- Antibody drug conjugate, intermediate, preparation method, pharmaceutical composition and uses thereof
-
Disclosed are an antibody drug conjugate IB, which uses ether linkages for connection, and improves the water solubility, stability and cytotoxicity in vivo and in intro, and an intermediate, a pharmaceutical composition, and uses of the antibody drug conjugate. The antibody drug conjugate has simple synthetic steps and a high yield.
- -
-
Page/Page column 108; 110
(2019/11/11)
-
- Fe2O3-Promoted Intermolecular Chlorotrifluoromethylthiolation of Alkenes
-
A simple, convenient method for intermolecular chlorotrifluoromethylthiolation of alkenes by using a low-cost and more abundant iron catalyst has been developed. This protocol provides a straightforward way to synthesize a variety of useful SCF3/sub
- Jia, Yimin,Qin, Hongmei,Wang, Na,Jiang, Zhong-Xing,Yang, Zhigang
-
p. 2808 - 2817
(2018/03/09)
-
- Aryl substituted phosphorothio amine derivatives and their use in medical application
-
The invention relates to an aryl-substituted phosphonaminate and an application of the aryl-substituted phosphonaminate in medical science, in particular to an aryl-substituted phosphonaminate showed in a general formula (I), stereoisomer of the aryl-subs
- -
-
Paragraph 0149-0153
(2017/09/12)
-
- Phosphamide derivative substituted by aryl group and medical applications thereof including a use in manufacturing drugs for treating virus infectious diseases
-
The present inventions relates to a phosphamide derivative substituted by an aryl group and medical applications thereof, which specifically relates to the phosphamide derivative substituted by an aryl group, stereoisomers thereof or the pharmaceutically
- -
-
Page/Page column 24; 25
(2017/10/14)
-
- 8034
-
Abstract A series of arabinose glycosyl sulfamides with varying alkyl chain types and lengths were synthesised as mimics of decaprenolphosphoarabinose (DPA), and as potential inhibitors of mycobacterial cell wall biosynthesis. Unprecedented conversion of
- Suthagar, Kajitha,Watson, Andrew J.A.,Wilkinson, Brendan L.,Fairbanks, Antony J.
-
p. 153 - 166
(2015/08/24)
-
- Synthesis of some acyclic quaternary ammonium compounds. Alkylation of secondary and tertiary amines in a two-phase system
-
A series of acyclic symmetrical and asymmetrical quaternary ammonium chlorides of the general formula R1R2R3N+AR4Cl- (R1 = Me, Bu; R2 = n-C12H25, PhCH2, C n H2n+1(OCH2CH2) m, n = 9 and 12, m = 1 and 2; R3 = n-C12H25, PhCH2, HOCH2CH2,-OOCCH2; R4 = n-C12H25, PhCH2; A = (CH2CH2O)1,2, CH2C(O)O) was synthesized by the alkylation of tertiary amines in a two-phase system containing water. A convenient method for the synthesis of the initial symmetrical and asymmetrical tertiary amines of the general formula MeNR1R2 (R1 = Me, Bu; R2 = n-C12H25, PhCH2, CnH2n+1(OCH2CH2) m, n = 9 and 12, m = 1 and 2) in an organic phase-aqueous phase heterogeneous system, which allows the use of aqueous solutions of alkali and amines, was developed. The improved method for the preparation of intermediate ethylene glycol and diethylene glycol monoethers is monoalkylation of glycols in dioxane using solid KOH in a two-phase system.
- Kharlamov,Artyushin,Bondarenko
-
p. 2445 - 2454
(2015/08/03)
-
- Towards the development of new subtype-specific muscarinic receptor radiopharmaceuticals - Radiosynthesis and ex vivo biodistribution of [ 18F]3-(4-(2-(2-(2-fluoroethoxy)ethoxy)ethylthio)-1,2, 5-thiadiazol-3-yl)-1-methyl-1,2,5,6-tetrahydropyrid
-
Muscarinic receptors have been implicated in neurological disorders including Alzheimer's disease, Parkinson's disease, and schizophrenia. Nineteen derivatives of thiadiazolyltetrahydropyridine (TZTP), a core that has previously shown high affinities towa
- Van Oosten, Erik M.,Wilson, Alan A.,Mamo, David C.,Pollock, Bruce G.,Mulsant, Benoit H.,Houle, Sylvain,Vasdev, Neil
-
experimental part
p. 1222 - 1232
(2011/02/24)
-
- Sulfate anion templated synthesis of a triply interlocked capsule
-
Sulfate templation has been used in the synthesis of a novel tris-urea-based triply interlocked capsule, whose structure has been verified by DOSY NMR, mass spectrometry and molecular modelling investigations. The Royal Society of Chemistry 2009.
- Li, Yitong,Mullen, Kathleen M.,Claridge, Tim D. W.,Costa, Paulo J.,Felix, Vitor,Beer, Paul D.
-
supporting information; experimental part
p. 7134 - 7136
(2010/03/25)
-
- The in vitro transport of model thiodipeptide prodrugs designed to target the intestinal oligopeptide transporter, PepT1
-
A thiodipeptide carrier system is shown to be effective at enabling a range of covalently bound molecules, including benzyl, benzoyl and ibuprofen conjugates, to be transported via the intestinal peptide transporter PepT1, demonstrating its potential as a rational drug delivery target.
- Foley, David,Pieri, Myrtani,Pettecrew, Rachel,Price, Richard,Miles, Stephen,Lam, Ho Kam,Bailey, Patrick,Meredith, David
-
supporting information; experimental part
p. 3652 - 3656
(2009/10/23)
-
- Synthesis of oligo(ethylene glycol) toward 44-mer
-
A synthetic method for oligo(ethylene glycol) toward 44-mer (FW = 1956.35) is described. Reiteration of Williamson's ether synthesis and hydrogenation to remove protecting benzyl group affords desired oligo(ethylene glycol) toward 44-mer in moderate yields. The advantages in this method are use of commercially easily available materials as starting materials and procedures avoiding difficulty in purification of the products as much as possible.
- Ahmed, Saleh A.,Tanaka, Mutsuo
-
p. 9884 - 9886
(2007/10/03)
-
- Highly selective Silver(I) oxide mediated monoprotection of symmetrical diols
-
Treatment of symmetrical diol with Ag2O and alkyl halide gave the monoprotected derivative in good to excellent yield.
- Bouzide, Abderrahim,Sauve, Gilles
-
p. 5945 - 5948
(2007/10/03)
-
- Ethoxylation of aralkyl alcohols
-
An important reaction, the oligoaddition of ethylene oxide to the alcoholic hydroxyl group was investigated.The aralkyl alcohols were chosen as base material: benzyl-, β-phenylethyl- and γ-phenylpropyl alcohols.The first members of their homologue ethoxylated series were prepared and used as standards for the determination of the average degree of ethoxylation (IR, UV, refractive indices) and of the molar mass distribution (HPLC).
- Huszar, Klara Parlagh,Klug, Otto,Parlagh, Gyula,Rusznak, Istvan,Sallay, Peter,et al.
-
p. 241 - 252
(2007/10/03)
-
- A novel way for hydroxyethylation by using clay catalysts
-
Hydroxyethylation of aralkyl alcohols (benzyl alcohol, 2-phenylethanol, 3-phenylpropanol) in the presence of a clay catalyst (K10) was successful. This method has some advantages in contrast with the conventional ones: effective, works at mild reaction conditions, ease the separation of catalyst from the reaction mixture.
- Sallay, Peter,Bekassy, Sandor,Ahmed, Mohamed H.,Farkas, Laszlo,Rusznak, Istvan
-
p. 661 - 664
(2007/10/03)
-
- Homogeneous hydroxyethylation of phenyl-substituted alcohols
-
Homogeneous glycol ether derivatives of phenyl group substituted alcohols (benzyl-, β-phenyl ethyl- and γ-phenyl propyl-) were synthesised by repeated Williamson synthesis starting in two cases from the halogen derivatives of the corresponding alcohols. In the case of β-phenylethanol the first homologue was prepared in the reaction of benzyl group protected ethylene chlorohydrine and β-phenyl-ethyl alcohol. The reaction product was hydrogenolysed (removing the benzyl group by hydrogenolyzis), halogenated and used to the synthesis of higher homologues as starting material.
- Sallay, Peter,Ahmed, Mohamed H. M.,Rusznak, Istvan,Farkas, Laszlo,Tungler, Antal
-
-
- Lack of effect of the length of oligoglycine- and oligo(ethylene glycol)-derived para-substituents on the affinity of benzenesulfonamides for carbonic anhydrase II in solution
-
Using 1H NMR spectroscopy, values of T2 have been determined for the methylene protons of the oligoglycine moieties of para-substituted benzenesulfonamides having structures H2NO2SC6H4CO(Gly)(n)OH (n = 1-6) bound at the active site of bovine carbonic anhydrase II (CA, EC 4.2.1.1). These values have been correlated with measurements of dissociation constants of these complexes, in order to infer motion of these ligands when bound to the enzyme. Motion of glycines 1-3 (those closest to the aryl ring) is hindered by their proximity to the protein; motion of glycines 4-6 is relatively unhindered. Despite the restriction to motion inferred for glycines 1-3, the values of K(d) for the six compounds (n = 1-6, 1-6) are indistinguishable within experimental uncertainty (± 20%): K(d) in μM (n) 0.30 (1); 0.26 (2); 0.33 (3); 0.37 (4); 0.37 (5); 0.34 (6). There is, therefore, an unexpected compensation of the loss in conformational entropy on binding by another contributor to the free energy.
- Jain, Ahamindra,Huang, Shaw G.,Whitesides, George M.
-
p. 5057 - 5062
(2007/10/02)
-
- Synthesis of Functionalised 12-,13- and 14-Membered Crown Ethers Bearing Exocyclic Polymerisable Groups and the Binding Properties and Conductivities of their Lithium Doped Polymers
-
The synthesis of a series of , and -membered crown ethers bearing an exocyclic polymerisable methacrylate is reported.The spacing group between the ring and the methacrylate is either a simple alkyl chain, or 6, or an oxydiethylene chain.The relative binding ability of the "mono and di-substituted" macrocyclic rings towards Li+ is compared by 13C NMR analysis.Radical polymerisation gives the amorphous polymers in which the glass transition temperature is primarily controlled by the nature of the spacer group.In the lithium doped polymers, for a given glass transition temperature, Tg, the -ring materials show enhanced ionic conductivities over the -ring analogues which may be related to the lower rate of lithium exchange (in the former series) or to an enhanced tendency of the -ring systems to form 2:1 complexes with more effective counterion separation.
- Collie, Luke,Denness, James E.,Parker, David,O'Carroll, Fiona,Tachon, Christine
-
p. 1747 - 1758
(2007/10/02)
-
- Competitive solvent extraction of alkali metal cations into chloroform by lipophilic acyclic proton-ionizable polyethers
-
A series of lipophilic acyclic polyether carboxylic acids and a corresponding polyether phosphonic acid monoethyl ester were synthesized in which the unit that contains the lipophilic and the proton-ionizable groups is held constant, but the polyether chain and its terminal group are systematically varied. Competitive solvent extraction of alkali metal cations from aqueous solutions into chloroform was performed to assess the influence of structural variation within the extractant molecule upon the extraction selectivity and efficiency. Many of the ionophores exhibited extraction selectivity for Li+. One of the simplest chelating agents gave an extraction selectivity order of Li+ ? Na+ > K+,Rb+ > Cs+ and a Li+/Na+ selectivity ratio of 4.9, while the selectivity ratios for Li+ over K+, Rb+, and Cs+ were 12 or higher.
- Walkowiak, Wladyslaw,Ndip, Grace M.,Desai, Dhimant H.,Lee, Han Koo,Bartsch, Richard A.
-
p. 1685 - 1690
(2007/10/02)
-
- Convenient One-pot Synthesis of (Z)-4-Benzyloxy-2-buten-1-ol
-
Simple and one-step procedure for the preparation of (Z)-4-benzyloxy-2-buten-1-ol from (Z)-2-buten-1,4-diol is described.
- Hiremath, S. V.,Reddy, D. R.,Kumar, M. Anil
-
-
- A NOVEL, UNEQUIVOCAL SYNTHESIS OF POLYETHYLENE GLYCOLS
-
Unequivocal synthesis of polyethyleneglycols is presented.The key step for this synthesis is the selective monobenzylation of oligoethyleneglycols by the phase transfer catalysis technique.
- Coudert, Gerard,Mpassi, Michel,Guillaumet, Gerald,Selve, Claude
-
-
- STREPTOCOCCUS PNEUMONIAE TYPE XIV POLISACCHARIDE: SYNTHESIS OF A REPEATING BRANCHED TETRASACCHARIDE WITH DIOXA-TYPE SPACER-ARMS
-
β-Glycosides of 2-acetamido-2-deoxy-D-glucopyranose were synthesised, using either 7-methoxycarbonyl-3,6-dioxa-1-heptanol or 8-azido-3,6-dioxa-1-octanol.Selective β-lactosylation of 7-methoxycarbonyl-3,6-dioxaheptyl 2-acetamido-3-O-benzyl-2-deoxy-β-D-glucopyranoside with hepta-O-acetyl-lactosyltrichloroacetimidate, followed by β-galactosylation of the secondary hydroxyl group with O-(2,3,4,6-tetra-O-acetyl-α-D-galactopyranosyl)trichloroacetamidate, catalytic hydrogenolysis, and O-deacetylation, gave 7-methoxycarbonyl-3,6-dioxaheptyl 2-acetamido-2-deoxy-4-O-β-D-galactopyranosyl-6-O-(4-O-β-D-galactopyranosyl-β-D-glucopyranosyl)-β-D-glucopyranoside.Selective β-lactosilation of 8-azido-3,6-dioxaoctyl 2-acetamido-3-O-benzyl-2-deoxy-β-D-glucopyranoside with hepta-O-acetyl-lactosyl bromide in the presence of silver triflate, followed by condensation with 2,3,4,6-tetra-O-acetyl-α-D-galactopyranosyl bromide in the presence of silver triflate, catalytic hydrogenolysis, and O-deacetylation, gave 8-azido-3,6-dioxaoctyl 2-acetamido-2-deoxy-4-O-β-D-galactopyranosyl-6-O-(4-O-β-D-galactopyranosyl-β-D-glucopyranosyl)-β-D-glucopyranoside.
- Amvam-Zollo, Paul-Henry,Sinay, Pierre
-
p. 199 - 212
(2007/10/02)
-
- 3-Fucosyl-N-acetyl lactosamine derivatives, and their biological applications
-
The invention relates to substitution derivatives of trisaccharide 3-fucosyl-N-acetyl lactosamine and to the immunological applications of these derivatives and of the trisaccharide itself particularly as diagnostic reagent and in therapy.
- -
-
-
- Multiple Benzo-fused Crown Ethers - Synthesis, Ion Selectivities in Membrane Electrodes and Inclusion of Water
-
New oligo-benzo-condensed crown-6 ligands 4, 6 - 9 having a different gradation of lipophilicity and of molecular rigidity are synthesized.For the known ligands 3 and 5 of similar constitution improved methods of preparation are described.The carrier efficiencies and ion selectivities of the various ligands for alkali and alkaline earth metal ions in liquid membrane electrodes of different composition are determined and discussed on the basis of the potentiometric selectivity factors lgKPotMgM.The possible behaviour of the new macrocycles in molecular inclusion is studied.A stable crystal lattice inclusion compound of 4 with water of composition 4*1/2 H2O is obtained.
- Weber, Edwin
-
p. 4439 - 4452
(2007/10/02)
-
- Synthesis of Lipophilic 18-Crown-6 Diacids for the Membrane Transport of Alkaline-Earth Cations
-
The synthesis of three different types of lipophilic 18-crown-6 diacids is described.A didecyl crown ether 2,3-diacid (1) was prepared as a minor product from a diiodide precursor (12) and threo-11,12-docosanediol by thallous ethoxide cyclization.The major nonpolymeric products resulted from elimination followed by cyclization to give 15-crown-5-derivatives.A crown ether 11,12-diamide 2,3-diacid (4) was prepared by a similar route involving cyclization of a benzyl protected precursor (26) and N,N,N',N'-tetramethyltartaramide (9).Isomeric syn and anti 2,11(12)-diamide 3,12(11)-diacid derivatives 6 and 7 were prepared from the known crown ether bisanhydride 8 and alkylamines.The product mixture was separated by chromatography, and the isomers were identified by comparison of acidity and stability constants for complexation with those of closely related syn/anti crown ether acids.
- Fyles, Thomas M.,McGavin, Cynthia A.,Whitfield, Dennis M.
-
p. 753 - 761
(2007/10/02)
-
- SYNTHESIS OF BISPEROXYDICARBONATES AND THEIR REACTIVITY
-
A series of symmetrical peroxydicarbonates were obtained from the chloroformates of diethylene or dipropylene glycol monoethers.Their homolysis in benzene and in the presence of styrene and α-naphthol was investigated.The effect of the structure of the organic fragment of the peroxide on the effective, induced, and monomolecular dissociation constants is discussed.A scheme is proposed for the transformation of the free radicals which form on the basis of kinetic data and analysis of the final thermal dissociation products.
- Fomin, V. A.,Etlis, V. S.,Nozrina, F. D.
-
-
- Topical mosquito repellents VII: Alkyl triethylene glycol monoethers
-
Normal and branched chain aliphatic monoethers of triethylene glycol are effective topical mosquito repellents. In terms of duration of protection, they are generally superior to the corresponding diethylene glycol analogs, and some are superior to diethyltoluamide. The n heptyl monoether of triethylene glycol affords double the protection time of diethyltoluamide under controlled laboratory conditions, and appears to be a useful new mosquito repellent.
- Johnson,DeGraw,Engstrom,Skinner,Brown,Skidmore,Maibach
-
p. 693 - 695
(2007/10/05)
-