18542-42-2Relevant articles and documents
Synthesis in solution of peptoids using Fmoc-protected N-substituted glycines
Kruijtzer, John A. W.,Liskamp, Rob M. J.
, p. 6969 - 6972 (1995)
A convenient synthesis of Fmoc-protected N-substituted glycine derivatives starting from ethyl bromoacetate is described. As an illustration of the use of these building blocks for the preparation of peptoids, the synthesis of the C-terminal penta retropeptoid of Substance P (SP) is shown.
Synthesis and optical properties of sulfur-containing monomers and cyclomatrix polyphosphazenes
Fushimi, Toshiki,Allcock, Harry R.
, p. 5349 - 5355 (2010)
Novel cyclotriphosphazenes with sulfur-containing spirocyclic side groups were synthesized and polymerized to cyclomatrix materials for potential optical applications. The cyclotriphosphazenes were designed to give a high content of the phosphazene unit and sulfur atoms, as well as the capability for polymerization by ring- opening of the side groups. The chemical structures of the monomers were confirmed by NMR spectrometry, mass spectrometry, and single-crystal X-ray diffraction. Transparent solids were obtained by thermal bulk polymerization, and these were analyzed by the use of DSC, infrared spectroscopy, and mass spectrometry. One of the resultant cyclomatrix polyphosphazenes had a refractive index at 589 nm of 1.6465 and an Abbe number of 39. The contribution of the phosphazene unit to the refractive index is discussed.
The chemistry of methyltitanium trichloride. II. Variable-temperature nuclear magnetic resonance and infrared spectra of some complexes of methyltitanium trichloride and of titanium tetrachloride with unsymmetrical bidentate ligands
Clark,McAlees
, p. 342 - 348 (1972)
The pseudooctahedral complexes of methyltitanium trichloride with the unsymmetrical bidentate ligands methyl β-dimethylaminoethyl ether, methyl β-methylthioethyl ether, and methyl β-dimethylaminoethyl sulfide are precipitated on mixing hexane solutions of methyltitanium trichloride and the appropriate ligand. They are intensely colored solids, extremely sensitive to atmospheric oxygen and moisture and thermally unstable, decomposing gradually on storage in vacuo at room temperature. The nmr spectra of the complexes show that, in solution, they prefer to adopt that meridional configuration in which the harder ligand atom lies trans to the titanium-methyl group. In their ir spectra, the complexes all show bands in the 450-490-cm-1 region, which are assigned to v(Ti-C). These bands are absent from the ir spectra of the corresponding complexes of titanium tetrachloride, which we have also prepared and characterized (mainly to assist in the assignment of nmr data). By contrast to the foregoing, the product isolated from the reaction of methyltitanium trichloride with N,N,N′,-N′-tetramethyl-o-aminobenzylamine (B) is a titanium(III) derivative which can be formulated as TiCl3 · B.
Application of sulforaphane and derivatives thereof as bacterial effector protein transcription inhibitor
-
Paragraph 0073; 0075-0077, (2021/03/31)
The invention discloses application of sulforaphane and derivatives thereof as a bacterial effector protein transcription inhibitor. The invention provides an application of sulforaphane and derivatives thereof in any one of application of the following 1) and 7): 1) prevention and treatment of pathogenic bacteria; 2) improvement of the resistance of plants to pathogenic bacteria; 3) inhibiting ofpathogenicity of pathogenic bacteria; 4) inhibiting of the function of a pathogenic bacterium III type secretion system; 5) inhibiting of the expression of effector protein related genes of a pathogenic bacterium type III secretion system; 6) inhibiting of the expression of a pathogenic bacteria transcription factor hrpL; and 7) using as a pathogenic bacteria effector protein transcription inhibitor. Experiments prove that the sulforaphane and the derivatives thereof can inhibit the function of a pathogenic bacteria type III secretion system by specifically inhibiting transcription of the pathogenic bacteria type III secretion system, can resist invasion of pathogenic bacteria without destroying interaction between plants and beneficial microorganisms, and have a wide application prospectin prevention and treatment of plant pathogenic bacteria.
Engineering Catalysts for Selective Ester Hydrogenation
Dub, Pavel A.,Batrice, Rami J.,Gordon, John C.,Scott, Brian L.,Minko, Yury,Schmidt, Jurgen G.,Williams, Robert F.
, p. 415 - 442 (2020/03/04)
The development of efficient catalysts and processes for synthesizing functionalized (olefinic and/or chiral) primary alcohols and fluoral hemiacetals is currently needed. These are valuable building blocks for pharmaceuticals, agrochemicals, perfumes, and so forth. From an economic standpoint, bench-stable Takasago Int. Corp.'s Ru-PNP, more commonly known as Ru-MACHO, and Gusev's Ru-SNS complexes are arguably the most appealing molecular catalysts to access primary alcohols from esters and H2 (Waser, M. et al. Org. Proc. Res. Dev. 2018, 22, 862). This work introduces economically competitive Ru-SNP(O)z complexes (z = 0, 1), which combine key structural elements of both of these catalysts. In particular, the incorporation of SNP heteroatoms into the ligand skeleton was found to be crucial for the design of a more product-selective catalyst in the synthesis of fluoral hemiacetals under kinetically controlled conditions. Based on experimental observations and computational analysis, this paper further extends the current state-of-the-art understanding of the accelerative role of KO-t-C4H9 in ester hydrogenation. It attempts to explain why a maximum turnover is seen to occur starting at 25 mol % base, in contrast to only 10 mol % with ketones as substrates.
SYNTHESIS OF FLUORO HEMIACETALS VIA TRANSITION METAL-CATALYZED FLUORO ESTER AND CARBOXAMIDE HYDROGENATION
-
Paragraph 0194, (2020/11/24)
This application is directed to use of transition metal-ligand complexes to hydrogenate fluorinated esters and carboxamides into fluorinated hemiacetals. Methods for synthesis of certain ligands are also provided.
Preparation method of indoleamine 2,3-dioxygenase inhibitor and intermediates thereof
-
Paragraph 0195-0201, (2019/07/16)
The invention relates to a preparation method of an indoleamine 2,3-dioxygenase inhibitor and intermediates thereof. The invention discloses a preparation method capable of industrialization. By the method, problems of long synthetic route, low yield and unsuitable industrialization in the prior art are solved. The invention also relates to some intermediates for generating the indoleamine 2,3-dioxygenase inhibitor, especially an intermediate as shown in the general formula (I).
Preparation method of lapatinib intermediate 2-(methanesulfonyl)ethylamine hydrochloride
-
Paragraph 0011; 0038-0040, (2017/10/13)
The invention discloses a preparation method of lapatinib intermediate 2-(methanesulfonyl)ethylamine hydrochloride. The preparation method comprises the steps of adopting 2-chloroethylamine hydrochloride (Compound 2) as a starting material, and under an alkaline condition, carrying out dimolecular substitution reaction on the starting material and sodium methyl mercaptide to prepare 2-methylmercapto ethylamine (Compound 3); then adopting water as a solvent, adding hydrochloric acid for salifying, and directly using hydrogen peroxide for oxidizing to obtain the 2-(methanesulfonyl)ethylamine hydrochloride (Compound 1). According to the preparation method provided by the invention, a synthetic route is short, the raw materials are simple and easy to get, the water is adopted as the solvent, the reaction condition is moderate, the after-treatment is simple, and the obtained product is good in quality and high in yield. The method can cause less three wastes, and is environmentally friendly and suitable for industrial production. The formula is shown in the specification.
Kengreal intermediates as well as preparation methods and application thereof
-
Paragraph 0085; 0086; 0087; 0088, (2017/08/27)
The invention discloses Kengreal intermediates as well as preparation methods and an application thereof. The intermediates respectively comprise chemical structures as shown in formula VI and formula VII. The intermediates can be applied to synthesis of a known key intermediate TEPAD of Kengreal, and the method has advantages of high total molar yield, simple operation without special requirements for equipment, safety without pollution, low cost, and the like; the method has extremely high practical value for industrialization of Kengreal, and compared with the prior art, the method has significant progress.
PROCESS FOR HOMOGENEOUSLY CATALYZED, HIGHLY SELECTIVE DIRECT AMINATION OF PRIMARY ALCOHOLS WITH AMMONIA TO PRIMARY AMINES WITH A HIGH VOLUME RATIO OF LIQUID PHASE TO GAS PHASE AND/OR HIGH PRESSURES
-
Paragraph 0075, (2013/09/26)
The present invention relates to a process for preparing primary amines comprising the process steps A) provision of a solution of a primary alcohol in a fluid, nongaseous phase,B) contacting of the phase with free ammonia and/or at least one ammonia-releasing compound and a homogeneous catalyst and optionallyC) isolation of the primary amine formed in process step B), characterized in that the volume ratio of the volume of the liquid phase to the volume of the gas phase in process step B is greater than 0.05 and/or in that process step B is carried out at pressures greater than 10 bar.
