1210430-94-6Relevant articles and documents
NOVEL PROCESS FOR THE SYNTHESIS OF ENANTIOMERICALLY PURE 2-METHOXY-5-[(2R)-2-(4-ALKYLPIPERAZIN-L-YL)PROPYL]-BENZENESULFONAMIDE
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Page/Page column 7, (2012/08/08)
Where R is C1-C3 alkyl, alkenyl A novel process for synthesis of compound of Formula 1 comprising steroselective catalytic reduction of compound of Formula IV under hydrogen gas pressure to obtain an intermediate compound of Formula II, which on coupling in presence of coupling agent and base in presence of organic solvent to obtain compound of Formula X, Formula X on reacting with deprotecting agent in presence of organic solvent results in formation of compound of Formula XI, condensation of Formula XI with alkyl halide results in formation of compound of Formula I.
Synthesis and α1-adrenoceptor antagonist activity of tamsulosin analogues
Sagratini, Gianni,Angeli, Piero,Buccioni, Michela,Gulini, Ugo,Marucci, Gabriella,Melchiorre, Carlo,Poggesi, Elena,Giardin, Dario
experimental part, p. 5800 - 5807 (2011/02/26)
Tamsulosin (-)-1 is the most utilized α1-adrenoceptor antagonist in the benign prostatic hyperplasia therapy owing to its uroselective antagonism and capability in relieving both obstructive and irritative lower urinary tract symptoms. Here we report the synthesis and pharmacological study of the homochiral (-)-1 analogues (-)-2-(-)-5, bearing definite modifications in the 2-substituted phenoxyethylamino group in order to evaluate their influence on the affinity profile for α1-adrenoceptor subtypes. The benzyl analogue (-)-3, displaying a preferential antagonist profile for α1A-than α1D-and α1B- adrenoceptors, and a 12-fold higher potency at α1A- adrenoceptors with respect to the α1B subtype, may have improved uroselectivity compared to (-)-1.