- Comparative study of the Kumada, Negishi, Stille, and Suzuki - Miyaura reactions in the synthesis of the indole alkaloids hippadine and pratosine
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The total synthesis of hippadine by a tandem metalation/cross-coupling/ lactamization strategy was investigated starting from either 7-bromoindole or a 6-halogenated methyl piperonate. The Kumada and Negishi cross-coupling reactions failed to provide any of the desired product. However, the Stille and Suzuki reactions furnished hippadine in low yields starting from the electron-deficient methyl 6-iodo- and 6-bromopiperonate, respectively. Starting from the metalated indole, only the Suzuki reaction occurred, affording hippadine in 67-74% and pratosine in 62% isolated yield.
- Mentzel, Uffe V.,Tanner, David,Tonder, Janne E.
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- Structure Elucidation of the Main Tetrahydroxyxanthones of Hypericum Seeds and Investigations into the Testa Structure
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Seeds from Hypericum species have recently been identified as an interesting source of xanthone derivatives. Extraction of seeds from H. perforatum with MeOH and subsequent concentration via polyamide adsorption yielded a fraction enriched in tetrahydroxy
- Lorenz, Peter,Heller, Annerose,Bunse, Marek,Heinrich, Miriam,Berger, Melanie,Conrad, Jürgen,Stintzing, Florian C.,Kammerer, Dietmar R.
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- SOS1 INHIBITORS
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The present invention relates to compounds that inhibit Son of sevenless homolog 1 (SOS1) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
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Paragraph 0231-0232
(2021/06/26)
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- THIOXANTHONE DERIVATIVES, COMPOSITION COMPRISING THE SAME AND PATTERN FORMING METHOD COMPRISING SAID COMPOSITION
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Latent photoinitiator compounds are described, as well as compositions containing such compounds and their uses in photoinitated methods for producing photoresist structures.
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Paragraph 0155-0158
(2020/02/14)
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- A synthetic camptothecin compound in 5-6 method of and ring structure (by machine translation)
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The present invention discloses a synthetic camptothecin compound in the 5 [...] 6 method of and ring structure, the method is that the conjugated structure of formula II occurs in the solvent alkene alkyne ester series cyclization reaction in the molecule, thus the system results in the type shown in I of the 5 [...] 6 and ring structure, the specific equation is: In the formula: R 1 and R 2 are respectively and independently selected from hydrogen, alkyl, cycloalkyl, aryl or heterocyclic group; or, R 1 and R 2 together form a saturated or unsaturated carbocyclic or heterocyclic; R 3 and R 4 are respectively and independently selected from hydrogen, alkyl, cycloalkyl, aryl or heterocyclic group; or, R 3 and R 4 together form a saturated or unsaturated carbocyclic or heterocyclic rings; selected from R C 1-C 4 alkyl; P is amino protecting group. The stated method of this invention has the advantages of simple operation, safety and environmental protection, low production cost, high yield, is suitable for large-scale production, and the like, to promote such compounds in the medical field with the extensive application of an important value. (by machine translation)
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Paragraph 0070; 0072; 0073
(2016/10/20)
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- COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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Compounds and their pharmaceutically acceptable salts for treatment of synucleinopathies, such as Parkinson's disease and tauopathies.
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Page/Page column 34
(2012/09/21)
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- Compounds for Use in the Detection of Neurodegenerative Diseases
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Provided are the use of the disclosed compounds as imaging agents and methods for in vivo imaging and detection of pathological characteristics unique to synuclein diseases, such as Parkinson's disease.
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- Synthesis of N-substituted benzo[c][1,7]- and benzo[c][1,8] phenanthrolin-(5H)-6-ones through a Pd-mediated Suzuki-Miyaura heteroaryl-aryl coupling reaction
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In the course of the search for non-camptothecin topoisomerase I inhibitors we have undertaken the synthesis of N-substituted benzo[c][1,7]- and benzo[c][1,8]phenanthrolinone derivatives. An intermolecular Suzuki-Miyaura heteroaryl-aryl coupling reaction was planned as the key step. Then a nitro reduction followed by a concomitant lactamization achieved the construction of the tetracycle structures. This methodology permitted a rapid and efficient elaboration of biologically potent compounds.
- Genès, Constance,Michel, Sylvie,Tillequin, Fran?ois,Porée, Fran?ois-Hugues
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experimental part
p. 10009 - 10015
(2010/02/27)
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- Oxygenated phenanthrenes via quinol ketals: Cyclization vs. migration
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2-methoxyphenanthrenes were prepared by reaction of lithiated 2-bromostyrenes with quinone monoketals followed by acid-mediated cyclization of the resulting p-arylquinol ketals. Substitution at the bromostyrene side-chain or the quinone monoketal ring had only a modest effect on yields, but oxygen substitution on the bromostyrene aromatic nucleus resulted in a competing 1,2-aryl migration arising during the quinol ketal cyclization step. The extent of this rearrangement was found to be a function of the Lewis acid/solvent system employed.
- Morrow, Gary W.,Marks, Tina M.,Sear, Debra L.
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p. 10115 - 10124
(2007/10/02)
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