- Non-natural amino acid and application thereof Recombinant protein and recombinant protein conjugate comprising same
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The invention provides a non-natural amino acid. A compound represented by formula (I) or an enantiomer thereof. The invention also provides application of the non-natural amino acid. Further, the present invention also provides a protein conjugate comprising the recombinant protein and of the non-natural amino acid prepared from the recombinant protein. The non-natural amino acid provided by the invention is simple and convenient to prepare, good in safety, not prone to inactivation during protein insertion, high in conjugate rate with a coupling part, and higher in stability of the obtained conjugate.
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Paragraph 0088; 0092; 0095
(2021/11/03)
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- PERIODONTAL DISEASE THERAPY
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Disclosed are formulations for oral films and other compositions containing therapeutic agents. The therapeutic agents interfere with succinate/succinate receptor signaling. The films and compositions of the present disclosure can be used to treat periodontal disease.
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Paragraph 0074; 0081; 0082
(2019/07/20)
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- Palladium-Catalyzed Carboxylation of Benzyl Chlorides with Atmospheric Carbon Dioxide in Combination with Manganese/Magnesium Chloride
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An efficient direct carboxylation of a series of benzyl chlorides with CO2 catalyzed by Pd(OAc)2/dicyclohexyl (2′,6′-dimethoxy-[1,1′-biphenyl]-2-yl)phosphine (SPhos) was developed to afford the corresponding phenylacetic acids in combination with Mn powder as a reducing reagent and MgCl2 as an indispensable additive. The reaction proceeded smoothly under 1 atm CO2. The application of Mn powder instead of a sensitive reducing reagent represents an operationally simple access to phenylacetic acids. Notably, MgCl2 is able to stabilize the (SPhos)2PdII(Bn)(Cl)(η1-CO2)(MgCl2) adduct and thus facilitates CO2 insertion into the PdII-C bond, which is supported by a DFT study. Specific effect: MgCl2 facilitates the direct insertion of CO2 into the PdII-C bond by stabilizing the PdII-CO2 adduct. With MgCl2 as an indispensable additive, the Pd-catalyzed carboxylation of various benzyl chlorides proceeded smoothly under 1 atm CO2, and the application of Mn powder instead of a sensitive reducing reagent makes this protocol an operationally simple access to phenylacetic acids.
- Zhang, Shuai,Chen, Wei-Qiang,Yu, Ao,He, Liang-Nian
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p. 3972 - 3977
(2016/01/26)
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- Palladium-catalyzed silver-mediated α-arylation of acetic acid: A new approach for the α-arylation of carbonyl compounds
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A new approach for the α-arylation of acetic acid through Pd-catalyzed silver-mediated direct C-H arylation of acetic acid with aryl iodides was developed. This protocol provided a straightforward method for the synthesis of a diverse set of α-phenylacetic acids. Palladium served on a silver platter: A new approach for the α-arylation of acetic acid through Pd-catalyzed silver-mediated direct C-H arylation of acetic acid with aryl iodides is presented. This protocol provides a straightforward method for the synthesis of a diverse set of α-phenylacetic acids. Deuteration experiments are performed to help elucidate the reaction mechanism.
- Wu, Guo-Jie,Guan, Jing,Han, Fu-She,Zhao, Yu-Long
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p. 1589 - 1593
(2014/06/24)
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- Ni-catalyzed direct carboxylation of benzyl halides with CO2
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A novel Ni-catalyzed carboxylation of benzyl halides with CO2 has been developed. The described carboxylation reaction proceeds under mild conditions (atmospheric CO2 pressure) at room temperature. Unlike other routes for similar means, our method does not require well-defined and sensitive organometallic reagents and thus is a user-friendly and operationally simple protocol for assembling phenylacetic acids.
- León, Thierry,Correa, Arkaitz,Martin, Ruben
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supporting information
p. 1221 - 1224
(2013/03/14)
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- PNA-based reagents for the direct and site-specific synthesis of thymine dimer lesions in genomic DNA
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An acetophenone containing PNA-based reagent was designed for the direct and site-specific synthesis of a cis-syn thymidine dimer lesion in genomic DNA. Copyright
- Pieck, J. Carsten,Kuch, David,Grolle, Friederike,Linne, Uwe,Haas, Clemens,Carell, Thomas
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p. 1404 - 1405
(2007/10/03)
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- Efficient photodecarboxylation of 3- and 4-acetylphenylacetic acids in aqueous solution
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The photochemistry of 3- and 4-acetylphenylacetic acids (6 and 7) has been studied in aqueous solution. This work is a continuation of research efforts aimed at understanding the structural effects on the efficacy for benzyl carbanion photogeneration via photodecarboxylation. The nitro group (at the 3- and 4-positions) is known to be an exceptionally good activating group on the benzene ring - because of its enhanced electron-withdrawing effect in the excited triplet state - for photodecarboxylation and the related photo-retro-aldol type process. It is shown in this work that the acetyl group is an equally good activating group for the photodecarboxylation. Thus, the photochemistry of 6 and 7 parallels much of what was observed for the corresponding nitrophenylacetic acids 1 and 2. Both 6 and 7 photodecarboxylate efficiently (Φd = 0.60 and 0.22, respectively, at pH 7) via the carboxylate form, to give observable (by laser flash photolysis) benzyl carbanion or related intermediates. The meta isomer 6 displays an acid-catalyzed pathway for photodecarboxylation at pH 3 and along with its enhanced overall reactivity, is consistent with a meta effect of the acetyl group. Triplet state reactivity is inferred from sensitization and laser flash photolysis experiments. Based on the results of this work, the acetyl group may now be viewed as an "enhanced" electron-withdrawing group (in the excited state) when attached to a benzene ring (i.e., in acetophenone derivatives) that is capable of inducing ionic reactions, which is not the traditional photochemistry that is expected from such compounds.
- Huck, Lawrence A.,Xu, Musheng,Forest, Kaya,Wan, Peter
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p. 1760 - 1768
(2007/10/03)
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- Efficient photodecarboxylation of aroyl-substituted phenylacetic acids in aqueous solution: A general photochemical reaction
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Photolysis (254-350 nm) of a variety of aroyl-substituted phenylacetic acids and p-acetylphenylacetic acid in aqueous solution at pH > pK(a) resulted in efficient photodecarboxylation (Φ = 0.2-0.7), to give in most cases a single product arising via the corresponding arylmethyl carbanion, indicating that photodecarboxylation is an efficient and general reaction for these types of compounds.
- Xu,Wan
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p. 2147 - 2148
(2007/10/03)
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- Enediyne derivatives useful for the synthesis of conjugates of methyltrithio antitumor agents
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This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.
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