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

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

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 
• 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 
• 774513-65-4 17-cyclopropylmethyl-4,5α-epoxy-3,14β-dihydroxy-6β-(N-methylbenzamido)morphinan 

Relevant articles and documents

NOVEL MORPHINANS USEFUL FOR TREATING MEDICAL DISORDERS

The present invention related to novel morphinans, compositions comprising the novel morphinans, and their uses as agonists of the kappa opioid receptor.

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

SYNTHESIS OF METABOLICALLY STABLE AGENTS FOR ALCOHOL AND DRUG ABUSE

Disclosed herein are compounds of formula (I); as defined herein, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same, and methods of using these compounds for the treatment of substance addiction.

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.

Morphinan derivative and its pharmaceutical applications

A morphinan derivative or its pharmacologically allowed acid addition salt represented with compound I, an analgesic and diuretic having its derivative or its salt as the active ingredient, and its production process are described. The compound of the present invention possesses strong analgesic activity and diuretic action as a highly selective κ-opioid agonist, allowing it to be used as a useful analgesic and diuretic.

Brain cell protective agent

The present invention relates to a novel brain cell protective agent having for its active ingredient a morphinan derivative represented with Compound 1 STR1 or pharmacologically acceptable acid addition salt thereof. The compounds used in the present inv

Antitussive agents

There are provided novel antitussive agents different from existing antitussive agents or those under development. Antitussive agents containing morphinan derivatives represented by compound 6: STR1 or pharmacologically acceptable acid-addition salts thereof and those derivatives or their salts as effective components. The antitussive agents according to the present invention have strong antitussive effects as highly selective κ-opioid agonists, and may thus be applied as useful antitussive agents in the prophylaxis and treatment of coughing in a patient in need thereof.