Brexpiprazole

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Brexpiprazole · all drugs expiring in 2029 →

Otsuka Pharmaceutical Co., Ltd.

Originator

2015

First approval

2029

Expiry (public)

$3.15B ▲

Peak sales

Small molecule

Type

Targets：5-HT2A, 5-HT1A, DRD2

Brand：REXULTIOD, Rexulti, RexultiOD, Rxulti

Indications (approved)：Schizophrenia, Alzheimer's disease, Agitation, Depression, Depressive disorder, Major depressive disorder

Regional status

Approved

2015-07-10

Approved

2018-07-26

China

Approved

2024-06-25

Japan

Approved

2018-01-19

Synthetic routes & intermediates3 routes

Originator routes × 1Optimised (non-patent) × 1Process routes × 1

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 3 · Total yield 13.6 g

Code	CAS No.	Intermediate
BREX-001	70500-72-0 Available	7-hydroxyquinolin-2(1H)-one
BREX-002	6940-78-9	1-bromo-4-chlorobutane
BREX-003	-	7-(4-chlorobutoxy)quinolin-2(1H)-one
BREX-004	-	1-(benzo[b]thiophen-4-yl)piperazine hydrochloride
BREX-005	5118-13-8 Available	4-bromobenzo[b]thiophene
BREX-006	110-85-0 Available	piperazine

OptimisedRoute 2Steps 5 · Total yield 1.3 g

Synthetic routes & intermediates Route 2

Code	CAS No.	Intermediate
BREX-007	387-45-1	2-chloro-6-fluorobenzaldehyde
BREX-008	57260-71-6 Available	tert-butyl piperazine-1-carboxylate
BREX-009	1096535-48-6	tert-butyl 4-(3-chloro-2-formylphenyl)piperazine-1-carboxylate
BREX-010	623-51-8	ethyl 2-mercaptoacetate
BREX-011	-	tert-butyl 4-(2-(ethoxycarbonyl)benzo[b]thiophen-4-yl)piperazine-1-carboxylate
BREX-012	-	4-(4-(tert-butoxycarbonyl)piperazin-1-yl)benzo[b]thiophene-2-carboxylic acid
BREX-013	-	tert-butyl 4-(benzo[b]thiophen-4-yl)piperazine-1-carboxylate

ProcessRoute 3Steps 7 · Total yield 14.3 g

Synthetic routes & intermediates Route 3

Code	CAS No.	Intermediate
BREX-007	387-45-1	2-chloro-6-fluorobenzaldehyde
BREX-014	141-84-4	2-thioxothiazolidin-4-one
BREX-015	65562-49-4	(Z)-5-(2,6-dichlorobenzylidene)-2-thioxothiazolidin-4-one
BREX-016	1420987-77-4	(Z)-3-(2,6-dichlorophenyl)-2-mercaptoacrylic acid
BREX-017	23967-57-9	4-chlorobenzo[b]thiophene-2-carboxylic acid
BREX-018	-	4-chlorobenzo[b]thiophene
BREX-001	70500-72-0 Available	7-hydroxyquinolin-2(1H)-one
BREX-002	6940-78-9	1-bromo-4-chlorobutane
BREX-003	-	7-(4-chlorobutoxy)quinolin-2(1H)-one
BREX-004	-	1-(benzo[b]thiophen-4-yl)piperazine hydrochloride

Frequently asked questions

What are the approved indications of Brexpiprazole?

Approved indications include: Schizophrenia, Alzheimer's disease, Agitation, Depression, Depressive disorder, Major depressive disorder.

When does the Brexpiprazole patent expire?

Based on public sources, the Brexpiprazole patent expires in 2029.

How many synthesis routes are recorded for Brexpiprazole?

3 synthesis routes are recorded; the shortest is 3 steps with 13.6 g total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Brexpiprazole intermediates?

4 intermediate CAS of Brexpiprazole 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 Brexpiprazole 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