- Amphiphilic dendrimer, synthesis method thereof, and application of amphiphilic dendrimer as drug delivery system
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The invention relates to a microenvironment response type amphiphilic dendrimer, a synthesis method thereof, and application of the microenvironment response type amphiphilic dendrimer as a drug delivery system. The microenvironment response type amphiphilic dendrimer is a compound with a structure as shown in a formula (I), a formula (II) or a formula (III) or pharmaceutically acceptable salt of the compound. The compound disclosed by the invention can be used as the nano delivery system based on tumor microenvironment specific response, has good solubility in an aqueous solution, can be self-assembled with a drug in the aqueous solution to form a relatively stable nano compound, can effectively deliver the loaded drug to a tumor site; and can responsively disassembl the nano-drug delivery carrier under corresponding stimulation to achieve the purpose of accurate drug release, so that the drug can be released to the focus part to the greatest extent, and the compound is a novel nano-delivery carrier.
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Paragraph 0096-0097; 0108-0110; 0147-0148; 0157-0158
(2021/08/07)
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- Continuous photochemical production of high purity linear mercaptan and sulfide compositions
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Continuous photochemical production of high purity linear mercaptan and sulfide-containing compositions.
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Page/Page column 24
(2021/11/03)
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- Silylating Disulfides and Thiols with Hydrosilicones Catalyzed by B(C6F5)3
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Hydrosilanes and silicones, catalyzed with B(C6F5)3, may be used to silylate thiols or cleave disulfides giving silyl thio ethers. Alcohols were found to react faster than thiols or disulfides, while alkoxysilanes (the Piers-Rubinsztajn reaction) were slower such that the overall order of reactivity was found to be HO>HS>SS>SiOEt. The resulting silane and silicone-protected thio ethers produced from the sulfur-based functional groups could be cleaved to thiols using alcohols or mild acid with rates that depend on the steric bulk of the siloxane.
- Brook, Michael A.,Liao, Mengchen,Zheng, Sijia
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supporting information
p. 2694 - 2700
(2021/06/25)
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- Nonenzymatic Dynamic Kinetic Resolution of in situ Generated Hemithioacetals: Access to 1,3-Disubstituted Phthalans
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The first nonenzymatic DKR reaction of hemithioacetals is developed. Hemithioacetals were formed in situ via thiol addition and subsequently underwent an intramolecular oxa-Michael reaction. The scope of the reaction was quite broad ranging from aliphatic to aromatic substituents and 1,3-disubstituted-1,3-dihyroisobenzofuran products were obtained in good yields with moderate diastereoselectivities and high enantioselectivities. (Figure presented.).
- Nath, Utpal,Chowdhury, Deepan,Pan, Subhas Chandra
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p. 1628 - 1633
(2018/03/21)
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- Two-step three-component process for one-pot synthesis of 8-alkylmercaptocaffeine derivatives
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A highly efficient, odourless and two-step three-component process for one-pot synthesis of some 8-alkylmercaptocaffeine derivatives has been described. The catalyst-free three-component reaction of alkyl bromides, thiourea, and 8-bromocaffeine gave 8-alkylmercaptocaffeine products in excellent to quantitative yields. In addition, the impact of parameters on sample reaction is discussed.
- Rad, M. N. Soltani,Maghsoudi
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p. 70335 - 70342
(2016/08/06)
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- SYNTHETIC METHOD FOR THE PREPARATION OF 1, 2-BENZISOTHIAZOLIN-3-ONE
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The present invention relates to a method for producing a 1,2-benzisothiazolin-3-one compound (I) by reacting a 2-halobenzonitrile compound (II) with a thiol compound (III) to form an intermediate (IV) and subsequently reacting the intermediate (IV) with a halogenation agent in the presence of water to form a reaction mixture (RM), comprising the 1,2-benzisothiazolin-3-one compound (I) and a halide compound (V).
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- Synthetic method for the preparation of 1,2-Benzisothiazolin-3-one
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The present invention relates to a method for producing a 1,2-benzisothiazolin-3-one compound (I) by reacting a 2-halobenzonitrile compound (II) with a thiol compound (III) to form an intermediate (IV) and subsequently reacting the intermediate (IV) with a halogenation agent in the presence of water to form a reaction mixture (RM), comprising the 1,2-benzisothiazolin-3-one compound (I) and a halide compound (V). R3-SH (III), R3_X1(V),
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Paragraph 0159; 0160; 0161
(2015/12/18)
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- Flavouring and odorant thiols from renewable natural resources by InIII-catalysed hydrothioacetylation and lipase-catalysed solvolysis
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A chemoenzymatic access to thiol compounds, including ethyl 3-thiobutanoate, 3-thio-p-menthene and 8-thio-p-menthan-2-one, three compounds of interest in flavour and fragrance chemistry presenting various fruity notes, is proposed. It involves an indium(III)-catalysed hydrothioacetylation of renewable precursors followed by an enzymatic solvolysis of the obtained thioesters by lipases in aqueous or organic solvents.
- Dia, Reine-Marie,Belaqziz, Rim,Romane, Abderrahmane,Antoniotti, Sylvain,Du?ach, Elisabet
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scheme or table
p. 2164 - 2167
(2010/06/13)
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- Oxidation/reduction interconversion of thiols and disulfides using hydrogen and oxygen catalyzed by a rhodium complex
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RhH(PPh3)4 catalyzes reduction of disulfides to thiols by hydrogen and RhH(PPh3)4/1,4- bis(diphenylphosphino)butane (dppb) catalyzes oxidation of thiols to disulfides by oxygen.
- Arisawa, Mieko,Sugata, Chiyoshi,Yamaguchi, Masahiko
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p. 6097 - 6099
(2007/10/03)
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- Synthesis and antifungal activities of alkyl N-(1,2,3-thiadiazole-4-carbonyl) carbamates and S-alkyl N-(1,2,3-thiadiazole-4-carbonyl) carbamothioates
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A series of alkyl N-(1,2,3-thiadiazole-4-carbonyl) carbamates and S-alkyl N-(1,2,3-thiadiazole-4-carbonyl) carbamothioates with unsubstituted or monobrominated straight chain alkyl groups were synthesized and evaluated as fungistatic agents against Gibberella zeae and Altemaria kikuchiana. These compounds showed variable antifungal activities at concentrations of 5 and 50 μg/mL The results showed that antifungal activities depended on the length of the alkyl chain with the optimal chain length of 6-11 carbons. Carbamic acid, (1,2,3-thiadiazole-4-ylcarbonyl)-, hexyl ester (4) showed a strong fungistatic activity against A. kikuchiana at both concentrations, with 90.7 and 54% growth inhibition at 50 and 5 μg/mL, respectively. Carbamic acid, (1,2,3-thiadiazole-4-ylcarbonyl)-, heptyl ester (5); Carbamic acid, (1,2,3-thiadiazole-4-ylcarbonyl)-, octyl ester (6); and Carbamic acid, (1,2,3-thiadiazole-4-ylcarbonyl)-, undecyl ester (9) showed strong fungistatic activity against G. zeae at both concentrations. Their growth inhibitions against G. zeae at the concentration of 5 μg/mL were 78, 63, and 59%, respectively.
- Li, Zaifeng,Wu, Zengru,Luo, Fuying
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p. 3872 - 3876
(2007/10/03)
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- Water effects on SmI2 reductions: A novel method for the synthesis of alkyl thiols by SmI2-promoted reductions of sodium alkyl thiosulfates and alkyl thiocyanates
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Water as a cosolvent has significant improving effect on the reductivity of SmI2 in the reduction of sodium alkyl thiosulfates and alkyl thiocyanates. A new method for synthesis of alkyl thiols by SmI 2/THF/H2O system has been developed.
- Zhan, Zhuang-Ping,Lang, Kai,Liu, Feng,Hu, Li-Ming
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p. 3203 - 3208
(2007/10/03)
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- A general and mild synthesis of thioesters and thiols from halides
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The conversion of a wide variety of halides to thioesters by reaction with potassium thiocetate under mild conditions is described, and the generality of the method is demonstrated.
- Zheng, Tu-Cai,Burkart, Maureen,Richardson, David E.
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p. 603 - 606
(2007/10/03)
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- Mild, selective deprotection of thioacetates using sodium thiomethoxide
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A mild method for the deprotection of thioacetates is described. The reaction can be conveniently carried out at room temperature, and is compatible with a wide range of functionality. The procedure was shown to chemoselectively remove a thioacetate in the presence of an acetate.
- Wallace, Owen B.,Springer, Dane M.
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p. 2693 - 2694
(2007/10/03)
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- Mechanism of the Solution-Phase Reaction of Alkyl Sulfides Atomic Hydrogen. Reduction via a 9-S-3 Radical Intermediate
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The low selectivity of benzyl alkyl sulfide fragmentation subsequent to its reaction with atomic hydrogen is indicative of a reaction that proceeds via an early transition state. The competitive reduction of a series of substituted-benzyl alkyl sulfides was insensitive to the substituent on the aromatic ring (ρ = -0.13, r = 0.99). The relative rates of fragmentation of a series of the substituted-benzyl alkyl sulfides gave a V-shaped Hammett plot. Both electron-donating and electron-withdrawing groups destabilized the transition state (ρ = +0.99, r = 0.999; ρ = -0.82, r = 0.992). Since the relative rates of disappearance of the alkyl benzyl sulfides are not substituent dependent, but the relative rates of fragmentation are, a 9-S-3 intermediate is preferred as the structure leading to products.
- Tanner, Dennis D.,Koppula, Sudha,Kandanarachchi, Pramod
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p. 4210 - 4215
(2007/10/03)
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- β-carboxy sulfonamide ACAT inhibitors
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β-Carboxy sulfonyl compounds of the formula STR1 wherein R1 is aryl, R3 is hydrogen or alkyl, R3 and R4 are hydrogen or alkyl, Y is --O--, --S--, or --NR2 --, and R5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.
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- Direct synthesis of thiols from halides and epoxides using hydrosulfide exchange resin in methanol
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Various thiols are prepared directly from the corresponding alkyl halides and epoxides using hydrosulfide exchange resin in methanol in the presence of equimolar amounts of triethylammonium chloride at room temperature. The reaction not only proceeds with unique chemoselectivity, but also gives better yields of thiols than most commonly used indirect methods and has an additional advantage of a simple workup.
- Choi,Yoon
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p. 373 - 375
(2007/10/02)
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- Synthesis of thiols via palladium catalyzed methanolysis of thioacetates with borohydride exchange resin
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Various thiols are prepared quantitatively from the corresponding thioacetates via Pd catalyzed methanolysis with borohydride exchange resin under a mild and neutral conditions. One-pot synthesis of thiols from alkyl halides through the formation of alkyl thioacetates using thioacetate exchange resin followed by methanolysis is also described.
- Choi,Yoon
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p. 2655 - 2663
(2007/10/02)
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- Kinetic and ab Initio Theoretical Study of Hydrogen Atom Abstraction from Thiols by Thiyl Radicals: Basis Rate Expressions for Reactions of Sulfur-Centered Radicals
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Arrhenius rate expressions were determined for the abstraction of hydrogen atom from thiophenol and hexanethiol by the octanethiyl radical at 25-100 deg C in nonane.Octanethiyl radicals were produced by steady-state photolysis of octyl thiobenzoate.Analysis of octyl disulfide and octanethiol provided relative rate expressions for abstraction of hydrogen atom from thiols versus self-termination of the octanethiyl radical.For hexanethiol, log (kabs/kt1/2) = (2.94 +/- 0.29) - (3.84 +/- 0.41)/θ, and for thiophenol, log (kabs/kt1/2) = (2.56 +/- 0.19) - (2.88 +/- 0.28)/θ; θ = 2.3 RT kcal/mol.Combining these expressions with the Smoluchowski expression for self-termination of octanethiyl in nonane, log (kt1/2) = 5.96 - 1.335/θ, which employs experimental diffusion coefficients of octanethiol and a spin selection factor ? = 1, yields, for thiophenol, log (kabs/M-1 s-1) = (8.52 +/- 0.18) - (4.22 +/- 0.27)/θ, and for hexanethiol, log (kabs/M-1 s-1) = (8.90 +/- 0.29) - (5.18 +/- 0.41)/θ (errors are 2?).The rate of disappearance of octanethiyl/diphenylketyl radical pairs in SDS micelles, determined by nanosecond optical spectroscopy, was found to be unchanged in a 700-G magnetic field, providing evidence for rapid intersystem crossing of sulfur-centered radical pairs and support for the assignment of ? = 1 above.Ab initio electronic structure calculations on the reaction HS. + HSH -> HSH + .SH, performed at SCF and correlated levels, predict an activation barrier of ΔH(excit.)298 = 4.6 kcal/mol, in close agreement with the experimental barrier for the octanethiyl + hexanethiol reaction.
- Alnajjar, M. S.,Garrossian, M. S.,Autrey, S. T.,Ferris, K. F.,Franz, J. A.
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p. 7037 - 7043
(2007/10/02)
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- A practical, one-step synthesis of primary thiols under mild and neutral conditions using bis(triorganotin) sulfides
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Thiols are obtained from primary organic halides and bis(triaryl/alkyltin) sulfides in the presence of fluoride ion in CH3CN/H2O at 20°C. This simple one-step methodology involving fluorodestannylation is carried out under mild and neutral conditions, in sharp contrast to virtually all known methods. Some attempts at utilizing triorganotin and triorganogermanium mercaptans for the same purpose are reported.
- Gingras,Harpp
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p. 1397 - 1400
(2007/10/02)
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- Rapid and Selective Reduction of Functionalized Aromatic Disulfides with Lithium Tri-tert-butoxyaluminohydride. A Remarkable Steric and Electronic Control. Comparison of Various Hydride Reagents
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Lithium tri-tert-butoxyaluminohydride (LTBA), an exceptionally mild reducing agent in organic synthesis, reduces functionalized aromatic disulfides to the corresponding thiols in quantitative yield.The reaction is rapid (for example, o-tolyl disulfide is reduced to completion in 60 min at 25 deg C) and can tolerate a wide variety of functional groups, such as halogen, nitro, carboxylic acid, and their derivatives.The presence of electron-withdrawing substituents dramatically enhances the rate of reduction (p-chlorophenyl disulfide is quantitatively reduced in 30 s) and electron-releasing substituents diminishes the rate of cleavage.The reaction is sensitive to steric effects (2,4-di-tert-pentylphenyl disulfide underwent 25percent reduction in 24 h).However, such hindered disulfides can be rapidly and quantitatively reduced in refluxing THF.The reaction of LTBA with alkyl disulfides is extremely sluggish.The reaction provides a useful and simple means for the facile and selective reduction of aromatic disulfides where this is required in synthetic operations.
- Krishnamurthy, S.,Aimino, D.
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p. 4458 - 4462
(2007/10/02)
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- Sulfur-containing imidazoles
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Novel imidazole mercaptals of the formula STR1 wherein each m is independently zero or one; and R1 and R2 each are independently selected from (lower)alkyl, cycloalkyl, cycloalkyl(lower)alkyl, phenyl, phenyl(lower)alkyl, thienyl, thienyl(lower)alkyl, pyridyl and pyridyl(lower)alkyl, in which the phenyl and heterocyclic rings optionally may contain from 1 to 3 substituents, and acid addition salts thereof, are useful antimicrobial agents.
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- A Novel Method for the Preparation of Thioformates and Thiols by using Thioformimidates
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Several new S-alkylated thioformimidates were synthesized and their applications to the synthesis of thiolformates and thiols were investigated.Keywords - thioformimidates; thiols; thiolformates; thioformanilide; Michel-type addition
- Matsubara, Yoshio,Nakamura, Toshiyuki,Yoshihara, Masakuni,Maeshima, Toshihishi
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p. 3389 - 3391
(2007/10/02)
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- Desulfuration Using Plasma Techniques, III. - Reaction of Thioethers
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Plasma desulfurations were tested with nine thioethers.While aliphatic, as well as aromatic thioethers and thiophene react easily, benzothiophenes are hard to desulfurize.Predominant reaction products are low molecular alkenes and alkanes (Table 1).Addition of oxygen greatly improves the results (Table 2).
- Suhr, Harald,Henne, Peter,Iacocca, Diodoro,Ropero, Marcos J.
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p. 441 - 446
(2007/10/02)
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- Antimicrobial composition and method containing N-(3,5-dihalophenyl)-imide compounds
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Novel N-(3,5-dihalophenyl)imide compounds, which exhibit a strong antimicrobial activity against microorganisms including phytopathogenic fungi, parasites of industrial products and pathogenic microorganisms, represented by the formula, STR1 wherein X and X' each represent halogens and A represents a substituted ethylene such as chloroethylene, C1 - C4 alkylthioethylene, C1 - C2 alkyl-ethylene or 1,2-di-C1 - C2 -alkyl-ethylene, a cyclopropylene such as 1,3-dimethylcyclopropylene, trimethylene, a cyclohexylene-1,2-, cyclohexenylene-1,2-, cyclohexadienylene-1,2- or o-phenylene. The N-(3,5-dihalophenyl)imide compounds can be obtained by any of methods which produce imide compounds or reaction of an N-(3,5-dihalophenyl)maleimide compound with a mercaptan, a hydrogen halide, phosphorus chloride or thionylchloride.
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- 3-Aryl-2-halothiopropionic acid s-esters
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Novel 3-aryl-2-halothiopropionic acid compounds of the formula STR1 wherein X is chlorine or bromine, R1 is hydrogen, a salt-forming cation, an aliphatic radical or a substituted aliphatic radical wherein the substituent is halogen, haloalkyl, hydroxy, alkoxy, alkoxy-carbonyl or aryl, R2 is hydrogen, halogen or alkyl R3 is hydrogen or alkyl n is an integer from 0 to 3; and R4 is halogen, alkyl, haloalkyl or nitro and wherein the radical R4, when n is 2 or 3, may be the same or different, Are outstandingly effective herbicides, exhibiting particularly selective action.
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