- Cannabidiol derivative as well as preparation method and medical application thereof
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The invention relates to a cannabidiol derivative and application thereof in medicine, in particular to a pyrimidine derivative as shown in a general formula (I), or a stereoisomer, a solvate, a metabolite, a prodrug, a pharmaceutically acceptable salt or a co-crystal thereof, and definition of each substituent in the general formula (I) is the same as that in the specification.
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Paragraph 0073; 0075; 0125; 0128-0134
(2021/07/10)
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- CONJUGATED CHEMICAL INDUCERS OF DEGRADATION AND METHODS OF USE
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The subject matter described herein is directed to antibody-CIDE conjugates (Ab-CIDEs), to pharmaceutical compositions containing them, and to their use in treating diseases and conditions where targeted protein degradation is beneficial.
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- Synthesis of Unprotected 2-Arylglycines by Transamination of Arylglyoxylic Acids with 2-(2-Chlorophenyl)glycine
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The transamination of α-keto acids with 2-phenylglycine is an effective methodology for directly synthesizing unprotected α-amino acids. However, the synthesis of 2-arylglycines by transamination is problematic because the corresponding products, 2-arylglycines, transaminate the starting arylglyoxylic acids. Herein, we demonstrate the use of commercially available l-2-(2-chlorophenyl)glycine as the nitrogen source in the transamination of arylglyoxylic acids, producing the corresponding 2-arylglycines without interference from the undesired self-transamination process.
- Inada, Haruki,Shibuya, Masatoshi,Yamamoto, Yoshihiko
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p. 11047 - 11059
(2020/10/12)
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- Total synthesis of the antiviral peptide antibiotic feglymycin
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An adaptable approach: The first highly convergent stereoselective synthesis of feglymycin (see structure) and its enantiomer is based on the coupling of repeating peptide fragments. The use of weakly basic conditions throughout the synthesis suppressed t
- Dettner, Frank,Haenchen, Anne,Schols, Dominique,Toti, Luigi,Nusser, Antje,Suessmuth, Roderick D.
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supporting information; experimental part
p. 1856 - 1861
(2009/09/06)
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- Total synthesis of (S)-(-)-curvularin: A ring-closing-metathesis-based construction of the macrocyclic framework
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A convergent, flexible, and efficient approach to the synthesis of curvularin is described. Key step is the high-yielding macrocyclic ring formation by ring-closing metathesis (RCM) using the Grubbs second-generation catalyst. Georg Thieme Verlag Stuttgar
- Mohapatra, Debendra K.,Rahaman, Hasibur,Pal, Rita,Gurjar, Mukund K.
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scheme or table
p. 1801 - 1804
(2009/04/08)
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- Radical-mediated cyclisation of ω-aryl-β-dicarbonyl compounds to tetrahydrobenzocyclohepten-6-ones, hexahydrobenzocycloocten-6-ones and naphthalen-2(1H)-ones
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Manganese(III) acetate in acetic acid promotes efficient radical-mediated oxidative cyclisation of ε-aryl-β-dicarbonyl and Z-γ,δ-unsaturated δ-aryl-β-dicarbonyl compounds carrying electron-releasing groups in the aromatic ring, forming 6,7,8,9-tetrahydro-5H-benzocyclohepten-6-ones and naphthalen-2(1H)-ones, respectively. The process is accompanied by secondary acetoxylation at the activated benzylic position of the initial cyclisation products, and is exemplified by the conversions of the ε- and δ-aryl-β-dicarbonyl compounds 6 and 11 into the benzocycloheptenone 18 and the naphthalenone 21, respectively. Application of the oxidation to the formation of 8-membered hexahydro- and tetrahydro-benzocycloocten-6-ones 19 and 22 from ζ-aryl-β-dicarbonyl and Z-γ,δ-unsaturated ζ-aryl-β-dicarbonyl compounds is limited by low reactivity, and in the latter case, by radical rearrangement followed by cyclisation to a tetralin.
- Jamie, Joanne F.,Rickards, Rodney W.
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p. 3613 - 3621
(2007/10/03)
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- Induction of liquid crystallinity by host-guest interactions
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A molecular clip is described which binds aromatic guests by an induced fit mechanism. It contains twelve long aliphatic chains and can evoke liquid-crystalline properties in a variety of molecules, including polymers and porphyrins, by a process of molecular recognition.
- Van Nunen, Johanna L. M.,Folmer, Brigitte F. B.,Nolte, Roeland J. M.
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p. 283 - 291
(2007/10/03)
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