-41-7 | (R)-tert-butyl 4-((S)-(benzyloxy)((4S,5S)-2,2-dimethyl-5-(((methylsulfonyl)oxy)methyl)-1,3-dioxolan-4-yl)methyl)-2,2-dimethyloxazolidine-3-carboxylate |
| MIGA-038 | 1704372-47-3 | (3S,4R,5S,6R)-5-(benzyloxy)-6-(hydroxymethyl)piperidine-3,4-diol |
常见问题（FAQ）
米加司他盐酸盐的适应症有哪些？
已批准的适应症包括：法布里病。
米加司他盐酸盐的专利什么时候到期？
米加司他盐酸盐的专利到期年暂无公开口径，本页会在数据管道核实后更新。
米加司他盐酸盐有几条合成路线？
本站收录 5 条合成路线，最短路线 4 步、总收率 10.5 mg。每条路线的中间体均带登记编号与 CAS 号。
米加司他盐酸盐的关键中间体在哪里可以采购？
米加司他盐酸盐路线中的中间体均已建立 CAS 档案，可直接按 CAS 发起询价，需求会进入供应网络撮合池。
如何获取米加司他盐酸盐中间体的报价？
在本页选择目标中间体的 CAS 进入档案页，或在询价页直接提交需求；CAS 会自动带入供需撮合流程，由供应网络反馈报价。
数据来源：多源数据交叉核实（仅结构化字段） · 2026-09-24