213316-32-6Relevant articles and documents
CALPAIN MODULATORS AND METHODS OF PRODUCTION AND USE THEREOF
-
, (2017/09/27)
The present technology relates to compounds, kits, compositions, and methods useful for the treatment of fibrotic disease. In some aspects, the present technology provides for treatment of various diseases or disorders associated or mediated, at least in part, by calpains, such as CAPN1, CAPN2, and/or CAPN9. The present technology is generally applicable to compounds which inhibit myofibroblast differentiation.
Synthesis method of (1R, 2S)-1-amino-2-vinyl ethyl cyclopropane dicarboxylate
-
Paragraph 0018; 0019; 0020; 0021, (2016/10/09)
The invention belongs to the technical field of preparation of anti hepatitis C virus drug intermediates and particularly relates to a synthesis method of (1R, 2S)-1-amino-2-vinyl ethyl cyclopropane dicarboxylate. The synthesis method comprises the specific steps that step one, benzaldehyde, glycine ethyl ester hydrochloride, toluene and triethylamine are used as raw materials to be synthesized into a compound 4; step two, the compound 4 and trans-1,4-dibromo butene react in the toluene and sodium ethoxide to prepare a compound 3; step three, the compound 3 and (2S)-2-[(3,5-dichlorobenzoyl peroxide) oxy] propionic acid react in the toluene, and then isopropyl alcohol and hexane are added to obtain a compound 2; step four, the compound 2 reacts with sodium hydroxide in the toluene to obtain a compound (1R, 2S)-1-amino-2-vinyl ethyl cyclopropane dicarboxylate. The synthesis method is simple in operation and suitable for industrialized production, the raw materials are cheap and easy to obtain, and the obtained target product is high in purity and chiral purity.
Macrocyclic compounds for suppressing replication of hepatitis C virus
-
Page/Page column 39; 40, (2016/05/24)
A compound as represented by Formula (I) is provided, wherein groups are defined in the description. The compound is used as HCV protease inhibitor for treating HCV infection.
Synthesis of bis-macrocyclic HCV protease inhibitor mk-6325 via intramolecular sp 2- sp 3 Suzuki-Miyaura coupling and ring closing metathesis
Li, Hongmei,Scott, Jeremy P.,Chen, Cheng-Yi,Journet, Michel,Belyk, Kevin,Balsells, Jaume,Kosjek, Birgit,Baxter, Carl A.,Stewart, Gavin W.,Wise, Christopher,Alam, Mahbub,Song, Zhiguo Jake,Tan, Lushi
supporting information, p. 1533 - 1536 (2015/03/30)
A practical asymmetric synthesis of the complex fused bis-macrocyclic HCV protease inhibitor MK-6325 (1) is described. Through the combination of a high yielding and low catalyst loading ring-closing metathesis (RCM) to forge the 15-membered macrocycle with an intramolecular sp2-sp3 Suzuki-Miyaura cross-coupling to append the 18-membered macrocycle, multikilogram access to the unique and challenging architecture of MK-6325 (1) has been achieved.
Dynamic kinetic resolution of dehydrocoronamic acid
Chaplin, David A.,Fox, Martin E.,Kroll, Sebastian H. B.
supporting information, p. 5858 - 5860 (2014/05/20)
Dehydrocoronamic acid can be racemised by dehydration of an N-acyl derivative to an azlactone, which undergoes facile racemisation. For the N-trifluoroacetyl derivative, the racemisation process was combined with an enzymatic resolution, to achieve a dynamic kinetic resolution process by which the racemate can be converted to either enantiomer. This journal is the Partner Organisations 2014.
METHOD FOR PRODUCING 1-AMINO-1-ALKOXYCARBONYL-2-VINYLCYCLOPROPANE
-
Page/Page column 31, (2013/02/28)
It is an object of the present invention to provide a novel method for producing (1R,2S)/(1S,2R)-1-amino-1-alkoxycarbonyl-2-vinylcyclopropane which is useful as a synthetic intermediate of therapeutic agents for hepatitis C and a synthetic intermediate thereof. According to the present invention, when a trans-2-butene derivative having a leaving group at each of the 1- and 4-positions is reacted with a malonic ester in the presence of a base, a specific amount of an alkali metal alkoxide or an alkali metal hydride is used as the base, and further a specific amount of a malonic ester is used to produce a cyclopropane diester, and further, chiral or achiral 1-amino-1-alkoxy-carbonyl-2-vinylcyclopropane and a salt thereof are synthesized using the cyclopropane diester.
ENZYMES AND METHODS FOR RESOLVING AMINO VINYL CYCLOPROPANE CARBOXYLIC ACID DERIVATIVES
-
Page/Page column 13, (2011/02/24)
Preparation and isolation of amino vinyl cyclopropane carboxylic acid derivatives and salts thereof, methods of resolving enantiomers, and methods of identifying compositions and/or enzymes that are capable of resolving racemic or partially enantiomerically enriched mixtures.
HCV PROTEASE INHIBITORS
-
Page/Page column 36; 44, (2010/04/03)
Novel compounds that are potent inhibitors of hepatitis C virus protease are provided. Pharmaceutical compositions containing one or more of these inhibitors, methods of preparing the inhibitors and methods of using the inhibitors to treat hepatitis C and related disorders also are provided.
Hepatitis C Virus Inhibitors
-
Page/Page column 23, (2009/12/02)
Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
UREA-CONTAINING PEPTIDES AS INHIBITORS OF VIRAL REPLICATION
-
, (2009/04/24)
The invention provides compounds urea-containing peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof. The variables T, R1-R9, J, L, M, Y, Z, m, n, and t are defined herein. Certain compounds of Formula