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溴化甲基纳曲酮

Tier C — Watch / trade

Methylnaltrexone Bromide

Progenics Pharmaceuticals Inc
Originator
2008
First approval
-
Expiry (public)
$0.11B ▲
Peak sales
化学药
Type

Targets：MOR1

Brand：Relistor

Indications (approved)：阿片类依赖、便秘、阿片类药物引起的便秘

Regional status

US
批准上市
2008-04-24
EU
批准上市
2008-07-01
China
临床一期
2023-12-15
Japan
-

Synthetic routes & intermediates5 routes

Originator routes × 1Optimised (non-patent) × 4Process 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 1 · Total yield 45 g
Synthetic routes & intermediates Route 1
CodeCAS No.Intermediate
METHB-00116590-41-3(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,3,4,4a,5,6-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7aH)-one
OptimisedRoute 2Steps 4 · Total yield 22.5 g
Synthetic routes & intermediates Route 2
CodeCAS No.Intermediate
METHB-00116590-41-3(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,3,4,4a,5,6-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7aH)-one
METHB-00233522-95-1(4R,4aS,7aR,12bS)-4a,9-dihydroxy-2,3,4,4a,5,6-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7aH)-one
METHB-0037051-34-5(bromomethyl)cyclopropane
METHB-004836602-51-8(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a-hydroxy-7-oxo-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-9-yl ethyl carbonate
METHB-0051082510-80-2(3S,4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-9-((ethoxycarbonyl)oxy)-4a-hydroxy-3-methyl-7-oxo-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-3-ium methyl sulfate
OptimisedRoute 3Steps 5 · Total yield 4.3 g
Synthetic routes & intermediates Route 3
CodeCAS No.Intermediate
METHB-00116590-41-3(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,3,4,4a,5,6-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7aH)-one
METHB-0037051-34-5(bromomethyl)cyclopropane
METHB-00652446-24-9(4R,4aS,7aR,12bS)-4a,9-dihydroxy-2,3,4,4a,5,6-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7aH)-one hydrochloride
METHB-007153567-11-4(4R,4aS,7aR,12bS)-9-(benzyloxy)-3-(cyclopropylmethyl)-4a-hydroxy-2,3,4,4a,5,6-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7aH)-one
METHB-0081013912-16-7(3S,4R,4aS,7aR,12bS)-9-(benzyloxy)-3-(cyclopropylmethyl)-4a-hydroxy-3-methyl-7-oxo-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-3-ium methyl sulfate
METHB-0091013912-02-1(3S,4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-3-methyl-7-oxo-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-3-ium methyl sulfate
OptimisedRoute 4Steps 3 · Total yield 74.2 g
Synthetic routes & intermediates Route 4
CodeCAS No.Intermediate
METHB-00116590-41-3(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,3,4,4a,5,6-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7aH)-one
METHB-01096453-52-0(4R,4aS,7aR,12bS)-9-((tert-butyldimethylsilyl)oxy)-3-(cyclopropylmethyl)-4a-hydroxy-2,3,4,4a,5,6-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7aH)-one
METHB-0111250269-27-2(3S,4R,4aS,7aR,12bS)-9-((tert-butyldimethylsilyl)oxy)-3-(cyclopropylmethyl)-4a-hydroxy-3-methyl-7-oxo-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-3-ium carbonate
OptimisedRoute 5Steps 3 · Total yield 5.2 g
Synthetic routes & intermediates Route 5
CodeCAS No.Intermediate
METHB-00116590-41-3(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,3,4,4a,5,6-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7aH)-one
METHB-01292398-33-9(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a-hydroxy-9-((2-(trimethylsilyl)ethoxy)methoxy)-2,3,4,4a,5,6-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7aH)-one
METHB-0131446094-54-7(3S,4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a-hydroxy-3-methyl-7-oxo-9-((2-(trimethylsilyl)ethoxy)methoxy)-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-3-ium iodide

Frequently asked questions

What are the approved indications of Methylnaltrexone Bromide?

Approved indications include: 阿片类依赖, 便秘, 阿片类药物引起的便秘.

When does the Methylnaltrexone Bromide patent expire?

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

How many synthesis routes are recorded for Methylnaltrexone Bromide?

5 synthesis routes are recorded; the shortest is 1 steps with 45 g total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Methylnaltrexone Bromide intermediates?

All intermediates in Methylnaltrexone Bromide 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 Methylnaltrexone Bromide 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