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盐酸毛果芸香碱
Tier C · 观察 / 贸易Pilocarpine Hydrochloride
Alcon Inc
原研
1951
首批上市
-
到期年（公开口径）
无销量数据
峰值销售
化学药
类型
靶点：mAChRs
商品名：Spersacarpin、PilaSite、Pilocarpina lux、Pilobuc、Pilopine HS、Isopto-<span class="highlightText">pilocarpine</span>、Pilogel、Salagen、Isopto carpine、Pilo、Pilocar
适应症（已批准）：闭角型青光眼、高眼压、开角型青光眼、瞳孔缩小、Sjtoegren综合征、虹膜炎、口腔干燥、青光眼
各地区研发/上市状态
美国
批准上市
1974-07-29
欧盟
无进展
2015-05-01
中国
批准上市
1981-01-01
日本
批准上市
1967-02-01
合成路线与中间体5 routes
原研路线 × 0优化路线（非专利）× 5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。
优化Route 2步骤 7 · 总收率 /
(I)115092-6-a636-61-3(II)115092-6-a70681-41-3(III)115092-6-a75-03-6(IV)115092-6-a—(V)115092-6-a—(VI)115092-6-a—(VII)115092-6-a39021-62-0(VIII)115092-6-a—(IX)115092-6-a—API · 盐酸毛果芸香碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)115092-6-a | 636-61-3 | (2R)-2-Hydroxysuccinic acid |
| (II)115092-6-a | 70681-41-3 | (R)-2-Hydroxysuccinic acid dimethylester |
| (III)115092-6-a | 75-03-6在售 | 1-Iodoethane |
| (IV)115092-6-a | - | Diethyl (2S,3R)-2-methyl-3-hydroxysuccinate |
| (V)115092-6-a | - | Dimethyl (2S,3R)-2-ethyl-3-[(4-nitrobenzene-1-sulfonyl)oxy]butanedioate |
| (VI)115092-6-a | - | Dimethyl (3R)-2-bromo-3-ethylbutanedioate |
| (VII)115092-6-a | 39021-62-0 | 1-Methyl-1H-imidazole-5-carbaldehyde |
| (VIII)115092-6-a | - | Methyl (3S,4S)-4-ethyl-2-(1-methyl-1H-imidazol-5-yl)-5-oxooxolane-3-carboxylate |
| (IX)115092-6-a | - | (2S,3R)-2-Ethyl-4-methoxy-3-[(1-methyl-1H-imidazol-5-yl)methyl]-4-oxobutanoic acid |
优化Route 3步骤 4 · 总收率 /
(I)115092-7-a123-72-8(II)115092-7-a922-68-9(III)115092-7-a—(IV)115092-7-a—(V)115092-7-a—(VI)115092-7-a—API · 盐酸毛果芸香碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)115092-7-a | 123-72-8 | 1-Butanone |
| (II)115092-7-a | 922-68-9 | Glyoxylic acid methyl ester |
| (III)115092-7-a | - | Methyl (2R,3S)-3-formyl-2-hydroxypentanoate |
| (IV)115092-7-a | - | (2S,3R)-2-Ethyl-3-hydroxy-4-methoxy-4-oxobutanoic acid |
| (V)115092-7-a | - | Diethyl (2S,3R)-2-methyl-3-hydroxysuccinate |
| (VI)115092-7-a | - | Dimethyl (2S,3R)-2-ethyl-3-[(4-methylbenzene-1-sulfonyl)oxy]butanedioate |
优化Route 4步骤 4 · 总收率 /
(I)115092-8-a636-61-3(IIa)115092-8-a7554-28-1(IIb)115092-8-a83540-97-0(III)115092-8-a75-03-6(IVa)115092-8-a—(IVb)115092-8-a—(Va)115092-8-a—(Vb)115092-8-a—(VIa)115092-8-a—(VIb)115092-8-a—API · 盐酸毛果芸香碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)115092-8-a | 636-61-3 | (2R)-2-Hydroxysuccinic acid |
| (IIa)115092-8-a | 7554-28-1 | (R)-Diethyl malate |
| (IIb)115092-8-a | 83540-97-0 | (R)-Diisopropyl 2-hydroxysuccinate |
| (III)115092-8-a | 75-03-6在售 | 1-Iodoethane |
| (IVa)115092-8-a | - | Diethyl (2S,3R)-2-ethyl-3-hydroxybutanedioate |
| (IVb)115092-8-a | - | Dipropan-2-yl (2S,3R)-2-ethyl-3-hydroxybutanedioate |
| (Va)115092-8-a | - | Diethyl (2S,3R)-2-ethyl-3-[(4-nitrobenzene-1-sulfonyl)oxy]butanedioate |
| (Vb)115092-8-a | - | Dipropan-2-yl (2S,3R)-2-ethyl-3-[(4-nitrobenzene-1-sulfonyl)oxy]butanedioate |
| (VIa)115092-8-a | - | Diethyl (3R)-2-bromo-3-ethylbutanedioate |
| (VIb)115092-8-a | - | Diisopropyl 2-bromo-3(R)-ethyl-butanedioate |
优化Route 5步骤 6 · 总收率 /
(I)115092-10-a—(II)115092-10-a542-78-9(III)115092-10-a—(IV)115092-10-a—(V)115092-10-a—(VI)115092-10-a—(VII)115092-10-a—(VIII)115092-10-a—API · 盐酸毛果芸香碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)115092-10-a | - | Methyl (2S)-2-hydroxybutanoate |
| (II)115092-10-a | 542-78-9 | 1,3-Propanedial |
| (III)115092-10-a | - | Methyl (2S)-2-ethyl-3-formyl-4-oxobutanoate |
| (IV)115092-10-a | - | Methyl (2S)-2-ethyl-4-hydroxy-3-(hydroxymethyl)butanoate |
| (V)115092-10-a | - | (3S)-3-Ethyl-4-(hydroxymethyl)oxolan-2-one |
| (VI)115092-10-a | - | 5-Chloro-1-methyl-1H-imidazole |
| (VII)115092-10-a | - | (3S)-3-Ethyl-4-(1-methyl-1H-imidazole-5-carbonyl)oxolan-2-one |
| (VIII)115092-10-a | - | (3S)-3-Ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]oxolan-2-one |
RouteRoute 1步骤 10 · 总收率 150mg(Pilocarpine Nitrate (API))
Pilocarpine Nitrate-02099776-32-6Pilocarpine Nitrate-021119117-34-9Pilocarpine Nitrate-022144461-05-2Pilocarpine Nitrate-023144461-06-3Pilocarpine Nitrate-0241826-67-1Pilocarpine Nitrate-0251192231-10-9Pilocarpine Nitrate-0261192231-09-6Pilocarpine Nitrate-027144461-10-9Pilocarpine Nitrate-028144461-11-0Pilocarpine Nitrate-01374-89-5Pilocarpine Nitrate-029—Pilocarpine Nitrate-03038993-98-5API · 盐酸毛果芸香碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Pilocarpine Nitrate-020 | 99776-32-6 | 2-(2,2-Dimethoxyethyl)propane-1,3-diol |
| Pilocarpine Nitrate-021 | 119117-34-9 | 2-[(Acetyloxy)methyl]-4,4-dimethoxybutyl acetate |
| Pilocarpine Nitrate-022 | 144461-05-2 | (2R)-2-(Hydroxymethyl)-4,4-dimethoxybutyl acetate |
| Pilocarpine Nitrate-023 | 144461-06-3 | (2S)-2-Formyl-4,4-dimethoxybutyl acetate |
| Pilocarpine Nitrate-024 | 1826-67-1 | Vinylmagnesium bromide |
| Pilocarpine Nitrate-025 | 1192231-10-9 | (2S)-2-(2,2-Dimethoxyethyl)pent-4-ene-1,3-diol |
| Pilocarpine Nitrate-026 | 1192231-09-6 | (5S)-5-(2,2-Dimethoxyethyl)-4-ethenyl-1,3-dioxan-2-one |
| Pilocarpine Nitrate-027 | 144461-10-9 | (3R,4R)-4-(2,2-Dimethoxyethyl)-3-ethenyldihydrofuran-2(3H)-one |
| Pilocarpine Nitrate-028 | 144461-11-0 | [(3R,4R)-4-Ethenyl-5-oxotetrahydrofuran-3-yl]acetaldehyde |
| Pilocarpine Nitrate-013 | 74-89-5 | Methylamine |
| Pilocarpine Nitrate-029 | - | (4R)-3-Ethylidene-4-[(2E)-2-(methylimino)ethyl]dihydrofuran-2(3H)-one |
| Pilocarpine Nitrate-030 | 38993-98-5 | (3E,4R)-3-Ethylidene-4-[(1-methyl-1H-imidazol-5-yl)methyl]dihydrofuran-2(3H)-one |
常见问题（FAQ）
盐酸毛果芸香碱的适应症有哪些？
已批准的适应症包括：闭角型青光眼、高眼压、开角型青光眼、瞳孔缩小、Sjtoegren综合征、虹膜炎、口腔干燥、青光眼。
盐酸毛果芸香碱的专利什么时候到期？
盐酸毛果芸香碱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。
盐酸毛果芸香碱有几条合成路线？
本站收录 5 条合成路线，最短路线 4 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
盐酸毛果芸香碱的关键中间体在哪里可以采购？
盐酸毛果芸香碱的多条路线中间体已挂接 CAS 档案，其中 1 个 CAS 已有优贝德（Unibest）供应网络在售报价，可在本页路线表中直接查看并询价。
如何获取盐酸毛果芸香碱中间体的报价？
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） · 2026-09-27