- A refining method of Venacaran hydrochloride
-
The present invention discloses a refining method of Venacaran hydrochloride; said method comprising preparation of Vinacarlan hydrochloride crude product and halogenated hydrocarbon washing, alkalinization, extraction, salting, recrystallization step, by the method of the present application, the peak time of about 32mins of unknown impurities ImpA may be completely removed, to obtain a quality superior to the preparation of the original Manufacturer Cadioomex Pharmaceutical Company of Wienakaran hydrochloride solids. The method is simple to operate, the conditions are mild, the requirements for the equipment are low, and the purity of the obtained Vinacarlan hydrochloride can reach more than 99.9%. At the same time, the method does not use heavy metals, which is conducive to the manufacture of Vi?akalan hydrochloride into injections.
- -
-
Paragraph 0048-0050
(2022/03/02)
-
- Synthesis of nature product kinsenoside analogues with anti-inflammatory activity
-
Kinsenoside is the major bioactive component from herbal medicine with a broad range of pharmacological functions. Goodyeroside A, an epimer of kinsenoside, remains less explored. In this report we chemically synthesized kinsenoside, goodyeroside A and their analogues with glycan variation, chirality inversion at chiral center(s), and bioisosteric replacement of lactone with lactam. Among these compounds, goodyeroside A and its mannosyl counterpart demonstrated superior anti-inflammatory efficacy. Furthermore, goodyeroside A was found to suppresses inflammatory through inhibiting NF-κB signal pathway, effectively. Structure-activity relationship is also explored for further development of more promising kinsenoside analogues as drug candidates.
- Song, Wei,Sun, Yong,Xu, Lintao,Sun, Yajing,Li, Tianlu,Peng, Peng,Lou, Hongxiang
-
supporting information
(2020/12/02)
-
- Asymmetric synthesis of (S)-dihydrokavain from l-malic acid
-
A practical and efficient asymmetric synthesis of (S)-dihydrokavain from known ethyl (S)-2-hydroxy-4-phenylbutanoate which is, in turn, readily available from l-malic acid as a cheap chiral pool material is described using regioselective ring-opening of the 1,2-cyclic sulfate with lithium-3,3,3-triethoxypropiolate and subsequent HgO/H2SO4-mediated lactonization as the key steps. Its opposite enantiomer (R)-dihydrokavain was also synthesized from d-malic acid using the same sequences of reactions for the purpose of optical purity determination.
- Eskici, Mustafa,Karanfil, Abdullah,?zer, M. Sabih,Kabak, Yal??n,Durucasu, ?nci
-
p. 2382 - 2390
(2018/10/20)
-
- Preparation method of chromanone 2-carboxylic acid or chroman 2-carboxylic acid derivatives
-
The present invention relates to a chromanone-2-carboxylic acid derivative and a chroman-2-carboxylic acid derivative which can be used as an intermediate for effective medicinal components currently available in the market, and to preparation methods the
- -
-
Paragraph 0136-0139
(2017/05/16)
-
- A method for preparing weinaweina kalland hydrochloride (by machine translation)
-
The invention discloses a method for preparing weinaweina kalland hydrochloride. The method to selectively amino protection, nucleophilic addition, nucleophilic substitution, deprotected, cyclized, reduction, into a salt by the reaction of the compound Wina carland hydrochloride. And after nuclear magnetic analysis test technology confirm its structure. It adopts the cheap and easily obtained starting materials to prepare, preparation method has advantages of simple operation, mild condition, easy industrialized production and the like, and avoids the use of heavy metal, is beneficial to the development of the oral. (by machine translation)
- -
-
Paragraph 0066-0068
(2017/11/27)
-
- Purification method of vernakalant hydrochloride
-
The invention discloses a purification method of vernakalant hydrochloride. The method comprises the steps of preparation of a vernakalant hydrochloride crude product and purification through the process of alkalinization, nonpolar solvent extraction, acidification and mixed solvent pulping, and thus a qualified product is obtained. The preparation method is simple in operation, mild in condition and easy for industrialized production, and the purity of the product reaches 99.9 percent, and the total impurity and single impurity are both less than 0.1 percent, so that the quality requirements for preparing medicine can be reached, and at the same time, the usage of heavy metal is avoided, and the development of injection forms is facilitated.
- -
-
Paragraph 0063-0065
(2017/01/12)
-
- Divergent Stereocontrolled Synthesis of the Enantiopure Tetracyclic Cores of Asparagamine A and Stemofoline via an Intramolecular 2-Propylidine-1,3-(bis)silane Bicyclization
-
A concise and highly diastereoselective synthesis of the polyfused tetracyclic cores of the Stemona alkaloids asparagamine A and stemofoline that relies on a 2-propylidine-1,3-(bis)silane bicyclization onto a enantiodefined pyrrolidine 2,5-di(cation) equivalent derived from l-malic acid is reported. A crucial feature of this divergent synthetic approach involves the solvolysis of a transient and highly labile tertiary-propargylic hydroxylactam trifluoroacetate in the strongly ionizing medium 5 M LiClO4/Et2O. The acyliminium ion generated in this manner undergoes stereospecific interception by the aforementioned (bis)silane nucleophile.
- Anderson, Bryon K.,Livinghouse, Tom
-
p. 9847 - 9855
(2015/11/03)
-
- COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY
-
Provided are indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which LRRK2 kinase is involved. Also provided are pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK2 kinase is involved.
- -
-
Page/Page column 100
(2014/09/29)
-
- COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY
-
The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
- -
-
Page/Page column 88
(2014/09/29)
-
- COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY
-
Disclosed are indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which LRRK2 kinase is involved. Also disclosed are pharmaceutical compositions in the prevention or treatment of such diseases in which LRRK2 kinase is involved.
- -
-
Page/Page column 87
(2014/09/29)
-
- COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY
-
The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
- -
-
Page/Page column 104
(2014/09/29)
-
- Efficient synthesis of kinsenoside and goodyeroside A by a chemo-enzymatic approach
-
Kinsenoside (1) and goodyeroside A (2), two naturally occurring stereoisomers with diverse biological activities, have been synthesized efficiently by a chemo-enzymatic approach with a total yield of 12.7%. The aglycones, (R)- and (S)-3-hydroxy-γ-butyrolactone, were prepared from D- and L-malic acid by a four-step chemical approach with a yield of 75%, respectively. These butyrolactones were then successfully glycosidated using β-D-glucosidase as a catalyst in a homogeneous organic-water system. Under the optimized enzymatic conditions, the yields of kinsenoside and goodyeroside A in the enzymatic steps both reached 16.8%.
- Zhang, Yang,Xia, Yihong,Lai, Yongji,Tang, Fang,Luo, Zengwei,Xue, Yongbo,Yao, Guangmin,Zhang, Yonghui,Zhang, Jinwen
-
p. 16950 - 16958
(2015/01/08)
-
- PROCESS FOR PREPARING AMINOCYCLOHEXYL ETHER COMPOUNDS
-
The present invention relates to a process for preparing aminocyclohexyl ether compounds of Formula I: or the pharmaceutically acceptable salts and esters thereof. In particular, the instant invention is directed towards a process for preparing (1R,2R)-2-
- -
-
Page/Page column 81-82
(2012/03/11)
-
- A flexible approach to grandisine alkaloids: Total synthesis of grandisines B, D, and F
-
This article describes in detail the first total synthesis of grandisine alkaloids, grandisines B, D, and F, which show affinity for the human b-opioid receptor. The key steps in this synthesis are construction of the isoquinuclidinone moiety of 2 by intr
- Kurasaki, Haruaki,Okamoto, Iwao,Morita, Nobuyoshi,Tamura, Osamu
-
experimental part
p. 12754 - 12763
(2010/06/14)
-
- SYNTHETIC PROCESS FOR AMINOCYCLOHEXYL ETHER COMPOUNDS
-
Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates and substrates are disclosed.
- -
-
Page/Page column 126
(2008/06/13)
-
- Beta-substituted-gamma-butyrolactones and a process for preparation thereof
-
The present invention is related to a process for the preparation of (S)- or (R)-β-substituted-γ-butyrolactones or a racemic mixture thereof. β-substituted-γ-succinic anhydrides are converted by zinc borohydride in a compatible solvent selected from tetra
- -
-
-
- Enantioselective entry to the Homalium alkaloid hoprominol: Synthesis of an (R,R,R)-hoprominol derivative
-
The diastereoselective synthesis of the N- and O-protected hoprominol derivative (R,R,R)-6 is described. The building up of the bicyclic O-silylated and di(N-tosylated) asymmetric scaffold 6 succeeded by convergent preparation of the two basic chiral azalactam units 7a and 7b and their subsequent iterative linking by a known method (Scheme 5). Both 4-alkyl-hexahydro-1,5-diazocin-2(1H)-ones 7a and 7b were prepared from the chiral β-amino acid portions 10a and 10b, respectively, by application of a set of reactions (e.g., N-alkylation of 10a,b and Sb(OEt)3-assisted cyclization of the resulting open-chain intermediates) already known. In comparison with the total syntheses of homaline (1) and homoprine (2), the newness of the described synthesis lies in the asymmetric approach to the difunctionalized fatty acid derivative 10b starting from (-)-(S)-malic acid (9) (Schemes 3 and 4). Key step in the preparation of 10b was the diastereoselective amination of the optically pure α,β-unsaturated δ-hydroxy homoallylic ester 14 via conjugate intramolecular aza-Michael cyclization of the acylic δ-(carbamoyloxy) intermediate 11.
- Ensch, Corinne,Hesse, Manfred
-
p. 233 - 246
(2007/10/03)
-
- Synthesis of new triazamacrocycles N-functionalised with α-(S)- hydroxycarboxylic acid pendant-arms
-
The synthesis of two new macrocyclic ligands, N,N',N''-tris[2(S)- hydroxybutyric acid]-1,4,7-triazacyclononane and N,N',N''-tris[2(S)- hydroxybutyric acid]-1,5,9-triazacyclododecane is reported. Each macrocycle bears three L-lactate-like pendant arms. Starting from L-malic acid, the absolute configuration of the α-(S)-hydroxy acid was kept along the synthesis leading to pure (S,S,S) enantiomers.
- Delagrange, Samuel,Nepveu, Francoise
-
p. 4989 - 4992
(2007/10/03)
-
- Enantioselective Synthesis of Pyrrolydinonyl Thymine Nucleoside Analogues
-
Enantioselective synthesis of a novel kind of optically active nucleoside analogues from natural malic acid is described. In the given nucleoside analogues the tetrahydrofuran ring is replaced by a pyrrolidinonyl ring bearing both a primary and a secondary hydroxy groups which could be useful for the preparation of novel oligonucleotides. Assay of the prepared nucleoside analogues showed non-activity against virus.
- Jin, Liren,Wu, Hong,Wu, Huailing,Huang, Peiqiang,Jung, Kyeongeun,Lim, Hong
-
p. 687 - 688
(2007/10/03)
-
- Synthesis of terminal disaccharide elements corresponding to the Ogawa and Inaba antigenic determinant from Vibrio cholerae O1
-
Vibrio cholerae O1 LPS terminal mono- and disaccharide elements were synthesized by reduction of the azido group in several 4-amino-4,6-dideoxy- D-mannose mono- and disaccharide derivatives, followed by coupling with 2,4- di-O-acetyl-3-deoxy-L-glycero-tetronic acid in the presence of 2-ethoxy-l- ethoxycarbonyl-1,2-dihydroquinoline. This compound represents a useful model in order to elucidate the size of the epitopes which define Ogawa and Inaba serotypes from Vibrio cholerae O1.
- Arencibia-Mohar, Adriana,Ariosa-Alvarez, Alina,Madrazo-Alonso, Odalys,Abreu, Elba Gonzalez,Garcia-Imia, Luis,Sierra-Gonzalez, Gustavo,Verez-Bencomo, Vicente
-
p. 163 - 170
(2007/10/03)
-
- Studies towards the synthesis of (+)-ptilomycalin A; stereoselective N-acyliminium ion coupling reactions to enantiopure C-2 substituted lactams
-
Highly stereoselective N-acyliminium ion coupling reactions of β-ketoester derived silyl enol ethers with enantiopure lactams derived from (S)-malic acid are reported. This reaction type is applied in the synthesis of the enantiopure C-2 substituted lactam 27, a plausible intermediate in a projected synthesis of ptilomycalin A.
- Louwrier, Saskia,Ostendorf, Martin,Boom, Arnoud,Hiemstra, Henk,Speckamp, W. Nico
-
p. 2603 - 2628
(2007/10/03)
-
- Novel stereoselective synthesis of (-)-enterolactone employing chiral unsaturated lactam
-
A novel convergent synthetic methodology of chiral antileukemic lignan lactones was developed by the use of optically active N-alkyl-α,β-unsaturated lactam elaborated from L-malic acid and the asymmetric synthesis of (-)-enterolactone was accomplished in short and simple steps.
- Yoda, Hidemi,Kitayama, Hidekazu,Katagiri, Takao,Takabe, Kunihiko
-
p. 3313 - 3322
(2007/10/02)
-
- Synthesis and Absolute Configuration of the Aristotelia Alkaloid Peduncularine
-
The first synthesis of the Aristotelia alkaloid peduncularine (1) is described.The synthetic sequence commences with (S)-malic acid and amounts to 16 steps.Key transformations are (1) the stereoselective transalkylation of the β-hydroxylactam dianion deri
- Klaver, Wim J.,Hiemstra, Henk,Speckamp, W. Nico
-
p. 2588 - 2595
(2007/10/02)
-
- Optisch aktive Lycopin-epoxide und Lycopin-glycole: Synthesen und chiroptische Eigenschaften
-
We present extensive spectral and chiroptical data on the pure and crystalline lycopene diepoxides 1-3 and glycols 4-9.A first synthetic approach to 1-9 with (+)-malic acid as starting material afforded 30 as a complex mixture of isomers (Scheme 1).Pure stereoisomers 1-9 were obtained using the enantiomerically pure epoxygeraniol 31 as starting material (Scheme 2).Differentiation of the (5Z)- from the (all-E)-isomers by 1H-NMR and UV/VIS alone is very difficult.
- Meier, Heidi,Uebelhart, Peter,Eugster, Conrad Hans
-
p. 106 - 123
(2007/10/02)
-
- Prostaglandins. 2. Synthesis of Prostaglandin F2α in Optically Active Form from Chiral Precursors
-
A synthetic route to optically active prostaglandins is described which use chiral starting materials.Acylation of the bis(magnesiobromide) salt of methyl hemimalonate with (S)-(-)-2-acetoxysuccinyl chloride led to unstable dimethyl (S)-4-acetoxy-3,6-diox
- Johnson, Francis,Paul, K.G.,Favara, Duccio,Ciabatti, Romeo,Guzzi, Umberto
-
p. 2190 - 2198
(2007/10/02)
-
