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Buy Nalbuphine powder Cas 20594-83-6

Buy Nalbuphine powder Cas 20594-83-6

Nalbuphine, also known by its brand name Nubain, is a mixed opioid agonist-antagonist that exhibits both agonistic and antagonistic properties on opioid receptors. It is a pale yellow solid with potent analgesic effects, making it a valuable narcotic for pain management. Buy Nalbuphine powder Cas 20594-83-6

20594-83-6

  • Basic information

    1. Product Name: nalbuphine
    2. Synonyms: Nalbuphinebase;17-[Cyclobutylmethyl]-4,5α-epoxymorphinan-3,6α,14-triol;NALBUPNINE;Nalbuphine (base and/or unspecified salts);C07251;NETZHAKZCGBWSS-CEDHKZHLSA-N
    3. CAS NO:20594-83-6
    4. Molecular Formula: C21H27NO4
    5. Molecular Weight: 357.447
    6. EINECS: 243-901-6
    7. Product Categories: Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals
    8. Mol File: 20594-83-6.mol

  • Chemical Properties

    1. Melting Point: 230.5°
    2. Boiling Point: 566.6°Cat760mmHg
    3. Flash Point: 296.5°C
    4. Appearance: / Buy Nalbuphine powder Cas 20594-83-6
    5. Density: 1.44g/cm3
    6. Vapor Pressure: 1.35E-14mmHg at 25°C
    7. Refractive Index:Buy Nalbuphine powder Cas 20594-83-6
    8. Storage Temp.: Buy Nalbuphine powder Cas 20594-83-6
    9. Solubility: Buy Nalbuphine powder Cas 20594-83-6
    10. PKA: 9.39±0.60(Predicted)
    11. CAS DataBase Reference: nalbuphine(CAS DataBase Reference)
    12. NIST Chemistry Reference: nalbuphine(20594-83-6)
    13. EPA Substance Registry System: nalbuphine(20594-83-6)

  • Safety Data

    1. Hazard Codes: Buy Nalbuphine powder Cas 20594-83-6
    2. Statements:Buy Nalbuphine powder Cas 20594-83-6
    3. Safety Statements: Buy Nalbuphine powder Cas 20594-83-6
    4. WGK Germany: Buy Nalbuphine powder Cas 20594-83-6
    5. RTECS: Buy Nalbuphine powder Cas 20594-83-6
    6. HazardClass: Buy Nalbuphine powder Cas 20594-83-6
    7. PackingGroup: Buy Nalbuphine powder Cas 20594-83-6
    8. Hazardous Substances Data: 20594-83-6(Hazardous Substances Data)

20594-83-6 Suppliers

20594-83-6 Usage

Uses

Used in Pain Management:
Nalbuphine is used as an analgesic for the management of moderate to severe pain. Its unique mechanism of action allows it to provide effective pain relief without the risk of respiratory depression and addiction associated with full opioid agonists.
Used in Obstetrics:
In the field of obstetrics, nalbuphine is used as an analgesic during labor and delivery. Its mixed agonist-antagonist properties make it suitable for managing pain without causing excessive sedation or respiratory depression in both the mother and the newborn.
Used in Veterinary Medicine:
Nalbuphine is also used in veterinary medicine as an analgesic for managing pain in animals. Its safety profile and effectiveness make it a popular choice for treating post-operative pain and other painful conditions in various species.
Used in Detoxification and Withdrawal Management:
Due to its antagonistic properties, nalbuphine is used in the treatment of opioid dependence and withdrawal. It can help alleviate withdrawal symptoms and reduce cravings, making it a valuable tool in detoxification and addiction treatment programs.

Originator

Nubain,Du Pont,US,1979

Manufacturing Process

To a slurry of 110.5 g of 14-hydroxydihydronormorphinone in 2.5 liters of methylene chloride and 280 ml of triethylamine was added a solution of 106 g of cyclobutanecarboxylic acid chloride in 500 ml of methylene chloride. The temperature of the reaction mixture was maintained at 20°C to 25°C during the addition. After 5 minutes the reaction mixture was brought to reflux and heated for 5 hours.It was then cooled, washed with water, dried over sodium sulfate and evaporated to dryness. The residue was crystallized from benzene and pentane to give 138.5 g of the dicyclobutanecarbonyl derivative, melting point about 112°C (dec.).The dicyclobutanecarbonyl derivative (136.7 g) was dissolved in 200 ml of tetrahydrofuran and added dropwise to a suspension of 34.2 g of lithium aluminum hydride in 1 liters of tetrahydrofuran. The temperature of the mixture rose to reflux during the addition. Reflux was maintained for 2 hours after the addition was completed. After cooling, 110 ml of ethyl acetate was added dropwise, followed by 30 ml of water, followed by a solution of 53 g of ammonium chloride in 125 ml of water. The resulting mixture was filtered and the inorganic precipitate was washed with methanol. Evaporation of the combined filtrates gave 66 g of N-cyclobutylmethyl-14-hydroxydihydronormorphinone, melting point 229°C to 231°C.

Therapeutic Function

Analgesic

Check Digit Verification of cas no

The CAS Registry Mumber 20594-83-6 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 2,0,5,9 and 4 respectively; the second part has 2 digits, 8 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 20594-83:
(7*2)+(6*0)+(5*5)+(4*9)+(3*4)+(2*8)+(1*3)=106
106 % 10 = 6
So 20594-83-6 is a valid CAS Registry Number.

InChI:InChI=1/C21H27NO4.ClH/c23-14-5-4-13-10-16-21(25)7-6-15(24)19-20(21,17(13)18(14)26-19)8-9-22(16)11-12-2-1-3-12;/h4-5,12,15-16,19,23-25H,1-3,6-11H2;1H/t15-,16+,19?,20-,21+;/m0./s1

20594-83-6SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) – Sixth revised edition

Version: 1.0

Creation Date: Aug 12, 2017

Revision Date: Aug 12, 2017

1.Identification

1.1 GHS Product identifier

Product name nalbuphine

1.2 Other means of identification

Product number –
Other names Nalbufina

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier’s details

More Details:20594-83-6 SDS

20594-83-6Relevant academic research and scientific papers

Nalbuphine preparation method and intermediate thereof

–

Paragraph 0092; 0093, (2021/05/08)

The invention discloses a nalbuphine preparation method and an intermediate thereof, and the nalbuphine is prepared by taking morphine as a raw material through acylation, catalytic oxidation, palladium/carbon hydrogenation reduction, N-methyl removal of chloroformic acid-1-chloroethyl ester, hydrolysis deprotection and nitrogen-methylcyclobutane substitution. According to the method, a chiral center is introduced from an initial raw material, in the whole reaction process, reactions and reagents which can influence the chiral center are not adopted, only conventional methods and equipment are used in the whole reaction process, and the method is easy and convenient to operate, mild in condition, short in route, high in overall yield and suitable for industrial production.

Preparation method of nalbuphine free alkali

–

Paragraph 0010; 0017-0032, (2020/05/30)

The invention discloses a preparation method of nalbuphine free alkali, i.e., (-)-17-(cyclobutylmethyl)-4,5alpha-epoxymorphine-3,6alpha,14-hydroxyl. A synthetic route of the preparation method is shown in the specification. According to the novel method, a new reduction reaction condition is adopted, so the purity of nalbuphine free alkali in a reduction product reaches 99%, and the problems of excessive generation of 6-beta isomers of the reduction product and difficulty in purification of the free alkali are avoided.

One-Pot Process for Synthesis of Nalbuphine Hydrochloride and Impurity Control Strategy

Chen, Yibo,Wu, Zenong,Yang, Zhezhou,Zhang, Fuli,Zhang, Tao,Zhao, Weili

, p. 1707 – 1717 (2020/12/01)

An improved kilogram-scale process of synthesis of nalbuphine was developed by investigating the critical parameters. Ten process-related impurities were identified, of which the source and control strategy was elucidated. Moreover, tetramethylammonium triacetoxyborohydride (Me4NBH(OAc)3) was developed to reduce the imine and ketone in one pot. As a result, 6-β-epimer was significantly controlled to only 0.08% in the crude nalbuphine. The improved process was robust at kilogram scale in 60.4% overall yield with 99.95% high-performance liquid chromatography (HPLC) purity.

PROCESS FOR OBTAINING 3,14-DIACETYLOXYMORPHONE FROM ORIPAVINE

–

, (2018/01/17)

The present invention relates to a new process for obtaining 3,14-diacetyloxymorphone from oripavine, a process to transform the obtained 3,14-diacetyloxymorphone into a noroxymorphone and a process to transform said noroxymorphone into naloxone, naltrexone, nalbuphine, nalfurafine or nalmefene.

CONVENIENT PREPARATION OF N-SUBSTITUTED MORPHINAN-6-OLS FROM MORPHINAN-6-ONES

–

Paragraph 0095, (2015/05/13)

Described herein are methods of preparing 6-hydroxy N-alkyl morphinan-6-ols from morphinan-6-ones, as illustrated below: wherein the variables R1, R2, R3, R10, R11, R14, and are as defined herein and wherein the reactions occur in a one-pot procedure using a boron based reducing agent.

General method of synthesis for naloxone, naltrexone, nalbuphone, and nalbuphine by the reaction of grignard reagents with an oxazolidine derived from oxymorphone

Endoma-Arias, Mary Ann A.,Cox, D. Phillip,Hudlicky, Tomas

, p. 1869 – 1873 (2013/07/19)

The N-oxide of O-acyloxymorphone, when treated with the Burgess reagent, provides the corresponding oxazolidine in a one-pot sequence and in excellent yield. The oxazolidine derived from oxymorphone, temporarily protected at O-3 and C-6, reacts with Grignard reagents to provide directly N-allyl, N-cyclopropylmethyl, and N-cyclobutylmethyl derivatives that are further converted to the title compounds, namely naltrexone, naloxone, nalbuphone, and nalbuphine in excellent yields. Each of these medicinal agents is obtained from the oxazolidine in a one-pot sequence. Complete spectral and experimental data are provided for all compounds. Copyright

PROCESS FOR THE PREPARATION OF MORPHINE ANALOGS VIA THE REACTION OF ORGANOMETALLIC REAGENTS WITH AN OXAZOLIDINE DERIVED FROM MORPHINANS

–

Paragraph 0081, (2013/08/15)

The oxazolidine derived from the reaction of oxymorphone with the Burgess reagent, temporariiy protected at 0-3 and C-6, reacts with Grignard or other suitable metallic or organometallic reagents to directly provide, for example, A/-allyl, A/-methylcyclopropyl and /V-methylcyclobutyl derivatives that are further converted into naltrexone, naloxone, nalbuphone and nalbuphine in excellent yields. These morphine analogs can be prepared from the oxazolidine in a one- pot synthesis.

PROCESS FOR REDUCING THE 6-KETO GROUP OF A MORPHINAN ALKALOID TO THE 6-HYDROXY GROUP BY HYDROGENATION

–

Page/Page column 4, (2011/04/13)

The present invention relates to a process for the reduction of a 6-keto group in a morphinan alkaloid to the corresponding 6-hydroxy group, comprising hydrogenating the 6-keto group using gaseous hydrogen in the presence of a heterogeneous catalyst and a solvent, to yield the 6-hydroxy morphinan alkaloid, wherein the reduction is carried out at a pH in the range of about 5 to about 7, and the 6-hydroxy morphinan alkaloid has an α:β ratio of > 85: 15.

PROCESS FOR MAKING MORPHINAN-6alpha-OLS

–

Page/Page column 6, (2010/03/02)

The present invention provides a process whereby morphinan-6-ones can be converted stereospecifically to the corresponding morphinan-6α-ols by catalytic hydrogenation under basic conditions.

PROCESSES FOR THE PREPARATION OF MORPHINANE AND MORPHINONE COMPOUNDS

–

Page/Page column 70, (2010/11/05)

The present application describes processes for the synthesis of morphinane and morphinone compounds, useful as pharmaceutical agents. Also included are novel intermediates useful in the preparation of these compounds. The process comprises quaternization of oripavine to provide a mixture of the R- and S-isomeric (at the nitrogen) quaternary salts. The R-isomer is readily isolated and converted to various N-(R)-morphinane and N-(S)-morphinone compounds. The R-isomer, S-isomer or a mixture of R- and S-isomers may be demethylated and converted to various morphinane and morphinone compounds.

Nalbuphine, sold under the brand names Nubain among others, is an opioid analgesic which is used in the treatment of pain.[6][10][8] It is given by injection into a vein, muscle, or fat.[6][8]

Side effects of nalbuphine include sedation, sweatiness, clamminess, nausea, vomiting, dizziness, vertigo, dry mouth, and headache.[10] Unlike other opioids, it has little to no capacity to cause euphoria or respiratory depression.[6][10] There is also little to no incidence of dysphoria, dissociation, hallucinations, and related side effects at typical therapeutic doses.[6][10] Nalbuphine is a mixed agonist/antagonist opioid modulator.[6][10] Specifically, it acts as a moderate-efficacy partial agonist or antagonist of the μ-opioid receptor (MOR) and as a high-efficacy partial agonist of the κ-opioid receptor (KOR), whereas it has relatively low affinity for the δ-opioid receptor (DOR) and sigma receptors.[11][10]

Nalbuphine was patented in 1968[12] and was introduced for medical use in the United States in 1979.[13][14] It is marketed in many countries throughout the world.[15]

Medical uses

Nalbuphine is indicated for the relief of moderate to severe pain. It can also be used as a supplement to balanced anesthesia, for preoperative and postoperative analgesia, and for obstetrical analgesia during labor and delivery. However, a 2014 Cochrane Systematic Review concluded that from the included studies, there was limited evidence to demonstrate that “0.1 to 0.3 mg/kg nalbuphine compared to placebo might be an effective postoperative analgesic” for pain treatment in children.[16] Further research is therefore needed to compare nalbuphine with other postoperative opioids.[16]

In addition to relieving pain, nalbuphine has been shown to reduce morphine-induced pruritus (itching).[17] Pruritus is a common side effect of morphine and other pure μ-opioid receptor (MOR) agonists. A systematic review of clinical trials concluded that nalbuphine is effective in counteracting morphine-induced pruritus, likely through central nervous system mechanisms.[18]

Evidence suggests that κ-opioid receptor (KOR) activation can counteract MOR-mediated effects in the brain.[19] This interaction may have broader implications for central nervous system disorders, including potential applications in treating Parkinson’s disease, where KOR agonism and MOR antagonism have been shown to reduce levodopa-induced dyskinesia and normalize striatal function.[20]

Morphine-induced pruritus may also result from histamine release by mast cells in the skin.[21] Both MORs and KORs are expressed in skin nerves and keratinocytes, indicating potential peripheral mechanisms for opioid-induced pruritus.[22] Histamine-mediated responses such as increased capillary permeability and vasodilation have been observed following intradermal administration of some opioids. However, nalbuphine does not elicit either a wheal or flare response, suggesting it does not promote histamine release from mast cells.[23]

Available forms

Nalbuphine is available in two concentrations, 10 mg and 20 mg of nalbuphine hydrochloride per mL. Both strengths contain 0.94% sodium citrate hydrous, 1.26% citric acid anhydrous, 0.1% sodium metabisulfite, and 0.2% of a 9:1 mixture of methylparaben and propylparaben as preservatives; pH is adjusted, if necessary, with hydrochloric acid. The 10 mg/mL strength contains 0.1% sodium chloride. The drug is also available in a sulfite and paraben-free formulation in two concentrations, 10 mg and 20 mg of nalbuphine hydrochloride per mL. One mL of each strength contains 0.94% sodium citrate hydrous, 1.26% citric acid anhydrous; pH is adjusted, if necessary, with hydrochloric acid. The 10 mg/mL strength contains 0.2% sodium chloride.[citation needed]

An investigational extended-release oral formulation is under development by Trevi Therapeutics.[24][independent source needed]

Side effects

A 2014 Cochrane Systematic Review by Schnabel et al., concluded that due to limited data, analysis of adverse events for children treated with nalbuphine compared to other opioids or placebo for postoperative pain, could not be definitively reported.[16]

Overdose

In case of overdose or adverse reaction, the immediate intravenous administration of naloxone (Narcan) is a specific antidote. Oxygen, intravenous fluids, vasopressors and other supportive measures should be used as indicated.[25] When administered concurrently with naloxone, nalbuphine is also useful for treating overdoses of potent opioids such as fentanyl, and its highly potent derivatives such as remifentanil and sufentanil, when naloxone alone is insufficient.[26]

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