172900-73-1Relevant articles and documents
DIHYDROQUINOLIZINONES AS ANTIVIRALS
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, (2018/09/19)
Compounds, specifically hepatitis B virus and/or hepatitis D virus inhibitors, more specifically compounds that inhibit HBe antigen and HBs antigen in a subject, for the treatment of viral infections, and methods of preparing and using such compounds. Formula (I):
Formal total synthesis of aliskiren
Peters, Byron K.,Liu, Jianguo,Margarita, Cristiana,Andersson, Pher G.
, p. 7292 - 7296 (2015/05/05)
The efficient and selective formal total synthesis of aliskiren is described. Aliskiren, a renin inhibitor drug, has received considerable attention, primarily because it is the first of the renin inhibitor drugs to be approved by the FDA. Herein, the formal synthesis of aliskiren by iridium-catalyzed asymmetric hydrogenation of two allylic alcohol fragments is reported. Screening a number of N,P-ligated iridium catalysts yielded two catalysts that gave the highest enantioselectivity in the hydrogenation, which gave the saturated alcohols in 97 and 93 % ee. In only four steps after hydrogenation, the fragments were combined by using the Julia-Kocienski reaction to produce late-stage intermediate in an overall yield of 18 %.
A PROCESS FOR THE PREPARATION OF INTERMEDIATES USEFUL IN THE PRODUCTION OF ALISKIREN
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, (2012/06/30)
A process for preparing 4-[(2R)-2-X-methyl)-3-methylbutyl]-1 -methoxy-2-3(3- methoxypropoxy)-benzene wherein X is a leaving group and use of this compound in the synthesis of aliskiren.
