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托伐普坦
Tier B · 提前布局Tolvaptan · 2028 年到期全部品种 →
Otsuka Holdings Co Ltd
原研
2009
首批上市
2028
到期年（公开口径）
$1.84B ▲
峰值销售
化学药
类型
靶点：V2R
商品名：Jinarc、苏麦卡、Samsca/Jinarc、Jynarque、Samsca
适应症（已批准）：常染色体显性多囊肾病、纤维化、低钠血症、心脏衰竭、抗利尿激素分泌失调综合征
各地区研发/上市状态
美国
批准上市
2009-05-19
欧盟
批准上市
2009-08-02
中国
批准上市
2011-09-07
日本
批准上市
2010-10-27
合成路线与中间体6 routes
原研路线 × 1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。
原研Route 1步骤 4 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| TOLV-001 | 160129-45-3 | 7-chloro-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
| TOLV-002 | 35675-46-8 | 3-methyl-4-nitrobenzoyl chloride |
| TOLV-003 | 137982-91-3 | 7-chloro-1-(2-methyl-4-nitrobenzoyl)-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
| TOLV-004 | 137977-97-0 | 1-(4-amino-2-methylbenzoyl)-7-chloro-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
| TOLV-005 | 933-88-0 | 2-methylbenzoyl chloride |
| TOLV-006 | 137973-76-3 | N-(4-(7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide |
优化Route 2步骤 10 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| TOLV-002 | 35675-46-8 | 3-methyl-4-nitrobenzoyl chloride |
| TOLV-007 | 91193-23-6 | S-(2-(4-chlorophenyl)-2-oxoethyl) O-ethyl carbonodithioate |
| TOLV-008 | 3377-92-2 | vinyl pivalate |
| TOLV-009 | 608139-02-2 | 4-(4-chlorophenyl)-1-((ethoxycarbonothioyl)thio)-4-oxobutyl pivalate |
| TOLV-010 | 804498-94-0 | 7-chloro-4-oxo-1,2,3,4-tetrahydronaphthalen-1-yl pivalate |
| TOLV-011 | 863762-02-1 | (Z)-7-chloro-4-(hydroxyimino)-1,2,3,4-tetrahydronaphthalen-1-yl pivalate |
| TOLV-012 | - | 3,3,7-trichloro-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl pivalate |
| TOLV-013 | - | 7-chloro-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl pivalate |
| TOLV-014 | 863762-10-1 | 7-chloro-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl pivalate |
| TOLV-015 | 863762-20-3 | 7-chloro-1-(2-methyl-4-nitrobenzoyl)-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl pivalate |
| TOLV-016 | 863762-24-7 | 1-(4-amino-2-methylbenzoyl)-7-chloro-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl pivalate |
| TOLV-017 | - | 7-chloro-1-(2-methyl-4-(2-methylbenzamido)benzoyl)-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl pivalate |
优化Route 3步骤 2 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| TOLV-001 | 160129-45-3 | 7-chloro-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
| TOLV-006 | 137973-76-3 | N-(4-(7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide |
| TOLV-018 | 317374-07-5 | N-(4-bromo-3-methylphenyl)-2-methylbenzamide |
优化Route 4步骤 4 · 总收率 4.85 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| TOLV-001 | 160129-45-3 | 7-chloro-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
| TOLV-002 | 35675-46-8 | 3-methyl-4-nitrobenzoyl chloride |
| TOLV-003 | 137982-91-3 | 7-chloro-1-(2-methyl-4-nitrobenzoyl)-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
| TOLV-004 | 137977-97-0 | 1-(4-amino-2-methylbenzoyl)-7-chloro-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
| TOLV-005 | 933-88-0 | 2-methylbenzoyl chloride |
| TOLV-006 | 137973-76-3 | N-(4-(7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide |
优化Route 5步骤 8 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| TOLV-001 | 160129-45-3 | 7-chloro-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
| TOLV-002 | 35675-46-8 | 3-methyl-4-nitrobenzoyl chloride |
| TOLV-003 | 137982-91-3 | 7-chloro-1-(2-methyl-4-nitrobenzoyl)-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
| TOLV-004 | 137977-97-0 | 1-(4-amino-2-methylbenzoyl)-7-chloro-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
| TOLV-005 | 933-88-0 | 2-methylbenzoyl chloride |
| TOLV-006 | 137973-76-3 | N-(4-(7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide |
| TOLV-019 | 96515-79-6 | 5-chloro-2-fluorobenzaldehyde |
| TOLV-020 | 124-02-7 | diallylamine |
| TOLV-021 | 1594771-76-2 | 5-chloro-2-(diallylamino)benzaldehyde |
| TOLV-022 | 1637784-90-7 | 1-allyl-7-chloro-2,3,4,5-tetrahydro-1H-2,5-epoxybenzo[b]azepine |
| TOLV-023 | 1637784-91-8 | 1-allyl-7-chloro-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
优化Route 6步骤 11 · 总收率 93 mg
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| TOLV-001 | 160129-45-3 | 7-chloro-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
| TOLV-002 | 35675-46-8 | 3-methyl-4-nitrobenzoyl chloride |
| TOLV-003 | 137982-91-3 | 7-chloro-1-(2-methyl-4-nitrobenzoyl)-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
| TOLV-004 | 137977-97-0 | 1-(4-amino-2-methylbenzoyl)-7-chloro-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
| TOLV-005 | 933-88-0 | 2-methylbenzoyl chloride |
| TOLV-006 | 137973-76-3 | N-(4-(7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide |
| TOLV-024 | 2516-95-2 | 5-chloro-2-nitrobenzoic acid |
| TOLV-025 | 51282-49-6 | methyl 5-chloro-2-nitrobenzoate |
| TOLV-026 | 5202-89-1 | methyl 2-amino-5-chlorobenzoate |
| TOLV-027 | 247237-38-3 | methyl 5-chloro-2-((4-methylphenyl)sulfonamido)benzoate |
| TOLV-028 | 2969-81-5 | ethyl 4-bromobutanoate |
| TOLV-029 | 247237-43-0 | methyl 5-chloro-2-((N-(4-ethoxy-4-oxobutyl)-4-methylphenyl)sulfonamido)benzoate |
| TOLV-030 | 1448365-49-8 | methyl 7-chloro-5-oxo-1-tosyl-2,3,4,5-tetrahydro-1H-benzo[b]azepine-4-carboxylate |
| TOLV-031 | 193686-76-9 | 7-chloro-1-tosyl-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one |
常见问题（FAQ）
托伐普坦的适应症有哪些？
已批准的适应症包括：常染色体显性多囊肾病、纤维化、低钠血症、心脏衰竭、抗利尿激素分泌失调综合征。
托伐普坦的专利什么时候到期？
按公开口径，托伐普坦的专利到期年为 2028 年。
托伐普坦有几条合成路线？
本站收录 6 条合成路线，最短路线 2 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
托伐普坦的关键中间体在哪里可以采购？
托伐普坦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。
如何获取托伐普坦中间体的报价？
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