ISSN:0365-6233    

DOI:10.1002/ardp.19943270103

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractA number of aminoketones with prospective local anaesthetic activity were prepared. The structure of the synthesized compounds was confirmed by spectroscopic and elemental analyses. The physicochemical parameters (pka and logP) were also investigated. The local anaesthetic activity was determinedin vitroon sciatic frog's nerve by the compound action potential technique: the phthalimide derivatives possess considerable local anaesthetic activity equal to that of lidocaine and higher than that of procaine.

ISSN:0365-6233    

DOI:10.1002/ardp.19943270104

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractFour novel series of 4(3H)‐quinazolinone derivatives have been prepared by cyclization of the key intermediates 3‐aryl‐2‐(3‐aryl‐3‐oxopropenyl)‐4‐(3H)‐quinazolinones with different reagents: 3‐aryl‐1‐iminocarbamoyl‐1H‐pyrazol‐5‐yl)‐4(3H)‐quinazolinones, 3‐aryl‐2‐(3‐aryl‐1‐thiocarbamoyl‐1H‐pyrazol‐5‐yl)‐4(3H)‐quinazolinones, 3‐aryl‐2‐(3‐aryl‐4,5‐dihydro‐1,2‐oxazol‐5‐yl)‐4(3H)‐quinazolinones, and 3‐aryl‐2‐(4‐aryl‐2‐thioxo‐1,2,5,6‐tetrahydro‐1,3‐diazin‐6‐yl)‐4(3H)‐quinazolinones. The an

ISSN:0365-6233    

DOI:10.1002/ardp.19943270105

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractDie racemischen und die enantiomeren Hexahydropyrimidin‐2‐one1a‐1elassen sich mit LiAlH4in hohen Ausbeuten zu den racemischen und den enantiomeren Hexahydropyrimidinen2a‐2ereduzieren. Die2a‐2e‐Enantiomere zeigen den gleichen Drehsinn wie die Ausgangsverbindungen. Die in Ethanol rechtsdrehenden Enantiomere (+)‐2a‐2dbesitzen

ISSN:0365-6233    

DOI:10.1002/ardp.19943270106

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractMono‐, di‐ und trisubstituierte 2‐Aminonicotinonitrile vom Typ8, 13, 14und19lassen sich aus Keton‐Mannich‐Basen Hydrochloriden4·HCl, Enonen12, β‐Aminovinylketonen17, 3‐Aminoacrolein‐Derivaten18sowie Vinamidinium Perchloraten21undin situerzeugtem 3,3‐Diamino‐acrylnitril (3) herstellen.Die Reaktion von4·HClmit3in Gegenwart von Ammoniumacetat führt hingegen in einer 2:1 Kondensation zu Tetrahyd

ISSN:0365-6233    

DOI:10.1002/ardp.19943270107

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractDas aus (S)‐Glutaminsäure zugängliche Hydroxymethyllacton1wird als TBDPS‐Ether2geschützt. Die Alkylierung des Lithiumenolats von2liefert die Lactone3a,bin hohem Diastereomerenüberschuß. Andererseits erhält man durch 1,4‐Addition derGilman‐Cuprate an10und Abspaltung der Schutzgruppe die Alkohole12a,b. Die Umsetzung der Alkohole4,12über die Mesylate5,13und die Azide6,14liefert nach katalytischer Hydrierung in Anwesenheit von Boc2O die Boc‐geschützten Amine7,15. Durch Behandlung mit methanolischer HCl erhält man die kristallinen Hydrochloride8,16, die durch Ringöffnung in die DAVA‐Derivate (δ‐Aminovaleriansäurederiva

ISSN:0365-6233    

DOI:10.1002/ardp.19943270108

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractThe highly estrogen receptor(ER)‐affinic compound 1,1‐bis(4‐hydroxy‐phenyl)‐2‐phenylethene (BHPE) was used as carrier ligand for a new cis‐platin derivative, aqua[1,1‐bis(4‐hydroxyphenyl)‐1,2‐diamino‐2‐phenyl‐ethane]sulfatoplatinum(II) (3‐PtSO4) for the therapy of the ER‐positive (i.e.hormone sensitive) breast cancer. The diamine ligand 1,1‐bis(4‐hydroxyphenyl)‐1,2‐diamino‐2‐phenylethane (3) was synthesized by transformation of theO‐methyl ether derivative of BHPE into the 1,2‐bisazido compound3bwith IN3/NaN3, reduction of both N3residues into NH2groups [3a] and subsequent ether cleavage with BBr3. From the diamine ligand3and K2PtI4a five‐membered chelate3‐PtI2was obtained which was transformed into3‐PtSO4with Ag2SO4. In comparison to BHPE the ER‐affinity of3‐PtSO4is markedly reduced.3‐PtSO4possesses, however, weak cytotoxic activity (P388) and antiestrogenic, but no estrogenic properties.3‐PtSO4is comparable with BHPE in terms of its activity

ISSN:0365-6233    

DOI:10.1002/ardp.19943270109

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractIn the determination of ammonia in sera usingo‐benzenesulfonamido‐p‐benzoquinone proteins cause false positive results. These findings contradict the reaction mechanism postulated in lit., according to which a dimer is formed through an NH‐bridge. As deduced by1H‐NMR‐, IR‐, UV‐, and mass spectroscopic investigations of the reaction product and by semi‐empirical MO‐calculations, charge transfer (CT)‐complexes3aare formed with ammonia as well as with proteins, amino acids, and amines. These CT‐complexes are in a solvent dependent equilibrium with their salts3b. Depending on the electron density of the amine compound, different subsequent

ISSN:0365-6233    

DOI:10.1002/ardp.19943270110

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

ISSN:0365-6233    

DOI:10.1002/ardp.19943270102

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY