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河豚毒素
Tier C · 观察 / 贸易Tetrodotoxin
Virios Therapeutics Inc
原研
-
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：Nav1.2、Nav1.5、Nav1.1
商品名：Tectin、Tocudin、Tetrodin
适应症（已批准）：神经痛、海洛因依赖、癌症疼痛、疼痛、中毒
各地区研发/上市状态
美国
临床二期
2025-02-21
欧盟
-
中国
临床二期
2014-05-07
日本
-
合成路线与中间体2 routes
原研路线 × 2优化路线（非专利）× 0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 39 · 总收率 1.9 mg
TETRO-026—TETRO-031588694-02-4TETRO-032588694-04-6TETRO-033588694-06-8TETRO-034588694-08-0TETRO-035588694-10-4TETRO-036107819-90-9TETRO-037588694-14-8TETRO-038—TETRO-039588694-16-0TETRO-040—TETRO-041588694-18-2TETRO-0427724-39-2TETRO-04313072-89-4TETRO-044616225-39-9TETRO-011(4a-S)588693-41-8TETRO-013(4a-S)588693-43-0TETRO-014(4a-S)588693-45-2TETRO-015(4a-S)588693-49-6TETRO-017(4a-S)1026479-97-9TETRO-019(4a-S)588693-57-6TETRO-020(4a-S)588693-60-1TETRO-021(4a-S)588693-65-6TETRO-022(4a-S)588693-67-8TETRO-023(4a-S)588693-75-8TETRO-027(4a-S)588693-83-8TETRO-028(4a-S)588693-87-2TETRO-029(4a-S)588693-94-1TETRO-030(4a-S)588693-98-5TETRO-0013366-47-0TETRO-00293662-86-3TETRO-003115352-42-6TETRO-004588693-26-9TETRO-005—TETRO-0061066-54-2TETRO-007588693-32-7TETRO-008116-11-0TETRO-009588693-35-0TETRO-010588693-37-2TETRO-012—TETRO-016588693-51-0TETRO-018588693-53-2TETRO-024588693-77-0TETRO-025588693-79-2API · 河豚毒素
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| TETRO-026 | - | (1S,5R,6R)-6-((benzyloxy)methoxy)-8-(((tert-butyldiphenylsilyl)oxy)methyl)-9-((S)-2,2-dimethyl-1,3-dioxolan-4-yl)-5-(2-((4-methoxyphenyl)diphenylmethoxy)ethyl)-2-oxa-4-azabicyclo[3.3.1]non-7-en-3-one |
| TETRO-031 | 588694-02-4 | ((1S,5R,6R,7R,8S,9S)-7-acetoxy-9-((benzyloxy)methoxy)-5-((tert-butoxycarbonyl)amino)-6-(2,2-dimethyl-1,3-dioxolan-4-yl)-8-hydroxy-2-oxabicyclo[3.3.1]non-3-en-8-yl)methyl benzoate |
| TETRO-032 | 588694-04-6 | ((1S,5R,6R,7R,8S,9S)-7-acetoxy-9-((benzyloxy)methoxy)-5-((tert-butoxycarbonyl)amino)-6-(2,2-dimethyl-1,3-dioxolan-4-yl)-8-hydroxy-3,4-dioxo-2-oxabicyclo[3.3.1]nonan-8-yl)methyl benzoate |
| TETRO-033 | 588694-06-8 | ((1S,4R,5S,6R,7R,8S,9S)-7-acetoxy-9-((benzyloxy)methoxy)-5-((tert-butoxycarbonyl)amino)-6-(2,2-dimethyl-1,3-dioxolan-4-yl)-4,8-dihydroxy-3-oxo-2-oxabicyclo[3.3.1]nonan-8-yl)methyl benzoate |
| TETRO-034 | 588694-08-0 | (1R,3S,5S,6S,7R,8R,9S,10R)-3-(benzoyloxy)-9-((benzoyloxy)methyl)-6-((benzyloxy)methoxy)-7-((tert-butoxycarbonyl)amino)-8-(2,2-dimethyl-1,3-dioxolan-4-yl)-2,4-dioxaadamantane-9,10-diyl diacetate |
| TETRO-035 | 588694-10-4 | (1R,3S,5S,6S,7R,8R,9S,10R)-3-(benzoyloxy)-9-((benzoyloxy)methyl)-7-((tert-butoxycarbonyl)amino)-8-(2,2-dimethyl-1,3-dioxolan-4-yl)-2,4-dioxaadamantane-6,9,10-triyl triacetate |
| TETRO-036 | 107819-90-9 | tert-butyl N-[[(2-methylpropan-2-yl)oxycarbonylamino]-methylsulfanylmethylidene]carbamate |
| TETRO-037 | 588694-14-8 | (1R,3S,5S,6S,7R,8R,9S,10R)-3-(benzoyloxy)-9-((benzoyloxy)methyl)-7-((Z)-2,3-bis(tert-butoxycarbonyl)guanidino)-8-(1,2-dihydroxyethyl)-2,4-dioxaadamantane-6,9,10-triyl triacetate |
| TETRO-038 | - | (4R,4aR,5R,6S,7S,9S,10R,10aR,11S)-9-(benzoyloxy)-6-((benzoyloxy)methyl)-2-((tert-butoxycarbonyl)amino)-4-hydroxy-1,4,4a,5,6,7,9,10-octahydro-5,9-epoxy-7,10a-methanooxocino[4,5-d]pyrimidine-6,10,11-triyl triacetate |
| TETRO-039 | 588694-16-0 | (4R,4aR,5R,6S,7S,9S,10R,10aS,11S)-2-amino-9-(benzoyloxy)-6-((benzoyloxy)methyl)-4,10-dihydroxy-1,4,4a,5,6,7,9,10-octahydro-5,9-epoxy-7,10a-methanooxocino[4,5-d]pyrimidine-6,11-diyl diacetate |
| TETRO-040 | - | (4R,4aR,5R,6S,7S,9S,10R,10aS,11S)-2-amino-9-(benzoyloxy)-6-((benzoyloxy)methyl)-10-hydroxy-4-methoxy-1,4,4a,5,6,7,9,10-octahydro-5,9-epoxy-7,10a-methanooxocino[4,5-d]pyrimidine-6,11-diyl diacetate |
| TETRO-041 | 588694-18-2 | (4R,4aR,5R,6S,7S,9S,10R,10aR,11S,Z)-1,3-diacetyl-2-(acetylimino)-9-(benzoyloxy)-6-((benzoyloxy)methyl)-4-methoxydecahydro-5,9-epoxy-7,10a-methanooxocino[4,5-d]pyrimidine-6,10,11-triyl triacetate |
| TETRO-042 | 7724-39-2 | (4R,4aR,5R,6S,7S,9S,10R,10aR,11S)-2-amino-6-(hydroxymethyl)-4-methoxy-1,4,4a,5,6,7,9,10-octahydro-5,9-epoxy-7,10a-methanooxocino[4,5-d]pyrimidine-6,9,10,11-tetraol |
| TETRO-043 | 13072-89-4 | (4S,6S,8R,9S,10S,11S,11aR,12R)-2-amino-9-(hydroxymethyl)-1,4,5a,6,8,9,10,11-octahydro-4,8,11a-(epimethanetriyl)-6,10-epoxyoxocino[4,3-f][1,3,5]oxadiazepine-6,9,11-triol |
| TETRO-044 | 616225-39-9 | (R)-2-((tert-butyldimethylsilyl)oxy)-2-((R)-2,2-dimethyl-1,3-dioxolan-4-yl)-N,N-dimethylacetamide |
| TETRO-011(4a-S) | 588693-41-8 | 1-((2S,6S)-2-(((tert-butyldimethylsilyl)oxy)methyl)-4-ethynyl-6-isopropoxy-3,6-dihydro-2H-pyran-3-yl)-3-hydroxypropan-2-one |
| TETRO-013(4a-S) | 588693-43-0 | (Z)-3-((2S,6S)-2-(((tert-butyldimethylsilyl)oxy)methyl)-4-ethynyl-6-isopropoxy-3,6-dihydro-2H-pyran-3-yl)-2-(methoxymethoxy)prop-2-en-1-ol |
| TETRO-014(4a-S) | 588693-45-2 | (1S)-1-((2S,6S)-2-(((tert-butyldimethylsilyl)oxy)methyl)-4-ethynyl-6-isopropoxy-3,6-dihydro-2H-pyran-3-yl)-1,3-dihydroxypropan-2-one |
| TETRO-015(4a-S) | 588693-49-6 | (1S)-1-((2S,6S)-2-(((tert-butyldimethylsilyl)oxy)methyl)-4-ethynyl-6-isopropoxy-3,6-dihydro-2H-pyran-3-yl)-3-((tert-butyldiphenylsilyl)oxy)-2-oxopropyl benzoate |
| TETRO-017(4a-S) | 1026479-97-9 | (1S)-1-((2S,6S)-2-(((tert-butyldimethylsilyl)oxy)methyl)-4-(1-((tert-butyldimethylsilyl)oxy)vinyl)-6-methoxy-3,6-dihydro-2H-pyran-3-yl)-3-((tert-butyldiphenylsilyl)oxy)-2-oxopropyl benzoate |
| TETRO-019(4a-S) | 588693-57-6 | (1S,3S,5R,8S)-5-((benzyloxy)methoxy)-1-(((tert-butyldimethylsilyl)oxy)methyl)-7-(((tert-butyldiphenylsilyl)oxy)methyl)-3-methoxy-3,5,8,8a-tetrahydro-1H-isochromen-8-yl benzoate |
| TETRO-020(4a-S) | 588693-60-1 | (1S,5R,8S)-1-(acetoxymethyl)-5-((benzyloxy)methoxy)-7-(((tert-butyldiphenylsilyl)oxy)methyl)-3-methoxy-3,5,8,8a-tetrahydro-1H-isochromen-8-yl benzoate |
| TETRO-021(4a-S) | 588693-65-6 | (1S,5R,8S)-5-((benzyloxy)methoxy)-7-(((tert-butyldiphenylsilyl)oxy)methyl)-3-hydroxy-1-(hydroxymethyl)-3,5,8,8a-tetrahydro-1H-isochromen-8-yl benzoate |
| TETRO-022(4a-S) | 588693-67-8 | (1S,4R,E)-4-((benzyloxy)methoxy)-2-(((tert-butyldiphenylsilyl)oxy)methyl)-6-((S)-2,2-dimethyl-1,3-dioxolan-4-yl)-5-(2-hydroxyethylidene)cyclohex-2-en-1-yl benzoate |
| TETRO-023(4a-S) | 588693-75-8 | (E)-methyl 2-((2R,5S)-2-((benzyloxy)methoxy)-4-(((tert-butyldiphenylsilyl)oxy)methyl)-6-((S)-2,2-dimethyl-1,3-dioxolan-4-yl)-5-hydroxycyclohex-3-en-1-ylidene)acetate |
| TETRO-027(4a-S) | 588693-83-8 | tert-butyl ((1R,2R,5S)-2-((benzyloxy)methoxy)-6-((S)-2,2-dimethyl-1,3-dioxolan-4-yl)-5-hydroxy-4-(hydroxymethyl)-1-(2-((4-methoxyphenyl)diphenylmethoxy)ethyl)cyclohex-3-en-1-yl)carbamate |
| TETRO-028(4a-S) | 588693-87-2 | ((1S,2S,4R,5S,6R)-5-((benzyloxy)methoxy)-4-((tert-butoxycarbonyl)amino)-3-((S)-2,2-dimethyl-1,3-dioxolan-4-yl)-2-hydroxy-4-(2-((4-methoxyphenyl)diphenylmethoxy)ethyl)-7-oxabicyclo[4.1.0]heptan-1-yl)methyl benzoate |
| TETRO-029(4a-S) | 588693-94-1 | ((1S,2R,4R,5S,6R)-2-acetoxy-5-((benzyloxy)methoxy)-4-((tert-butoxycarbonyl)amino)-3-((S)-2,2-dimethyl-1,3-dioxolan-4-yl)-4-(2-((4-methoxyphenyl)diphenylmethoxy)ethyl)-7-oxabicyclo[4.1.0]heptan-1-yl)methyl benzoate |
| TETRO-030(4a-S) | 588693-98-5 | ((1S,2R,4R,5S,6R)-2-acetoxy-5-((benzyloxy)methoxy)-4-((tert-butoxycarbonyl)amino)-3-((S)-2,2-dimethyl-1,3-dioxolan-4-yl)-4-(2-oxoethyl)-7-oxabicyclo[4.1.0]heptan-1-yl)methyl benzoate |
| TETRO-001 | 3366-47-0 | (2R,3R,4S)-2-(acetoxymethyl)-3,4-dihydro-2H-pyran-3,4,5-triyl triacetate |
| TETRO-002 | 93662-86-3 | (2R,3S,6S)-2-(acetoxymethyl)-6-isopropoxy-3,6-dihydro-2H-pyran-3,5-diyl diacetate |
| TETRO-003 | 115352-42-6 | (2S,3R,6S)-6-(hydroxymethyl)-2-isopropoxy-3,6-dihydro-2H-pyran-3-ol |
| TETRO-004 | 588693-26-9 | (2S,6S)-6-(((tert-butyldimethylsilyl)oxy)methyl)-2-isopropoxy-2H-pyran-3(6H)-one |
| TETRO-005 | - | (2S,3R,6S)-6-(((tert-butyldimethylsilyl)oxy)methyl)-2-isopropoxy-4-methyl-3,6-dihydro-2H-pyran-3-ol |
| TETRO-006 | 1066-54-2在售 | ethynyltrimethylsilane |
| TETRO-007 | 588693-32-7 | (2S,3R,6S)-6-(((tert-butyldimethylsilyl)oxy)methyl)-2-isopropoxy-4-((trimethylsilyl)ethynyl)-3,6-dihydro-2H-pyran-3-ol |
| TETRO-008 | 116-11-0 | 2-methoxyprop-1-ene |
| TETRO-009 | 588693-35-0 | tert-butyl(((2S,5R,6S)-6-isopropoxy-5-(prop-1-en-2-yloxy)-4-((trimethylsilyl)ethynyl)-5,6-dihydro-2H-pyran-2-yl)methoxy)dimethylsilane |
| TETRO-010 | 588693-37-2 | 1-((2S,3S,6S)-2-(((tert-butyldimethylsilyl)oxy)methyl)-6-isopropoxy-4-((trimethylsilyl)ethynyl)-3,6-dihydro-2H-pyran-3-yl)propan-2-one |
| TETRO-012 | - | (Z)-3-((2S,6S)-2-(((tert-butyldimethylsilyl)oxy)methyl)-4-ethynyl-6-isopropoxy-3,6-dihydro-2H-pyran-3-yl)-2-hydroxyacrylaldehyde |
| TETRO-016 | 588693-51-0 | (2S,5S,6S,8aS)-4-acetyl-6-(((tert-butyldiphenylsilyl)oxy)methyl)-6-hydroxy-2-methoxy-2,4a,5,6,8,8a-hexahydropyrano[3,4-b]pyran-5-yl benzoate |
| TETRO-018 | 588693-53-2 | (1S,3S,8S)-1-(((tert-butyldimethylsilyl)oxy)methyl)-7-(((tert-butyldiphenylsilyl)oxy)methyl)-3-methoxy-5-oxo-3,5,8,8a-tetrahydro-1H-isochromen-8-yl benzoate |
| TETRO-024 | 588693-77-0 | (E)-methyl 2-((2R,5S,6R)-2-((benzyloxy)methoxy)-4-(((tert-butyldiphenylsilyl)oxy)methyl)-5-(carbamoyloxy)-6-((S)-2,2-dimethyl-1,3-dioxolan-4-yl)cyclohex-3-en-1-ylidene)acetate |
| TETRO-025 | 588693-79-2 | methyl 2-(6-((benzyloxy)methoxy)-8-(((tert-butyldiphenylsilyl)oxy)methyl)-9-((S)-2,2-dimethyl-1,3-dioxolan-4-yl)-3-oxo-2-oxa-4-azabicyclo[3.3.1]non-7-en-5-yl)acetate |
原研Route 2步骤 16 · 总收率 /
TETRO-045108275-53-2TETRO-046616225-40-2TETRO-047616225-41-3TETRO-048616225-42-4TETRO-049616225-43-5TETRO-050616225-44-6TETRO-051616225-45-7TETRO-052616225-46-8TETRO-053616225-46-8TETRO-054616225-48-0TETRO-055616225-49-1TETRO-056616225-50-4TETRO-057616225-51-5TETRO-058616225-52-6TETRO-059616225-53-7API · 河豚毒素
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| TETRO-045 | 108275-53-2 | (R)-2-((tert-butyldimethylsilyl)oxy)-2-((R)-2,2-dimethyl-1,3-dioxolan-4-yl)acetaldehyde |
| TETRO-046 | 616225-40-2 | (S)-benzyl 2-((S)-((tert-butyldimethylsilyl)oxy)((R)-2,2-dimethyl-1,3-dioxolan-4-yl)methyl)-4-hydroxy-5-oxo-2,5-dihydrofuran-3-carboxylate |
| TETRO-047 | 616225-41-3 | (S)-benzyl 2-((S)-((tert-butyldimethylsilyl)oxy)((R)-2,2-dimethyl-1,3-dioxolan-4-yl)methyl)-5-oxo-4-(pivaloyloxy)-2,5-dihydrofuran-3-carboxylate |
| TETRO-048 | 616225-42-4 | (S)-5-((S)-((tert-butyldimethylsilyl)oxy)((R)-2,2-dimethyl-1,3-dioxolan-4-yl)methyl)-4-(2-diazoacetyl)-2-oxo-2,5-dihydrofuran-3-yl pivalate |
| TETRO-049 | 616225-43-5 | (4'R,7S,7aS)-7-((tert-butyldimethylsilyl)oxy)-2',2'-dimethyl-2,4-dioxo-4,5,7,7a-tetrahydro-2H-spiro[benzofuran-6,4'-[1,3]dioxolan]-3-yl pivalate |
| TETRO-050 | 616225-44-6 | (3aS,4R,5aS,8S,8aS,8bS)-2,2,2',2'-tetramethyl-7-oxohexahydro-3aH-spiro[[1,3]dioxolo[4,5-e]benzofuran-4,4'-[1,3]dioxolan]-8-yl pivalate |
| TETRO-051 | 616225-45-7 | (S)-2-(dimethylamino)-2-oxo-1-((3aS,4R,7S,7aS)-2,2,2',2'-tetramethyl-6-methylenetetrahydro-3aH-spiro[benzo[d][1,3]dioxole-4,4'-[1,3]dioxolan]-7-yl)ethyl pivalate |
| TETRO-052 | 616225-46-8 | (S)-1-((3aS,4S,5R,6R,7S,7aS)-6-allyl-5-hydroxy-2,2,2',2'-tetramethyltetrahydro-3aH-spiro[benzo[d][1,3]dioxole-4,4'-[1,3]dioxolan]-7-yl)-2-(dimethylamino)-2-oxoethyl pivalate |
| TETRO-053 | 616225-46-8 | (S)-1-((3aS,4S,5R,6R,7S,7aS)-6-allyl-5-hydroxy-2,2,2',2'-tetramethyltetrahydro-3aH-spiro[benzo[d][1,3]dioxole-4,4'-[1,3]dioxolan]-7-yl)-2-(dimethylamino)-2-oxoethyl pivalate |
| TETRO-054 | 616225-48-0 | (3aS,4S,5R,8S,9S,9aS,10R)-10-allyl-2,2,2',2'-tetramethyl-7-oxohexahydrospiro[5,9-methano[1,3]dioxolo[4,5-d]oxocine-4,4'-[1,3]dioxolan]-8-yl pivalate |
| TETRO-055 | 616225-49-1 | (3aS,4S,5R,8S,9R,9aS,10R)-10-allyl-8-hydroxy-2,2,2',2'-tetramethyltetrahydrospiro[5,9-methano[1,3]dioxolo[4,5-d]oxocine-4,4'-[1,3]dioxolan]-7(3aH)-one |
| TETRO-056 | 616225-50-4 | (3aS,4S,5R,8S,9S,9aS,10R)-10-(2-chloroethyl)-2,2,2',2'-tetramethyl-7-oxohexahydrospiro[5,9-methano[1,3]dioxolo[4,5-d]oxocine-4,4'-[1,3]dioxolan]-8-yl carbamate |
| TETRO-057 | 616225-51-5 | (3aS,4'S,6R,7aS,10aS,10bR,11R)-11-(2-chloroethyl)-2',2',9,9-tetramethyldihydro-1H-spiro[6,10b-methano[1,3]dioxolo[4',5':5,6]oxocino[4,3-d]oxazole-7,4'-[1,3]dioxolane]-2,4(3aH,6H)-dione |
| TETRO-058 | 616225-52-6 | tert-butyl ((3aS,4S,5R,8S,9S,9aS,10R)-8-hydroxy-2,2,2',2'-tetramethyl-7-oxo-10-vinylhexahydrospiro[5,9-methano[1,3]dioxolo[4,5-d]oxocine-4,4'-[1,3]dioxolan]-9-yl)carbamate |
| TETRO-059 | 616225-53-7 | (3aS,4S,5R,8S,9S,9aS,10R)-9-amino-8-hydroxy-2,2,2',2'-tetramethyl-10-vinyltetrahydrospiro[5,9-methano[1,3]dioxolo[4,5-d]oxocine-4,4'-[1,3]dioxolan]-7(3aH)-one |
常见问题（FAQ）
河豚毒素的适应症有哪些？
已批准的适应症包括：神经痛、海洛因依赖、癌症疼痛、疼痛、中毒。
河豚毒素的专利什么时候到期？
河豚毒素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。
河豚毒素有几条合成路线？
本站收录 2 条合成路线，最短路线 16 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
河豚毒素的关键中间体在哪里可以采购？
河豚毒素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。
如何获取河豚毒素中间体的报价？
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） · 2026-10-12