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托伐普坦
Tier B — Position earlyTolvaptan · all drugs expiring in 2028 →
Otsuka Holdings Co Ltd
Originator
2009
First approval
2028
Expiry (public)
$1.84B ▲
Peak sales
化学药
Type
Targets：V2R
Brand：Jinarc、苏麦卡、Samsca/Jinarc、Jynarque、Samsca
Indications (approved)：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
Regional status
US
批准上市
2009-05-19
EU
批准上市
2009-08-02
China
批准上市
2011-09-07
Japan
批准上市
2010-10-27
Synthetic routes & intermediates6 routes
Originator routes × 1Optimised (non-patent) × 5Process routes × 0
Routes are ordered originator first, then optimised / process (non-patent) routes; each lists steps, overall yield and the intermediate table (code / CAS / name) — ready for supplier sourcing and RFQ. Rendered by this site from structured data; no third-party route graphics used.
OriginatorRoute 1Steps 4 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 |
OptimisedRoute 2Steps 10 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 |
OptimisedRoute 3Steps 2 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 |
OptimisedRoute 4Steps 4 · Total yield 4.85 g
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 |
OptimisedRoute 5Steps 8 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 |
OptimisedRoute 6Steps 11 · Total yield 93 mg
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 |
Frequently asked questions
What are the approved indications of Tolvaptan?
Approved indications include: 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.
When does the Tolvaptan patent expire?
Based on public sources, the Tolvaptan patent expires in 2028.
How many synthesis routes are recorded for Tolvaptan?
6 synthesis routes are recorded; the shortest is 2 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Tolvaptan intermediates?
All intermediates in Tolvaptan routes have CAS profiles — you can submit an RFQ per CAS and it enters the Unibest matching pool.
How do I get a quote for Tolvaptan intermediates?
Open the CAS profile of the target intermediate from this page, or submit an RFQ directly — the CAS enters the matching flow automatically and the supply network responds with quotes.
Source: cross-verified data (structured fields only) · 2026-09-24