218430-63-8Relevant articles and documents
Highly enantioselective organocatalytic Biginelli and Biginelli-like condensations: Reversal of the stereochemistry by tuning the 3,3′-disubstituents of phosphoric acids
Li, Nan,Chen, Xiao-Hua,Song, Jin,Luo, Shi-Wei,Fan, Wu,Gong, Liu-Zhu
supporting information; experimental part, p. 15301 - 15310 (2010/01/30)
Organocatalytic enantioselective Biginelli and Biginelli-like reactions by chiral phosphoric acids derived from 3,3′-disubstituted binaphthols have been investigated. The size of 3,3′-substituents of the catalysts is able to control the stereochemistry of
Efficient synthesis of the optically active dihydropyrimidinone of a potent α1A-selective adrenoceptor antagonist
Sidler, Daniel R.,Barta, Nancy,Li, Wenjie,Hu, Essa,Matty, Louis,Ikemoto, Nori,Campbell, Jeffrey S.,Chartrain, Michel,Gbewonyo, Kozo,Boyd, Russell,Corley, Edward G.,Ball, Richard G.,Larsen, Robert D.,Reider, Paul J.
, p. 646 - 652 (2007/10/03)
The convergent synthesis of a potent α1A-selective adrenoceptor antagonist is described. Salient features of the synthesis include the enzymatic resolution of a racemic dihydropyrimidinone and the use of a palladium coupling reaction in the synthesis of 2,4′-dipyridyl.
Alpha 1a adrenergic receptor antagonists
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, (2008/06/13)
This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.