7 results about "Thebaine" patented technology

The present application provides a method for determining the content of codeine, morphine, papaverine, narcotine and thebaine in poppy oil, and belongs to the technical field of detection methods. The method comprises the following steps: (1) preparation of an isotopic internal standard working solution; (2) adding an adsorbent to the poppy oil sample, stirring and adsorbing, filtering, adding the solid into a solvent, heating and desorbing, filtering, washing, combining the washing liquid and the filtrate, adding the isotopic internal standard working solution, filtering, constant volume, and preparing a test sample solution; (3) preparation of a control stock solution; (4) preparation of a control sample solution; (5) determination of the content of codeine, morphine, papaverine, narcotine and thebaine in poppy oil by LC-MS / MS. The present application uses a simple and effective method to determine the content of codeine, morphine, papaverine, narcotine and thebaine in poppy oil, has a larger linear range, a lower detection limit, a high accuracy, a high sensitivity, and a good linearity, and is a reliable and effective detection method.

The invention relates to a tetrahydrothebaine derivative as well as a preparation method and application thereof, in particular to a 7alpha-(4 '-substituted amidophenyl)-6alpha, 14alpha-endo-ethylidene (alkenyl)-tetrahydrothebaine derivative as shown in a general formula (I) or pharmaceutically acceptable salts thereof and a preparation method of the 7alpha-(4'-substituted amidophenyl)-6alpha, 14alpha-endo-ethylidene (alkenyl)-tetrahydrothebaine derivative. And to the use of such derivatives in the preparation of medicaments for the treatment and / or prevention of pain, irritable bowel syndrome, pruritus, addiction, depression. The derivative disclosed by the invention has a remarkable improvement effect in the aspects of agonistic activity of the kappa opioid receptor, subtype selectivity of the kappa opioid receptor and central safety.

The invention discloses a preparation method of a buprenorphine hydrochloride key intermediate, particularly provides an improved method for preparing 7 alpha [(S)-1-hydroxy-1, 2, 2-trimethylpropyl]-6, 14-diethylidene-6, 7, 8, 14-tetrahydrothebaine, and belongs to the technical field of medical intermediates. The compound is a key intermediate for synthesizing buprenorphine hydrochloride. The solid of the key intermediate is obtained with high yield and high purity through the method, and the method is simple and convenient to operate and suitable for industrial production.

The application belongs to the field of pharmacy, discloses a fused ring morphine derivative and a preparation method and application thereof, and relates to N-cyclopropylmethyl-4'-substituted aminonalepotem series derivatives with formula (I) and pharmaceutically acceptable salts. The derivative with formula (I) is prepared by reacting thebaine with a substituted phenyl vinyl ketone reagent and through a series of conversion methods. Among them, N-cyclopropylmethyl-(4'-benzoyl amino) nalepotem (SLL-1062) is a typical high selectivity mu opioid receptor antagonist, and can be applied to the research and development in the fields of diagnosis and treatment of opioid and other narcotic analgesic dependence, opioid drug-induced intestinal dysfunction, sedative hypnotics and acute alcohol poisoning, opioid and other narcotic analgesic poisoning and the like.

This application relates to a 7α-substituted phenyltetrahydrothebaine derivative, its preparation method, and its uses. Specifically, it relates to a 7α-substituted phenyltetrahydrothebaine derivative as shown in general formula (I) or a pharmaceutically acceptable salt thereof, and its preparation method, and to the use of such derivatives in the preparation of analgesic, anti-anxiety, anti-addiction, and antidepressant drugs. The derivatives of this invention exhibit significantly enhanced agonist activity and subtype selectivity of δ-opioid receptors.

The invention provides a method for determining the contents of codeine, morphine, papaverine, narcotine and thebaine in poppy oil, and belongs to the technical field of detection methods. Comprising the following steps: (1) preparing an isotope internal standard working solution; (2) adding an adsorbent into the opium poppy oil sample, stirring for adsorption, filtering, adding a solid into a solvent, heating for desorption, filtering, washing, combining a washing solution and a filtrate, adding an isotope internal standard working solution, filtering, and fixing the volume to obtain a test solution; (3) preparing a control stock solution; (4) preparing a reference substance solution; and (5) determining the contents of codeine, morphine, papaverine, narcotine and thebaine in the opium poppy oil by adopting LC-MS / MS (Liquid Chromatography-Mass Spectrometry / Mass Spectrometry). The simple and effective method is adopted for determining the contents of codeine, morphine, papaverine, narcotine and thebaine in the opium poppy oil, the linear range is large, the detection limit is low, the accuracy rate is high, the sensitivity is high, the linearity is good, and the method is a reliable and effective detection method.

This application relates to a 7α-substituted piperazine morphine derivative, its preparation method, and its uses. Specifically, it relates to 7α-(N-substituted piperazine)-tetrahydrothebaine derivatives as shown in general formula (I) or pharmaceutically acceptable salts thereof, and their preparation methods. Furthermore, it relates to the use of such derivatives in the preparation of analgesic, anti-irritable bowel syndrome, antipruritic, anti-addictive, and antidepressant drugs. The derivatives described in this invention exhibit significantly enhanced κ-receptor agonist activity and κ-receptor subtype selectivity.