- A convenient method for the preparation of α-ketoacetals
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A convenient method for the preparation of α-ketoacetal derivatives 2a-g was developed by addition of Grignard reagent (1a-g) to commercially available ethyl diethoxyacetate (3) in 60-96% yield.
- Adamczyk, Maciej,Johnson, Donald D.,Mattingly, Phillip G.,Pan, You,Reddy, Rajarathnam E.
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- Bisdeoxycoelenterazine derivatives for improvement of bioluminescence resonance energy transfer assays
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We report here syntheses of bisdeoxycoelenterazine derivatives that show significantly improved kinetics of the bioluminescent reaction. All derivatives contain a protecting group at the carbonyl group of the imidazopyrazinone moiety that ensures slower light signal decay. The longer lasting light signal offers the possibility of real-time imaging of protein-protein interactions. Copyright
- Levi, Jelena,De, Abhijit,Cheng, Zhen,Gambhir, Sanjiv Sam
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- Deuterated compound based on cavity enterostatin - h as well as preparation method and application thereof
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The invention discloses a deuterated compound based on caescein - h, a preparation method and application thereof, and the chemical structural formula is as follows. In-flight R1 Phenyl or deuterated phenyl groups R2 Hydrogen or deuterium, R3 Hydrogen or deuterium, R4 Hydrogen or deuterium, R5 Hydrogen or deuterium, R6 Hydrogen or deuterium, R1 -R6 At least one group in the group is a deuterated group. The deuterated compound provided by the invention is used as a biological luminescent substrate, and can monitor the distribution of luciferase in vivo and outside. Compared with the cavity enterostatin - h, the method for preparing the deuterated compound of the cavity enterostatin - is simple, the reaction steps are classic, the operability is high, the cost - h is low, and the method has a good practical value.
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Paragraph 0028; 0066; 0073-0074
(2021/11/26)
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- HETEROARYL DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSTION FOR PREVENTING OR TREATING DISEASES ASSOCIATED WITH PI3 KINASES, CONTAINING SAME AS ACTIVE INGREDIENT
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The present invention relates to a heteroaryl derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition for preventing or treating diseases associated with PI3 kinases, containing the same as an active ingredient. The heteroaryl derivative according to the present invention has an excellent effect of selectively inhibiting PI3 kinases, thereby being useful in preventing or treating PI3 kinase diseases such as: cancers, autoimmune diseases, and respiratory diseases.
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Paragraph 0729-0731
(2018/04/26)
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- New bioluminescent coelenterazine derivatives with various C-6 substitutions
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A series of new coelenterazine analogs with varying substituents at the C-6 position of the imidazopyrazinone core have been designed and synthesized for the extension of bioluminescence substrates. Some of them display excellent bioluminescence properties compared to DeepBlueC or native coelenterazine with both in vitro and in vivo biological evaluations, thus placing these derivatives among the most ideal substrates for Renilla bioluminescence applications.
- Jiang, Tianyu,Yang, Xingye,Zhou, Yubin,Yampolsky, Ilia,Du, Lupei,Li, Minyong
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p. 7008 - 7018
(2017/09/01)
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- Luminescence of coelenterazine derivatives with C-8 extended electronic conjugation
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Replacement of the methylene group at the C-8 position with an extended electronic conjugation is a new promising method to develop red-shifted coelenterazine derivatives. In this paper, we have described an oxygen-containing coelenterazine derivative with a significant red-shifted (63 nm) bioluminescence signal maximum relative to coelenterazine 400a (DeepBlueC, 1). In cell imaging, the sulfur-containing coelenterazine derivative displayed a significantly (1.77 ± 0.09; P ≤ 0.01) higher luminescence signal compared to coelenterazine 400a and the oxygen-containing coelenterazine derivative exhibited a slightly (0.74 ± 0.08; P ≤ 0.05) lower luminescence signal. It is beneficial to understand further the underlying mechanisms of bioluminescence.
- Yuan, Ming-Liang,Jiang, Tian-Yu,Du, Lu-Pei,Li, Min-Yong
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supporting information
p. 550 - 554
(2016/04/26)
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- Novel bioluminescent coelenterazine derivatives with imidazopyrazinone C-6 extended substitution for: Renilla luciferase
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Two series of novel coelenterazine analogues (alkynes and triazoles) with imidazopyrazinone C-6 extended substitution have been designed and synthesized successfully for the extension of bioluminescent substrates. After extensive evaluation, some compounds display excellent bioluminescence properties compared with DeepBlueC in cellulo, thus becoming potential molecules for bioluminescence techniques.
- Jiang, Tianyu,Yang, Xiaofeng,Yang, Xingye,Yuan, Mingliang,Zhang, Tianchao,Zhang, Huateng,Li, Minyong
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p. 5272 - 5281
(2016/07/06)
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- Coelenterazine analog and preparing method and application thereof
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The invention discloses a coelenterazine analog and a preparing method and application thereof. The coelenterazine analog has the general structure formula (I) shown in the description, wherein R1, R2 and R3 in the formula are different substituents. According to application of the compound as a bioluminescence substrate, the existence and quantity (including the enzyme level, the cell level and the animal level) of coelenterazine luciferase can be detected with bioluminescence, and the in vitro, cell and in vivo distribution imaging of luciferase can be detected; the compound can serve as a report signal to detect the pharmacologic action and the toxic effect of medicine on the enzyme level, the cell level and the animal level under the existence of luciferase.
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Paragraph 0144-0146; 0151; 0152
(2018/02/04)
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- IMIDAZO[1,2-α]PYRAZIN-3(7H)-ONE DERIVATIVES BEARING A NEW ELECTRON-RICH STRUCTURE
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The present invention relates to compound of formula I : and their use as chemiluminescent and/or bioluminescent reagents.
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Page/Page column 38
(2011/02/24)
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- Bisdeoxycoelenterazine derivatives, methods of use, and BRET2 systems
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Embodiments of the present disclosure provide for: compositions, BRET systems, kits, and the like.
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- Reactions of cyclopropanone acetals with alkyl azides: Carbonyl addition versus ring-opening pathways
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(Chemical Equation Presented) The Lewis acid-mediated reactions of substituted cyclopropanone acetals with alkyl azides were found to strongly depend on the structure of the ketone component. When cyclopropanone acetal was treated with alkyl azides, N-substituted 2-azetidinones and ethyl carbamate products were obtained, arising from azide addition to the carbonyl, followed by ring expansion or rearrangement, respectively. When 2,2-dimethylcyclopropanone acetals were reacted with azides in the presence of BF3· OEt2, the products obtained were α-amino-α′- diazomethyl ketones, which arose from C2-C3 bond cleavage of the corresponding cyclopropanone, giving oxyallyl cations that were captured by azides. Aryl-substituted cyclopropanone acetals, when subjected to these conditions, afforded [1,2,3]oxaborazoles exclusively, which were also the result of C2-C3 bond rupture, azide capture, and then loss of nitrogen. In the reactions of n-hexyl-substituted cyclopropanone acetals with alkyl azides, a mixture of 2-azetidinones and regioisomeric [1,2,3]-oxaborazoles was obtained. The reasons for the different behavior of the various systems are discussed.
- Grecian, Scott,Desai, Pankaj,Mossman, Craig,Poutsma, Jennifer L.,Aube, Jeffrey
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p. 9439 - 9447
(2008/03/14)
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