- Atropine hapten and synthesis method thereof, antigen, antibody and application
-
The invention discloses an atropine hapten and a synthesis method thereof, an antigen, an antibody and an immunodetection device which is convenient to use, rapid, simple and convenient to operate, high in sensitivity and accuracy, and capable of measuring atropine on site. The atropine hapten has a structure as shown in a formula (I) which is described in the specification. The atropine hapten provided by the invention is a proper atropine hapten which is prepared by using nortropine as a raw material and can be more fully exposed to an immune system of an animal. The atropine hapten is coupled with a carrier protein to prepare the artificial antigen; and the atropine artificial antigen is used for immunizing animals, and the monoclonal antibody with high specificity to atropine is prepared by adopting a cell fusion technology.
- -
-
Paragraph 0037; 0040-0041; 0048; 0050; 0054; 0056
(2020/05/01)
-
- Insertion of Alkylidene Carbenes into B-H Bonds
-
We have developed a protocol for insertion of alkylidene carbenes into the B-H bonds of amine-borane adducts, enabling, for the first time, the construction of C(sp2)-B bonds by means of carbene-insertion reactions. Various acyclic and cyclic alkenyl borane-amine adducts were prepared from readily accessible starting materials in good to high yields and were subsequently subjected to a diverse array of functional group transformations. The unprecedented spiro B-N heterocycles prepared in this study have potential utility as building blocks for the synthesis of pharmaceuticals. Preliminary mechanistic studies suggest that insertion of the alkylidene carbenes into the B-H bonds of the amine-borane adducts proceeds via a concerted process involving a three-membered-ring transition state.
- Yang, Ji-Min,Guo, Feng-Kai,Zhao, Yu-Tao,Zhang, Qiao,Huang, Ming-Yao,Li, Mao-Lin,Zhu, Shou-Fei,Zhou, Qi-Lin
-
supporting information
p. 20924 - 20929
(2020/12/23)
-
- A new method for preparing ipratropine (by machine translation)
-
The invention discloses a ipratropine preparation method, comprises the following steps: benzene acetic acid methyl ester (III) as the starting material, the reaction process for preparing substituted α - formyl benzene acetic acid methyl ester (IV); tropine is mellow with methyl bromide reaction to prepare the compound (II); compound (II) with a compound (IV) reaction of compounds (V), compound (V) reduction process of preparing ipratropine anhydride, through the refining preparation ipratropine (VII), the method is simple in operation, high safety, low cost, is more suitable for industrial production. (by machine translation)
- -
-
Paragraph 0041
(2017/09/02)
-
- Study on the synthesis and biological activities of α-substituted arylacetates derivatives
-
Anisodamine was isolated from the medicinal herb, it was used in the treatment of gastrointestinal smooth muscle spasm, infective toxic shock and organophosphorus intoxication. But there is no report about anisodamine with α-glucosidase inhibitory activity. In order to find novel α-glucosidase inhibitors, a series of α-substituted arylacetates derivatives have been synthesized based on the active unit of anisodamine. In α-glucosidase assay, compound 9 in Schiff base form and compound 22 in ester form show strong inhibition against α-glucosidase with IC50value of 46.81?μM and 83.76?μM, respectively. Compounds 9 and 22 exhibit comparable good antidiabetic activities as commercial drug Glimepiride. In addition, Schiff bases of α-substituted arylacetates show antitumor activities against human cancer cell lines, where compound 9 with thiourea moiety performs the best antitumor activity. We anticipate that our research will provide potential candidate scaffolds for antidiabetic drug design.
- Liu, Jinbing,Chen, Changhong,Wu, Fengyan,Tang, Junyuan
-
supporting information
p. 1715 - 1719
(2016/07/27)
-
- Diastereospecific nazarov cyclization of fully substituted dienones: Generation of vicinal all-carbon-atom quaternary stereocenters
-
No vacancy: Fully substituted dienones that are highly polarized by a vinylogous carbonate group were found to undergo a remarkably rapid and diastereospecific Nazarov cyclization that led to cyclopentenones with vicinal all-carbon-atom quaternary centers (see example; SEM=2-(trimethylsilyl) ethoxymethyl, Tf=trifluoromethanesulfonyl). Copyright
- Jolit, Anais,Vazquez-Rodriguez, Saleta,Yap, Glenn P. A.,Tius, Marcus A.
-
supporting information
p. 11102 - 11105
(2013/10/22)
-
- Sigmatropic rearrangement of ammonium ylideskey step in the synthesis of methyl 2-formylphenyl acetate
-
N-Cyanomethyl-N,N-dimethyl-N-(-methoxycarbonyl)benzylammonium salts 5 were synthesized and treated with different base/solvent systems, giving the products of sigmatropic rearrangements [2,3] 7 and [1,2] 8. In reactions carried out in liquid ammonia, [2,3] rearrangement definitively prevailed. Pure 7(or mixture of 7 and 8) were deprotected to afford methyl 2-formylphenyl acetate (9) in good yield.
- Kowalkowska, Anna,Jonczyk, Andrzej
-
scheme or table
p. 3308 - 3317
(2011/09/21)
-
- Regioselective and stereoselective glycidic oxirane ring opening: A new entry to optically pure α-alkyl α-hydroxy β-amino acid derivatives
-
The BF3·OEt2 catalyzed oxirane ring opening of glycidic esters or amides with acetonitrile afforded the corresponding 2-oxazolines under very mild conditions in good yields. The reactions are completely regioselective (the nitrogen attacks the β-carbon) and stereoselective (with inversion of configuration) starting from 2-alkyl or 2,3-dialkyl glycidic derivatives, but the stereoselectivity is lost and the regioselectivity is completely inverted from 2-aryl derivatives. The 2-oxazolines obtained are readily hydrolyzed into β-amino, α-hydroxy esters or amides. (C) 2000 Elsevier Science Ltd.
- García Ruano, Jose L.,García Paredes, Cristina
-
p. 5357 - 5361
(2007/10/03)
-
- Flash Photolytic Decarbonylation and Ring-Opening of 2-(N-(Pentafluorophenyl)amino)-3-phenylcyclopropenone. Isomerization of the Resulting Ynamine to a Ketenimine, Hydration of the Ketenimine, and Hydrolysis of the Enamine Produced by Ring-Opening
-
Flash photolysis of 2-(N-(pentafluorophenyl)amino)-3-phenylcyclopropenone, 4, in aqueous solution was found to produce N-(pentafluorophenyl)phenylethynamine, 3, by the expected photodecarbonylation reaction and also 2-phenyl-3-(N-(pentafluorophenyl)amino)acrylic acid, 5, by an apparently unprecedented photochemical ring-opening process. The ynamine underwent rapid isomerization to N-(pentafluorophenyl)phenylketenimine, 9, by an acid-catalyzed route that involves rate- determining proton transfer to the β-carbon atom of the ynamine and also by a base-catalyzed route involving equilibrium ionization of the N-H bond of the ynamine to give an ynamide ion followed by rate-determining β-carbon protonation of this ion. Saturation of the base catalysis allowed determination of the acidity constant of the ynamine; the result, pQa = 10.23, makes this amine a remarkably strong nitrogen acid. Hydration of the ketenimine 9 gave N-(pentafluorophenyl)phenylacetamide, 6, as the ultimate product produced by this reaction route, and hydrolysis of the aminoacrylic acid 5 gave pentafluoroaniline, 7, and 2-phenylformylacetic acid, 10, which underwent decarboxylation to phenylacetaldehyde, 8, as the ultimate products of this route.
- Chiang,Grant,Guo,Kresge,Paine
-
p. 5363 - 5370
(2007/10/03)
-
