- Industrial synthesis of 4-chloro, 11β-arylestradiol: How to circumvent a poor diastereoselectivity
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An industrial synthesis of 11β-arylestrone derivatives is described, based on the conjugate opening of a mixture of allylic 5(10)-α and -β epoxides by an aryl cuprate generated catalytically, followed by hydrolysis and subsequent aromatisation of the isomeric mixture of arylation products. An original method for selective 4-chlorination of estrone derivatives is also described.
- Prat, Denis,Benedetti, Francoise,Girard, Gilles Franc,Bouda, Lahlou Nait,Larkin, John,Wehrey, Christian,Lenay, Jacques
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p. 219 - 228
(2013/09/04)
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- NOVEL ALKYNE COMPOUNDS HAVING AN MCH ANTAGONISTIC EFFECT AND MEDICAMENTS CONTAINING THESE COMPOUNDS
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The invention relates to alkyne compounds of general formula (I), in which groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings as cited in Claim 1. The invention also relates to medicaments containing at least one inventive alkyne. The MCH receptor antagonistic effect renders the inventive medicaments suitable for treating metabolic disorders and/or eating disorders, in particular, obesity, bulimia, anorexia, hyperphagia and diabetes.
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Page/Page column 107
(2008/06/13)
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- Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
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The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
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- Synthesis, characterization, and fluorescence quenching of novel cationic phenyl-substituted poly(p-phenylenevinylene)s
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Three new phenyl-substituted poly(p-phenylenevinylene) (Ph-PPV) derivatives with amino-functionalized groups were synthesized through either Gilch reaction for poly{2,5-bis[4′-2-(N,N-diethylamino)ethoxyphenyl]-1,4-phenylenevinylene (P1) or Wittig reaction for poly{2,5-bis(4′-decyloxyphenyl)-1,4-phenylenevinylene-alt-2,5-bis[4′ -2-(N,N-diethylamino)ethoxyphenyl]-1,4-phenylenevinylene} (P2) and poly(2,5-bis{4′-2-[2-(2-methoxyethoxy)ethoxy]ethoxyphenyl}-1,4-phenylenevi nylene-alt-2,5-bis[4′-2-(N,N-diethylamino)ethoxyphenyl]-1,4- phenylenevinylene) (P3). Green light-emitting cationic polymers, poly{2,5-bis(4′-decyloxyphenyl)-1,4-phenylenevinylene-alt-2,5-bis[4′ -2-(N,N,N-triethylammonium)ethoxyphenyl]-1,4-phenylenevinylene} dibromide (P2′) and poly(2,5-bis{4′-2-[2-(2-methoxyethoxy)ethoxy]ethoxyphenyl}-1,4-phenylenevi nylene-alt-2,5-bis[4′-2-(N,N,N-triethylammonium)ethoxyphenyl]-1, 4-phenylenevinylene) dibromide (P3′), were prepared from the neutral polymers P2 and P3, respectively. Water solubility was achieved on P3′ through increase of the hydrophilicity of the side chains. The acid-assistant reversible solubility of P1 makes it promising in preparing light-emitting multilayer devices. On the basis of FT-IR and 1H NMR spectra, it was found that P1 is primarily of trans-vinyl while P2 and P3 are of 80% and 81% cis-vinyl, respectively, which depends on the polymerization method employed. The bulky phenyl substituents successfully impeded the interchain interaction which led to quantum efficiency as films comparable to that of solutions. Quaternization also resulted in more twisted conformation of the polymer main chain which was supported by both blue-shifted absorption and reduced quantum efficiency of P2′ and P3′ in solutions and as films than that of the neutral polymers. The fluorescence of P3′ was efficiently quenched by an anionic quencher Fe(CN)64-, Ksv of which is 3.3 × 106 M-1. However, a modified Stern-Volmer plot showed that 9% of the fluophores could not be accessible to the quencher, which may result from the twisted conformation or intermolecular aggregation.
- Fan, Qu-Li,Lu, Su,Lai, Yee-Hing,Hou, Xiao-Yuan,Huang, Wei
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p. 6976 - 6984
(2007/10/03)
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- 3-[2-(4-Anisidino)phenyl]-1-phenyl-1-propiophenones and propanols
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The invention relates to novel 1-(4-R1 O-phenyl)-2-(4-R2 -phenyl)-6-R3 -1,2,3,4-tetrahydroquinolines having anti-fertility and hypocholesterolemic activities, to their preparation, and to novel intermediates therefor.
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- Certain 1,2-diphenyl-1,2,3,4-tetrahydroquinoline compounds
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The invention relates to novel 1-(4-R1 O-phenyl)-2-(4-R2 -phenyl)-6-R3 -1,2,3,4-tetrahydroquinolines having antifertility and hypocholesterolemic activities, to their preparation, and to novel intermediates therefor.
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