Granisetron

Tier C — Watch / trade

Granisetron

Kyowa Hakko Kirin Co Ltd

Originator

1997

First approval

Expiry (public)

$0.15B ▲

Peak sales

Small molecule

Type

Targets：5-HT3

Brand：Sancuso, Sustol

Indications (approved)：Chemotherapy-induced nausea and vomiting, Nausea, 呕吐, 手术后恶心呕吐

Regional status

Approved

2008-09-12

Approved

2012-04-20

China

Approved

1997-01-01

Japan

Synthetic routes & intermediates6 routes

Originator routes × 0Optimised (non-patent) × 6Process 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.

OptimisedRoute 1Steps 2 · Total yield 10g

Granisetron-00150890-83-0Granisetron-002106649-02-9Granisetron-00376272-56-5API · Granisetron

Code	CAS No.	Intermediate
Granisetron-001	50890-83-0	1-Methylindazole-3-carboxylic acid
Granisetron-002	106649-02-9	1-Methyl-1H-indazole-3-carbonyl chloride
Granisetron-003	76272-56-5	endo-9-Methyl-9-azabicyclo[3.3.1]nonan-3-amine

OptimisedRoute 2Steps 3 · Total yield /

Granisetron-0045130-24-5Granisetron-005—Granisetron-006—Granisetron-007—API · Granisetron

Code	CAS No.	Intermediate
Granisetron-004	5130-24-5	Chloridocarbonic acid vinyl ester
Granisetron-005	-	1-Methyl-N-[(1R,3R,5S)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]-1H-indazole-3-carboxamide
Granisetron-006	-	ethenyl (1R,3R,5S)-3-(1-methyl-1H-indazole-3-amido)-9-azabicyclo[3.3.1]nonane-9-carboxylate
Granisetron-007	-	N-[(1R,3R,5S)-9-azabicyclo[3.3.1]nonan-3-yl]-1-methyl-1H-indazole-3-carboxamide

OptimisedRoute 3Steps 9 · Total yield /

Granisetron-00891-56-5Granisetron-00974-88-4Granisetron-0102058-74-4Granisetron-01114271-46-6Granisetron-00150890-83-0Granisetron-002106649-02-9Granisetron-00376272-56-5Granisetron-012111-30-8Granisetron-013593-51-1Granisetron-014542-05-2Granisetron-015552-70-5Granisetron-0165470-11-1Granisetron-0176164-67-6Granisetron-01888475-55-2API · Granisetron

Code	CAS No.	Intermediate
Granisetron-008	91-56-5	2,3-Indolinedione
Granisetron-009	74-88-4 Available	Iodomethane
Granisetron-010	2058-74-4	1-Methyl-1H-indole-2,3-dione
Granisetron-011	14271-46-6	3,3-Dimethoxy-1-methyl-1,3-dihydro-2H-indol-2-one
Granisetron-001	50890-83-0	1-Methylindazole-3-carboxylic acid
Granisetron-002	106649-02-9	1-Methyl-1H-indazole-3-carbonyl chloride
Granisetron-003	76272-56-5	endo-9-Methyl-9-azabicyclo[3.3.1]nonan-3-amine
Granisetron-012	111-30-8	Glutaraldehyde
Granisetron-013	593-51-1	Methanamine hydrochloride
Granisetron-014	542-05-2	1,3-Acetonedicarboxylic acid
Granisetron-015	552-70-5	9-Methyl-9-azabicyclo[3.3.1]nonan-3-one
Granisetron-016	5470-11-1 Available	Hydroxylamine hydrochloride
Granisetron-017	6164-67-6	N-Hydroxy-9-methyl-9-azabicyclo[3.3.1]nonan-3-imine
Granisetron-018	88475-55-2	1-Methyl-2,3-dihydro-1H-indole

OptimisedRoute 4Steps 1 · Total yield 8.02g(Granisetron-001)

Granisetron-0194498-67-3Granisetron-02074-89-5Granisetron-00150890-83-0API · Granisetron

Code	CAS No.	Intermediate
Granisetron-019	4498-67-3	1H-Indazole-3-carboxylic acid
Granisetron-020	74-89-5	Methylamine
Granisetron-001	50890-83-0	1-Methylindazole-3-carboxylic acid

OptimisedRoute 5Steps 6 · Total yield 93.06mg(Granisetron (Free))

Granisetron-0213740-52-1Granisetron-00376272-56-5Granisetron-022—Granisetron-023—Granisetron-0242411174-21-3Granisetron-00974-88-4Granisetron-005—Granisetron-025271-44-3Granisetron-026—API · Granisetron

Code	CAS No.	Intermediate
Granisetron-021	3740-52-1	2-(2-Nitrophenyl)acetic acid
Granisetron-003	76272-56-5	endo-9-Methyl-9-azabicyclo[3.3.1]nonan-3-amine
Granisetron-022	-	endo-N-[(1R,3r,5S)-9-Methyl-9-azabicyclo[3.3.1]nonan-3-yl]-2-(2-nitrophenyl)acetamide
Granisetron-023	-	endo-2-(2-Aminophenyl)-N-[(1R,3r,5S)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]acetamide
Granisetron-024	2411174-21-3	endo-N-[(1R,3r,5S)-9-Methyl-9-azabicyclo[3.3.1]nonan-3-yl]-1H-indazole-3-carboxamide
Granisetron-009	74-88-4 Available	Iodomethane
Granisetron-005	-	1-Methyl-N-[(1R,3R,5S)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]-1H-indazole-3-carboxamide
Granisetron-025	271-44-3	1,2-Benzodiazole
Granisetron-026	-	3-(Trifluoromethyl)-1H-indazole

OptimisedRoute 6Steps 1 · Total yield 14mg(Granisetron-019)

Granisetron-02764132-13-4Granisetron-0194498-67-3API · Granisetron

Code	CAS No.	Intermediate
Granisetron-027	64132-13-4	(1H-Indazol-3-yl)methanol
Granisetron-019	4498-67-3	1H-Indazole-3-carboxylic acid

Frequently asked questions

What are the approved indications of Granisetron?

Approved indications include: Chemotherapy-induced nausea and vomiting, Nausea, 呕吐, 手术后恶心呕吐.

When does the Granisetron patent expire?

No public expiry year is available for Granisetron yet; this page updates once verified.

How many synthesis routes are recorded for Granisetron?

6 synthesis routes are recorded; the shortest is 1 steps with 8.02g(Granisetron-001) total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Granisetron intermediates?

2 intermediate CAS of Granisetron are available through the Unibest supply network — see the route tables on this page and request a quote per CAS.

How do I get a quote for Granisetron 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