172900-75-3Relevant academic research and scientific papers
HEPATITIS B VIRUS SURFACE ANTIGEN INHIBITOR
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Paragraph 0151; 0158; 0159, (2020/04/21)
Disclosed in the present invention is a new 11-oxo-7,11-dihydro-6h-benzo-[f]pyrido[1,2-d][1,4]azepine oxepin-10-carboxylic acid derivative serving as a hepatitis B virus surface antigen inhibitor. Specifically disclosed are a compound represented by formula (V) or a pharmaceutically acceptable salt thereof, and applications of the compound represented by formula (V) or the pharmaceutically acceptable salt thereof and a pharmaceutical composition thereof in the treatment of viral hepatitis B.
Aliskiren intermediate preparation method
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Paragraph 0091; 0093; 0094, (2019/03/25)
The present invention relates to the technical field of pharmaceutical preparation method, the preparation method of the existing long reaction time, the problem of low yield, provides a aliskiren preparation method, comprises the following steps: S1, 1st intermediate preparation: the raw material is dissolved in a solvent, adding sodium hypochlorite and sodium bisulfite reaction, shall be 1st intermediate; S2, intermediate in the preparation of 2nd: to the 1st intermediate dropping 4 - bromo - 1 - methoxy - 2 - (3 - methoxy third oxygen radical) benzene, tetrahydrofuran solution, adding low [...] catalyst, to obtain the 2nd intermediate; S3, aliskiren intermediate preparation: will be soluble in ethyl acetate in the 2nd intermediate, then adding water, nitrogen replacement 3 times, the hydrogen replaced 3 times after adding the hydrogen hydrogenation reaction, to obtain the product. By adding low deuterium water as a catalyst, help to accelerate the step S2 of the reaction rate, the reaction time is shortened, while at the same time help to improve the step S2 in the reaction yield, and then make the total reaction yield can be improved.
DIHYDROQUINOLIZINONES AS ANTIVIRALS
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Paragraph 00483; 00485; 00486; 00659; 00661; 00662; 001602, (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 %.
An improved and economical process for the manufacture of the key intermediate of aliskiren, a new potent renin inhibitor
Wang, Fan,Xu, Xiao-Ying,Wang, Fei-Ying,Peng, Lin,Zhang, Yong,Tian, Fang,Wang, Li-Xin
, p. 1458 - 1462 (2013/12/04)
An improved, practical, economical and efficient process for the production of (2S,4S)-2-amino-4-(4-methoxy-3-(3-methoxypropoxy)benzyl)-5-methylhexanoic acid, a key intermediate of the new potent renin inhibitor of aliskiren, in a total yield over 30% is described. This process avoids expensive reagents and chromatographic purifications, and is easily scaled up in industry.
AN IMPROVED PROCESS FOR THE PREPARATION OF ALISKIREN
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Page/Page column 3; 4; 5; 9; 13, (2013/12/03)
The present invention relates to an improved process for the preparation of renin inhibitor Aliskiren intermediates of Formula-II and further conversion into Aliskiren and its pharmaceutically acceptable salts.
PROCESS FOR THE PREPARATION OF (2S,4S,5S,7S)-N-(2-CARBAMYL-2- METHYLPROPYL)-5-AMINO-4-HYDROXY-2,7-DIISOPROPYL-8-[4-METHOXY-3-(3- METHOXYPROPOXY)PHENYL]-OCTANAMIDE HEMIFUMARATE AND ITS INTERMEDIATES THEREOF
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Page/Page column 58, (2011/12/14)
The present invention relates to a process for the preparation of (2S,4S,5S,7S)-N-(2- Carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxy propoxy )phenyl]-octanamide compound of formula- 1 and its pharmaceutically acceptable salts thereof. Further, relates to the processes for the preparation of (R)-4-(2-(halomethyl)-3- methylbutyl)-l-methoxy-2-(3-methoxypropoxy) benzene and (R)-2-(4-methoxy-3-(3-methoxy propoxy) benzyl)-3-methyIbutan-l-ol useful intermediates in the synthesis of compound of formula- 1.
AMIDE INHIBITORS OF RENIN
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, (2010/06/13)
The present invention relates to new amide inhibitors of renin, pharmaceutical compositions thereof, and methods of use thereof
Aryl- and Heteroaryl-Ethyl-Acylguanidine Derivatives, Their Preparation and Their Application in Therapeutics
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Page/Page column 20, (2009/08/18)
Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).
1-HETEROCYCLYLAMINO-2-HYDROXY-3-AMINO-ω-ARYLALKANES
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Example 1, (2010/11/28)
1-Heterocyclylamino-2-hydroxy-3-amino-?-arylalkanes of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, medicinally active ingredients.
