A new series of aryl clonazepam derivatives (11-16) have been synthesized by employing Suzuki Cross-coupling reaction, which includes the reaction of clonazepam with suitable derivative boronic acid at the presence of Pd(PPh3)4 as catalyst, and Na2CO3 as a base. The structures of the newly synthesized compounds were assigned by 1 H, 13 C and 2D NMR spectroscopic techniques.
Prepare new derivatives 5-(3-Fluoro-biphenyl-2-yl)-7-nitro-1,3-dihydro-benzo[e] [1,4]diazepin-2-ol (88)and 5-Nitro-2’-(7-nitro-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-5-yl)-biphenyl-3-carboxylic acid (89)compound from clonazepam and identified by spectrum of 13C-NMR and showed spectrum 1H-NMR . Clonazepam has massive adverse effect on prostate,lung,liver,kidney and spleen 3-new derivatives 5-(3-Fluoro-biphenyl-2-yl)-7-nitro-1,3-dihydro-benzo[e] [1,4]diazepin-2-ol (88) has limited effect and there is no clear changes in most organs studies.4-5-Nitro-2’-(7-nitro-2-oxo-2,3-dihydro-1Hbenzo[e][1,4]diazepin-5-yl)-biphenyl-3-carboxylic acid (89)compound has significant adverse effect but still less potent than clonazepam.
OBJECTIVE
To characterization and synthesis of new drugs related to clonazepam as well as to overcome massive adverse effect of clonazepam and increase the potency and half live of drugs.
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