Nalbuphine preparation method and intermediate thereof
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.
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Paragraph 0063-0071
(2021/05/08)
Synthetic method of morphine derivative and applications
The invention discloses a synthetic method of a morphine derivative. The method employs morphine as an initial raw material, and selective protection and glycosylation are carried out in order to obtain a target product. The HPLC purity of M3G obtained by the synthetic method reaches 99.8%, and the M3G can be used as a reference substance or a standard substance for researching quality of relatedproducts.
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Paragraph 0062-0063
(2018/05/07)
6-ACETYLMORPHINE ANALOGS, AND METHODS FOR THEIR SYNTHESIS AND USE
The present invention relates to novel 6-acetylmorphine analogs, and methods for their synthesis and use. Such analogs are designed to provide a convenient linkage chemistry for coupling under mild conditions to a suitable group on a target protein, polypeptide, solid phase or detectable label.
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Paragraph 0094; 00134
(2014/10/04)
6-O-Glycosylation of morphine derivatives using thioglycosides as glycosyl donors
A novel approach was developed for the synthesis of the pharmaceutically important morphine and dihydromorphine 6-β-D-glucuronides. The key step involves a selective 6-O-glycosylation of 3-O-protected morphines and dihydromorphines with thioglycosides that serve as glycosyl donors in the presence of thiophilic promoters. This novel approach may be useful for the O-glycosylation of other alkoloid derivatives.
Rukhman,Yudovich,Nisnevich,Gutman
p. 1241 - 1246
(2007/10/03)
Selective Aminolysis of Benzoates and Acetates of α-Hydroxy Acids and Phenols with Benzylamine and Butan-1-amine
Benzoates and acetates of α-hydroxy acids and phenols undergo facile aminolysis on treating with benzylamine or butan-1-amine in benzene at room temperature.Under the same conditions acetates and benzoates of alcohols are unaffected.
Bell, Kevin H.
p. 1723 - 1735
(2007/10/02)
Ligand determination of spin labeled compounds by receptor displacement
Compounds are provided for use in assays of organic compounds, where organic compounds of biological interest are determined at extremely low concentrations by combining in a medium, the composition to be determined, hereinafter referred to as ligand, a high molecular weight material of at least 10,000 molecular weight, which has a site spatially characterisitc of the ligand, hereinafter referred to as receptor, and an analog of the ligand having a free radical functionality hereinafter referred to as "ligand analog". The ligand analog and ligand in the medium compete for the receptor site, the amount of ligand analog bound to the receptor, being dependent on the amount of ligand present in the medium. By following the change in electron spin resonance spectrum of the ligand analog and comparing it to the change in spectrum which would be obtained in the absence of any ligand, the amount of ligand can be determined.
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(2008/06/13)
Spin labeled compounds
Compounds are provided for use in assays of organic compounds, where organic compounds of biological interest are determined at extremely low concentrations by combining in a medium, the composition to be determined, hereinafter referred to as ligand, a high molecular weight material of at least 10,000 molecular weight, which has a site spatially characteristic of the ligand, hereinafter referred to as receptor, and an analog of the ligand having a free radical functionality, hereinafter referred to as "ligand analog". The ligand analog and ligand in the medium compete for the receptor site, the amount of ligand analog bound to the receptor, being dependent on the amount of ligand present in the medium. By following the change in electron spin resonance spectrum of the ligand analog and comparing it to the change in spectrum which would be obtained in the absence of any ligand, the amount of ligand can be determined.
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(2008/06/13)
INVESTIGATIONS ON THE BIOSYNTHESIS OF MORPHINE ALKALOIDS.