2- Amino-1-fluor

Am i no-4-(ethoxycarbon yl-mct hy l)-4-meth y 1- 5-oxo-4,5,6,7-tetrahydro- 64 2-Amino-5-fluor- 872 2-Amino-6-hydroxy- 1036 -Hydrochlorid... 

Bis-[trifluormethyl -dimethyl-amino-fluor-methyl-phospho-ran72 100%... 

Alkoxy-[bis-(trimethylsilyl)-amino]-fluor-methyl- XIII/5, 236 Alkoxy-tris-[2-methyi-phenyl]-X1I1/5, 193... 

Fluor-4-amino- 783 2-Fluor-4-nitro- 783 Halogen-2-hydroxy- 599 4-Hydrazino- -methylester 219... 

A direct catalytic conversion of esters, lactones, and carboxylic acids to oxazolines was efficiently achieved by treatment with amino alcohols in the presence of the tetranuclear zinc cluster Zn4(0C0CF3)60 as catalyst, essential for condensation and cyclodehydration reactions. For example, the use of (5)-valinol allowed the easy synthesis of oxazolines 125 and 126 in satisfactory yields <06CC2711>. A one-pot direct preparation of various 2-substituted oxazolines (as well as benzoxazoles and oxadiazoles) was also performed from carboxylic acids and amino alcohols (or aminophenols or benzhydrazide) using Deoxo-Fluor reagent <06TL6497>. 

Non-isotopic assays have been developed using synthetic acetylated forms of fluorescein-labeled substrates. A number of artificial substrates containing acetylated lysines based on some proteins, such as histones, p53 and p300/CBP, are available for HDAC enzyme activities [11-14]. These include the generic peptides (Fluor-de-Lys), Ac-GA-(NH-Ac-K)-amino-4-methylcoumarin (AMC), Boc-K(Ac)-7-AMC, Ac-NH-GGK(Ac)-AMC [12] and Ac-NH-RHK(Ac)K(Ac)-AMC [14]. The generic peptide... 

Various amino acids have been replaced by 4-F-Phe or hexafluorovaline in peptidic hormones oxytocin (4-F-Phe —> lyr), bradykinin (4-F-Phe —> Phe), and angiotensin II. The consequences are diverse, but the stability toward hydrolytic enzymes is generally enhanced. Thus, incorporation of Fs-valine in an octapeptide antagonist of angiotensin II (Sar-AII) notably enhances its in vivo antagonist activity. Analogues of TRH (thyrotropin-releasing hormone), in which histidine is replaced by a fluor-ohistidine (4-F-His and 2-F-His —> His), have better in vivo activities, while the affinities are lower. 

Aus 2,4(5)-Difluor-5(4)-ethoxycarbonyl-imidazol erhalt man durch selektive Substitution des Fluor-Atoms in 2-StelIung mit Ammoniak in Methanol 2-Amino-5(4)-ethoxycarbonyl-4(5)-fluor-imidazol in 65% Ausbeute928. 

Der Austausch von Amino-Gruppen am Imidazol-Ring fiihrt praktisch immer liber das Di-azonium-Salz. In den meisten Fallen werden die Diazonium-Salze aber nicht isoliert, sondern in situ weiter umgesetzt. Am haufigsten wird die Amino-Gruppe durch die Nitro-Gruppe oder ein Fluor-Atom ausgetauscht. 

Dagegen erhalt man aus 4,4 -Diamino-3,3 -bi-furazanyl mit 2-Fluor-l,3,5-trinitro-benzol je nach Reaktionsbedingungen 4 -Amino-4-(2,4,6-trinitro-anilino)-3,3 -bi-(furazanylj (56% Schmp. 222-2231 ) bzw. 4,4 -Bis-[2,4,6-trinitro-anilino]-3,3 -bi-(furazanyl) [83% Schmp. 315° (Zers.)]232 ... 

Neben den beschriebenen Halogen-, Alkyl-, Alkoxy- und Nitro-Gruppen-substituierten Azobenzolen sind durch Kondensation von Fluor- und Cyan-substituierten Anilinen mit Nitroso-benzolen in saurer Losung auch 4-Butyl-4 -cyan-1, 4-Amino-3,5-difluor-2 und 4-Amino-2,3,5,6-tetrafluor-azobenzol3 zuganglich. 

Cllj /rans) CH2 CH(CHj) 1,57 6d erythro-2-Amino-3-fluor-butan-sdure-( 2-methyl-propyl-ester) 95 1... 

Umsetzung von 1-Brom-alkanen mit N-Benzyl-hydroxylamin in Phosphorsaure-tris-[di-methylamid] (HMPT), Dehydratisierung des so gebildeten N-Alkyl-N-benzyl-hydroxyl-amins mit 2-Fluor-l-methyl-pyridinium-(4-methyl-benzolsulfonat) und saure Hydrolyse des entstandenen N-Benzyliden-amins ergibt 1-Amino-alkane in guten Ausbeuten3. 

NHj F 1 h3c-c-ch-oh 1 1 h3c cn F fj CH-OH CN tiberschub an NH3 UberschuB an NH3 Methanol 30 rain NH3 einlci — ten bei —7SQ, dann 5 Woche 20-30 dann Solvetis ent-fernen und Hydrolyse mit 48% HBrin H20 2-Amino-3 fluor-3-methyl- propansdure Amino-( 1-fluor-cyclohexyl)-essigsaure 63 57 i... 

Die Reaktion von 1,2-Diamino-benzol mit Bis-[2,2,2-trifluor-l-trifluormethyl-ethoxy]-tri-phenyl-phosphoran fuhrt zur N-Monosubstitution unter Bildung von 2-Amino-l-(2,2,2-tr fluor-l-trifluormethyl-ethylamino)-benzol (62%)3 ... 

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