Genotoxicity of Newly Synthesised Imidazole-2(2-2 benzylidene hydrazinyl)-5,5 diphenyl-1,5dihydro -4-imidazol-4one(4-chloro derivative)

2012 ◽  
Vol 5 (2) ◽  
pp. 251-255
Author(s):  
G.E. SUHASINI ◽  
M. NIRMALA ◽  
RASHMI SHIVA KUMAR ◽  
ARCHANA GIRI
Keyword(s):  
Chloro Derivative

Fluorinated analogues of tricyclic neuroleptics: 6,9-difluoro derivative of 10-(4-methylpiperazino)-10,11-dihydrodibenzo[b,f]thiepin

1980 ◽  
Vol 45 (10) ◽  
pp. 2688-2694 ◽  
Author(s):  
Irena Červená ◽  
Marta Hrubantová ◽  
Emil Svátek ◽  
Jiří Holubek ◽  
Miroslav Ryska ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Title Compound ◽  
Substitution Reaction ◽  
Polyphosphoric Acid ◽  
Satisfactory Yield ◽  
Chloro Derivative ◽  
Cns Activity

The acid VI, obtained from 2,5-difluorothiophenol (IV) and (2-iodophenyl)acetic acid, afforded by cyclization with polyphosphoric acid 6,9-difluorodibenzo[b,f]thiepin-10(11H)-one (VII) in a satisfactory yield. Two further steps led to the chloro derivative X giving by a substitution reaction with 1-methylpiperazine the title compound III. This substance exhibits some 10% incoordinating activity of the unsubstituted compound I and an indication of cataleptic activity, in contrast to the inactive analogous dichloro compound II. The bulky atom of chlorine in the vicinity of the methylpiperazine residue interferes evidently with the CNS activity; the influence of the atom of fluorine is much less pronounced in this line.

Electrophilic Addition and Substitution Reactions of Bis((trifluoromethyl)sulfonyl)amide and Its N-Chloro Derivative

1994 ◽  
Vol 33 (15) ◽  
pp. 3281-3288 ◽  
Author(s):  
Ashwani Vij ◽  
Yuan Y. Zheng ◽  
Robert L. Kirchmeier ◽  
Jean'ne M. Shreeve
Keyword(s):  
Electrophilic Addition ◽  
Substitution Reactions ◽  
Chloro Derivative

Neuartige Allylboran- und Allyldiboran(4)-Derivate / Novel Allylboran- and Allyldiboran(4) Derivatives

1990 ◽  
Vol 45 (7) ◽  
pp. 985-988 ◽  
Author(s):  
Gabriele Knörzer ◽  
Hermann Seyffer ◽  
Hans Pritzkow ◽  
Walter Siebert
Keyword(s):  
Structure Analysis ◽  
X Ray ◽  
Chloro Derivative ◽  
Chloro Derivatives ◽  
Derivatives Of

Allyldiboran(4) derivatives la—c are obtained from allylmagnesium chloride and chloro derivatives of diboran(4). la—c are air-sensitive liquids; heating of le did not yield a 2,3-dihydro-l,2-diborole derivative (B). Reaction between 1,1-bis(dichloroboryl)-3,3-dimethyl-butane (5) and H2C=C(CH2SnMe3)2 (4) leads to the heat-sensitive chloro derivative 2a, in which the chlorine is substituted by Me3SiNMe2 to give stable 1,3-bis-dimethylamino-5-methylene-2-neopentyl- 1,3-diborinane (2 b). 1,2-Bis(dichloroboryl)benzene and 4 yield the chloro derivative 3a, and its substitution with HN(i-Pr)2 leads to 1,4-bis(diisopropylamino)-2,3-benzo-6-methylene-1,4,5,7-tetrahydro-1,4-diborepine (3 b). The X-ray structure analysis reveals a folded tetrahydro-1,4-diborepine ring.

2',3'-O-Carbonyl derivatives of 6-azauridine in the synthesis of its 5-substituted and 5'-deoxy derivatives

1987 ◽  
Vol 52 (8) ◽  
pp. 2070-2082
Author(s):  
Pavel Drašar ◽  
Jiří Beránek
Keyword(s):  
Thionyl Chloride ◽  
Alkaline Hydrolysis ◽  
Triphenyl Phosphine ◽  
Carbonyl Derivatives ◽  
Tributyltin Hydride ◽  
Chloro Derivative ◽  
Ammonium Halides ◽  
Chloro Derivatives ◽  
Derivatives Of ◽  
Dichloro Derivative

Preparation of 2',3'-O-carbonyl derivatives of 5'-deoxy-6-azauridine and 6-azauridine using 1,1'-carbonyldiimidazole has been elaborated. 5'-Chloro and 5'-bromo derivatives were prepared by treatment of the 5'-O-mesyl derivative with quaternary ammonium halides, 5'-chloro derivatives also by direct halogenation with thionyl chloride in hexamethylphosphortriamide or with tetrachloromethane, triphenyl phosphine, and dimethylformamide. Derivatives of 5'-bromo-6-azauridine were reduced with tributyltin hydride to 5'-deoxy-6-azauridine compounds. 6-Azauridine 2',3'-carbonate (IVa) and its 5'-derivatives IVc and IVe on treatment with imidazole in dimethylformamide afforded 2,2'-anhydronucleosides IIIa-IIIc. The 2,2'-anhydro-5'-deoxy compound IIIc underwent alkaline hydrolysis to 5'-deoxy-1-β-D-arabino-pentofuranosyl-6-azauracil (VIa). Treatment of 2,2'-anhydro-5'-deoxy-5'-chloro derivative IIIb with hydrogen chloride led to 2',5'-dichloro derivative If.

A Facile Synthesis of 9-Deaza Analogue of Olomoucine

2003 ◽  
Vol 68 (4) ◽  
pp. 779-791 ◽  
Author(s):  
Petr Čapek ◽  
Miroslav Otmar ◽  
Milena Masojídková ◽  
Ivan Votruba ◽  
Antonín Holý
Keyword(s):  
Cell Growth ◽  
Growth Inhibition ◽  
Cell Lines ◽  
Alkaline Solution ◽  
Catalytic Hydrogenation ◽  
Cell Growth Inhibition ◽  
Facile Synthesis ◽  
Hydroxymethyl Group ◽  
Chloro Derivative

Heating of 6-(benzylamino)-2-chloro-9-deazapurine (3) with ethanolamine afforded 6-(benzylamino)-2-[(2-hydroxyethyl)amino]-9-deazapurine (8). Its treatment with formaldehyde in alkaline solution, after protection of the OH group with DMTr, led to hydroxymethylation at position 9. Conversion of the hydroxymethyl group to methyl was performed by catalytic hydrogenation under simultaneous deprotection, which resulted in the formation of the 9-deaza analogue 1 of olomoucine. Compound 1 does not exhibit any significant in vitro cell growth inhibition of CCRF-CEM, HeLa and L-1210 cell lines. Cytostatic activity was found in 6-(benzylamino)-9-deazapurine (2) and its 2-chloro derivative 3 in CCRF-CEM cells with IC50 13.3 and 15.8 μM, respectively.

scholarly journals Antioxidant Activity of Carvone and Derivatives against Superoxide Ion

2017 ◽  
Vol 12 (5) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Sofia Pombal ◽  
Yaiza Hernández ◽  
David Diez ◽  
Eily Mondolis ◽  
Aldahir Mero ◽  
...  
Keyword(s):  
Organic Chemistry ◽  
Antioxidant Activity ◽  
Natural Product ◽  
Building Blocks ◽  
Starting Material ◽  
Superoxide Ion ◽  
Chloro Derivative

Carvone has corroborated its versatility as starting material for building blocks synthesis in organic chemistry, being achieved a new chiral lactone. It has been done a study on the antioxidant activity against superoxide of carvone and a chloro derivative that show the potent activity of the natural product ( R)-carvone, 1.

Potential noncataleptic neuroleptic agents: 2,3-Dichloro-10-[4-(2-hydroxyethyl)piperazino]-10,11-dihydrobenzo[b,f]thiepin

1984 ◽  
Vol 49 (4) ◽  
pp. 992-1001 ◽  
Author(s):  
Jiří Urban ◽  
Antonín Dlabač ◽  
Martin Valchář ◽  
Miroslav Protiva
Keyword(s):  
Benzoic Acid ◽  
Potassium Carbonate ◽  
Title Compound ◽  
Substitution Reaction ◽  
Polyphosphoric Acid ◽  
Dopamine Metabolism ◽  
Nitro Derivative ◽  
High Dose ◽  
Chloro Derivative ◽  
Hydroxyethyl Piperazine

The 6-nitro derivative V, obtained by nitration of 3,4-dichlorobrombenzene, was transformed via the amine VI and nitrileVII to 2-bromo-4,5-dichlorobenzoic acid (IX). Its reaction with thiophenol in 3-methyl-1-butanol in the presence of potassium carbonate and catalytic amounts of copper and cuprous iodide afforded 4,5-dichloro-2-(phenylthio)benzoic acid (Xa) which was reduced to the alcohol XIa. The transformation to the homologous acid XIVa proceeded via noncharacterized intermediates XIIa and XIIIa. The cyclization with polyphosphoric acid at 150 °C resulted in 2,3-dichlorodibenzo[b,f]thiepin-10(11H)-one (XV) which was reduced to the alcohol XVI. Treatment with hydrogen chloride gave the unstable chloro derivative XVII whose substitution reaction with 1-(2-hydroxyethyl)piperazine led to the title compound II. Its dimethanesulfonate showed properties of a little toxic and noncataleptic tranquillizer. Because it does not influence the dopamine metabolism in rat brain in a rather high dose, it cannot be considered a neuroleptic.

Synthesis of a Chloro Derivative of DL-Vasicine1

1959 ◽  
Vol 24 (6) ◽  
pp. 753-755 ◽  
Author(s):  
PHILIP L. SOUTHWICK ◽  
SHELDON E. CREMER
Keyword(s):  
Chloro Derivative

The synthesis of some novel N-chloro-Δ1-4-azasteroids by efficient N-chlorination of azasteroid lactams with trichloroisocyanuric acid

1991 ◽  
Vol 69 (9) ◽  
pp. 1482-1486 ◽  
Author(s):  
Thomas G. Back ◽  
Joseph H.-L. Chau ◽  
Brian P. Dyck ◽  
Patricia L. Gladstone
Keyword(s):  
Key Words ◽  
High Yield ◽  
Principal Product ◽  
Chloro Derivative ◽  
Trichloroisocyanuric Acid

The preparation of N-chloro-Δ1-4-azasteroids 2a–2c from lactams 1a–1c was achieved conveniently and in high yield with trichloroisocyanuric acid. The treatment of 20β-hydroxy-4-aza-5α-pregn-1-en-3-one (1d) with this reagent produced the less stable N-chloro compound 2d, which reacted further to afford 4-aza-5α-pregn-1-en-3,20-dione (4) as the principal product. The similar chlorination of 4-azacholest-5-en-3-one (5) occurred at C-6, giving 6-chloro-4-azacholest-5-en-3-one (6). Photolysis of N-chloro-4-aza-5α-cholest-1-en-3-one (2a) in methanol produced the transient N-acyl imine 7, which was trapped by the solvent to afford 5-methoxy-4-azacholest-1-en-3-one (8), along with 4-azacholesta-1,5-dien-3-one (9) and its 6-chloro derivative 10. Key words: N-chloroazasteroid, Δ1-4-azasteroid, N-chloro-Δ1-4-azasteroid, trichloroisocyanuric acid, N-chlorination.

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