102869-99-8

Basic information

• Product Name: (5α,6β)-17-(CyclopropylMethyl)-4,5-epoxy-6-(MethylaMino)-Morphinan-3,14-diol
• Synonyms: Des-N-(3-furanyl-2-propenaMide) Nalfurafine;(4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-7-(methylamino)-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,9-diol
• CAS NO: 102869-99-8
• Molecular Formula: C₂₁H₂₈N₂O₃
• Molecular Weight: 356.45862
• Product Categories: Intermediates & Fine Chemicals;Metabolites & Impurities;Pharmaceuticals
• Mol File: 102869-99-8.mol
• Article Data: 8

Chemical Properties

• Boiling Point: 541.6±50.0 °C(Predicted)
• Appearance: /
• Density: 1.38±0.1 g/cm3(Predicted)
• PKA: 9.44±0.60(Predicted)
• CAS DataBase Reference: (5α,6β)-17-(CyclopropylMethyl)-4,5-epoxy-6-(MethylaMino)-Morphinan-3,14-diol(CAS DataBase Reference)
• NIST Chemistry Reference: (5α,6β)-17-(CyclopropylMethyl)-4,5-epoxy-6-(MethylaMino)-Morphinan-3,14-diol(102869-99-8)
• EPA Substance Registry System: (5α,6β)-17-(CyclopropylMethyl)-4,5-epoxy-6-(MethylaMino)-Morphinan-3,14-diol(102869-99-8)

Safety Data

• Hazardous Substances Data: 102869-99-8(Hazardous Substances Data)

Usage

Description

(5α,6β)-17-(CyclopropylMethyl)-4,5-epoxy-6-(MethylaMino)-Morphinan-3,14-diol is a white solid compound that serves as an opioid receptor antagonist. It plays a crucial role in the development of opioid κ-agonist TRK-820 and other related compounds.

Uses

Used in Pharmaceutical Industry:
(5α,6β)-17-(CyclopropylMethyl)-4,5-epoxy-6-(MethylaMino)-Morphinan-3,14-diol is used as an opioid receptor antagonist for the preparation of opioid κ-agonist TRK-820 and other related compounds. Its antagonistic properties allow it to modulate the activity of opioid receptors, which can be beneficial in the treatment of various medical conditions.

Upstream product

• 16590-41-3 Naltrexone 
• 74-89-5 methylamine 
• 593-51-1 methylamine hydrochloride 
• 75768-72-8 naltrexone hydrochloride 

Downstream Products

• 152657-84-6 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan 
• 774513-65-4 17-cyclopropylmethyl-4,5α-epoxy-3,14β-dihydroxy-6β-(N-methylbenzamido)morphinan 
• 152657-77-7 N-[(5R,6R)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-phenyl-N-methylpropanamide hydrochloride 
• 152658-57-6 N-[(4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,3,4,4a,5,6,7,7a octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]-N-methylcinnamamide hydrochloride 
• 152658-17-8 nalfurafine hydrochloride 
• 152658-01-0 (2E)-N-[(5R,6R)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-methylphenyl)-N-methylprop-2-enamide hydrochloride 
• 152657-71-1 N-[(5R,6R)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-2-(3,4-dichlorophenyl)-N-methylacetamide hydrochloride 

Relevant articles and documents

Activity of N-methyl-α- and -β-funaltrexamine at opioid receptors

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Crystals of morphinan derivative, manufacturing method thereof, and pharmaceutical composition using the same

The present invention relates to a X-form crystal of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride and the manufacturing method thereof, wherein the X-form crystal of the compound has char

Morphinan derivatives and pharmaceutical use thereof

A morphinan derivative or its pharmaceutically acceptable acid addition salt represented with, for example, and an analgesic, diuretic, antitussive and brain cell protector having its derivative or its salt as the active ingredient are described. The compound of the present invention possesses strong analgesic activity, diuretic action and antitussive action as a highly selective κ-opioid agonist, allowing it to be used as a useful analgesic, diuretic and antitussive. On the other hand, the compound of the present invention also possesses remarkable cerebro-neuroprotective activity, thus allowing it be used as a useful cerebro-neuroprotective agents.