Bosentan Hydrate

Tier C — Watch / trade

Bosentan Hydrate

F. Hoffmann-La Roche

Originator

2001

First approval

Expiry (public)

No sales data

Peak sales

Small molecule

Type

Targets：ETAR, ETBR

Brand：Tracleer, Stayveer

Indications (approved)：溃疡, Pulmonary arterial hypertension, Pulmonary hypertension, Systemic sclerosis

Regional status

Approved

2001-11-20

Approved

2002-05-14

China

Approved

2006-03-23

Japan

Approved

2005-04-11

Synthetic routes & intermediates5 routes

Originator routes × 1Optimised (non-patent) × 3Process 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 5 · Total yield /

BOSE-00190-05-1BOSE-002685-87-0BOSE-00320730-58-9BOSE-004—BOSE-005329923-15-1BOSE-006150728-13-5BOSE-0076292-59-7BOSE-008150727-06-3BOSE-009107-21-1API · Bosentan Hydrate

Code	CAS No.	Intermediate
BOSE-001	90-05-1	2-methoxyphenol
BOSE-002	685-87-0	diethyl 2-bromomalonate
BOSE-003	20730-58-9	diethyl 2-(2-methoxyphenoxy)malonate
BOSE-004	-	pyrimidine-2-carboximidamide hydrochloride
BOSE-005	329923-15-1	5-(2-methoxyphenoxy)-[2,2'-bipyrimidine]-4,6-diol
BOSE-006	150728-13-5	4,6-dichloro-5-(2-methoxyphenoxy)-2,2'-bipyrimidine
BOSE-007	6292-59-7	4-(tert-butyl)benzenesulfonamide
BOSE-008	150727-06-3	4-(tert-butyl)-N-(6-chloro-5-(2-methoxyphenoxy)-[2,2'-bipyrimidin]-4-yl)benzenesulfonamide
BOSE-009	107-21-1 Available	ethane-1,2-diol

OptimisedRoute 2Steps 3 · Total yield 107 mg

BOSE-006150728-13-5BOSE-0076292-59-7BOSE-0102162-31-4BOSE-011—BOSE-012—API · Bosentan Hydrate

Code	CAS No.	Intermediate
BOSE-006	150728-13-5	4,6-dichloro-5-(2-methoxyphenoxy)-2,2'-bipyrimidine
BOSE-007	6292-59-7	4-(tert-butyl)benzenesulfonamide
BOSE-010	2162-31-4	2-((tetrahydro-2H-pyran-2-yl)oxy)ethan-1-ol
BOSE-011	-	4-chloro-5-(2-methoxyphenoxy)-6-(2-((tetrahydro-2H-pyran-2-yl)oxy)ethoxy)-2,2'-bipyrimidine
BOSE-012	-	4-(tert-butyl)-N-(5-(2-methoxyphenoxy)-6-(2-((tetrahydro-2H-pyran-2-yl)oxy)ethoxy)-[2,2'-bipyrimidin]-4-yl)benzenesulfonamide

OptimisedRoute 4Steps 6 · Total yield 1.26 g

BOSE-006150728-13-5BOSE-0076292-59-7BOSE-013150728-12-4BOSE-014—BOSE-01814080-23-0BOSE-019150726-89-9BOSE-020621-63-6BOSE-0211250871-99-8BOSE-0221174918-30-9API · Bosentan Hydrate

Code	CAS No.	Intermediate
BOSE-006	150728-13-5	4,6-dichloro-5-(2-methoxyphenoxy)-2,2'-bipyrimidine
BOSE-007	6292-59-7	4-(tert-butyl)benzenesulfonamide
BOSE-013	150728-12-4	5-(2-methoxyphenoxy)-[2,2'-bipyrimidine]-4,6(1H,5H)-dione
BOSE-014	-	potassium ((4-(tert-butyl)phenyl)sulfonyl)(6-chloro-5-(2-methoxyphenoxy)-[2,2'-bipyrimidin]-4-yl)amide
BOSE-018	14080-23-0	pyrimidine-2-carbonitrile
BOSE-019	150726-89-9	dimethyl 2-(2-methoxyphenoxy)malonate
BOSE-020	621-63-6	2,2-diethoxyethan-1-ol
BOSE-021	1250871-99-8	4-(tert-butyl)-N-(6-(2,2-diethoxyethoxy)-5-(2-methoxyphenoxy)-[2,2'-bipyrimidin]-4-yl)benzenesulfonamide
BOSE-022	1174918-30-9	4-(tert-butyl)-N-(5-(2-methoxyphenoxy)-6-(2-oxoethoxy)-[2,2'-bipyrimidin]-4-yl)benzenesulfonamide

OptimisedRoute 5Steps 5 · Total yield 77.6 g

BOSE-006150728-13-5BOSE-0076292-59-7BOSE-008150727-06-3BOSE-0221174918-30-9BOSE-023—BOSE-0241448588-52-0BOSE-0251448588-53-1API · Bosentan Hydrate

Code	CAS No.	Intermediate
BOSE-006	150728-13-5	4,6-dichloro-5-(2-methoxyphenoxy)-2,2'-bipyrimidine
BOSE-007	6292-59-7	4-(tert-butyl)benzenesulfonamide
BOSE-008	150727-06-3	4-(tert-butyl)-N-(6-chloro-5-(2-methoxyphenoxy)-[2,2'-bipyrimidin]-4-yl)benzenesulfonamide
BOSE-022	1174918-30-9	4-(tert-butyl)-N-(5-(2-methoxyphenoxy)-6-(2-oxoethoxy)-[2,2'-bipyrimidin]-4-yl)benzenesulfonamide
BOSE-023	-	(2,2-dimethyl-1,3-dioxolane-4,5-diyl)dimethanol
BOSE-024	1448588-52-0	N,N'-((((2,2-dimethyl-1,3-dioxolane-4,5-diyl)bis(methylene))bis(oxy))bis(5-(2-methoxyphenoxy)-[2,2'-bipyrimidine]-6,4-diyl))bis(4-(tert-butyl)benzenesulfonamide)
BOSE-025	1448588-53-1	N,N'-(((2,3-dihydroxybutane-1,4-diyl)bis(oxy))bis(5-(2-methoxyphenoxy)-[2,2'-bipyrimidine]-6,4-diyl))bis(4-(tert-butyl)benzenesulfonamide)

ProcessRoute 3Steps 5 · Total yield 214.47 g

BOSE-006150728-13-5BOSE-0076292-59-7BOSE-013150728-12-4BOSE-014—BOSE-0157580-85-0BOSE-016—BOSE-017—API · Bosentan Hydrate

Code	CAS No.	Intermediate
BOSE-006	150728-13-5	4,6-dichloro-5-(2-methoxyphenoxy)-2,2'-bipyrimidine
BOSE-007	6292-59-7	4-(tert-butyl)benzenesulfonamide
BOSE-013	150728-12-4	5-(2-methoxyphenoxy)-[2,2'-bipyrimidine]-4,6(1H,5H)-dione
BOSE-014	-	potassium ((4-(tert-butyl)phenyl)sulfonyl)(6-chloro-5-(2-methoxyphenoxy)-[2,2'-bipyrimidin]-4-yl)amide
BOSE-015	7580-85-0	2-(tert-butoxy)ethanol
BOSE-016	-	N-(6-(2-(tert-butoxy)ethoxy)-5-(2-methoxyphenoxy)-[2,2'-bipyrimidin]-4-yl)-4-(tert-butyl)benzenesulfonamide
BOSE-017	-	2-((6-((4-(tert-butyl)phenyl)sulfonamido)-5-(2-methoxyphenoxy)-[2,2'-bipyrimidin]-4-yl)oxy)ethyl formate

Frequently asked questions

What are the approved indications of Bosentan Hydrate?

Approved indications include: 溃疡, Pulmonary arterial hypertension, Pulmonary hypertension, Systemic sclerosis.

When does the Bosentan Hydrate patent expire?

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

How many synthesis routes are recorded for Bosentan Hydrate?

5 synthesis routes are recorded; the shortest is 3 steps with 107 mg total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Bosentan Hydrate intermediates?

1 intermediate CAS of Bosentan Hydrate 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 Bosentan Hydrate 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) · 2026-09-27