Tolvaptan
Tier B — Position earlyTolvaptan · all drugs expiring in 2028 →
Targets：V2R
Brand：Jinarc, Samsca/Jinarc, Jynarque, Samsca
Indications (approved)：Autosomal dominant polycystic kidney disease, Fibrosis, Hyponatraemia, Heart failure, Syndrome of inappropriate antidiuretic hormone secretion
Regional status
Factories producing this API1
Factories registered as producing this API in our sourcing network (RFQ records + product master), sorted by RFQ activity; the snapshot carries no cost or customer data.
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Sign in to view factories →Synthetic routes & intermediates6 routes
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.
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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: Autosomal dominant polycystic kidney disease, Fibrosis, Hyponatraemia, Heart failure, Syndrome of inappropriate antidiuretic hormone secretion.
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) · 2026-09-29