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For skin ulcer care of pyrazolo [1, 5 – a] pyridine drug molecule and its preparation method and application (by machine translation)

The invention discloses a method for skin ulcer care of pyrazolo [1, 5 – a] pyridine drug molecule and its preparation method and application, which belongs to the technical field of medical synthesis. Technical proposal of the invention points are: for skin ulcer care of pyrazolo [1, 5 – a] pyridine pharmaceutical molecular, has the following molecular structure: The invention also specifically discloses the used for skin ulcer care of pyrazolo [1, 5 – a] pyridine pharmaceutical molecular preparation method and can be used for the skin ulcer care in the application of the pharmaceutical composition. The invention integrated sulfur aza compound has sedative, the promotion of growth hormone secretion, anti-ulcer, sterilizing and the like, to synthesize a for skin ulcer care of pyrazolo [1, 5 – a] pyridine pharmaceutical molecular and has carried on the antibacterial activity test, the detection of such compounds to the skin ulcer caused by bacillus anthracis and Staphylococcus aureus better to have inhibitory activity, and then made into pharmaceutical ointment and clinical care experiment, found care effect is more obvious. (by machine translation)

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Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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H2 storage abilities of some novel Pd(II) complexes containing 2H[1,4]benzothiazin-3(4H)-one

Initially, a novel series of mixed ligand Pd(II) complexes of 2H[1,4]benzothiazin-3(4H)-one (Hbto) and diamine or phosphine ligands were successfully prepared with yields of 61 to 92%. The treatment of Na2PdCl4 with Hbto in acetone with 1:2 Pd to Hbto ratio affords cis-[PdCl2(Hbto)2] (1) that delivers an appropriate entry into mixed-ligand Hbto complexes. The complex (1) was used as a precursor for preparation the complexes of the type [Pd(Hbto)2(kappa2-diamine)]Cl2; (diamine = en (2a), bipy (2b), phen (2c)) and [Pd(Hbto)2(kappa2-diphosphine)]Cl2; (diphosphine = dppm (3a), dppe (3b), dppp (3c), dppf (3d)). Likewise, the mono phosphine (PPh3) was used to prepare the contrast complex with complex (1), however, to dissipate the suspicion that define complex [Pd(Hbto)2(PPh3)2]Cl2 is present in the cis or trans structure, two methods were used to prepare this complex, both of which demonstrated that the cis is the preferred structure for the complex [Pd(Hbto)2(PPh3)2]Cl2 (4). For all as-prepared complexes, the characterization techniques (molar conductivity, IR, 1H-, 13C-{1H}, 31P-{1H}NMR and elemental analyses) prove that the Hbto links to Pd(II) in a mono-dentate fashion through the exocyclic oxygen atom. To benefit from the complexes prepared, some as-prepared complexes (1), (2b) and (4) have been evaluated for their H2 storage at 77 K after measuring the N2 adsorption/desorption isotherms in order to get some information about BET surface areas of the samples. The results demonstrate that the selected prepared complexes were all able of storing the H2 and among the complexes (1), (2b) and (4), (2b) was the best one and was able to store 5.4 wt% of H2 under 70 bar and 77 K.

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Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Reference of 72287-26-4, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.72287-26-4, Name is [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium(II), molecular formula is C34H28Cl2FeP2Pd. In a article£¬once mentioned of 72287-26-4

A 3-aryl-2-cyclopenten-1-one compound method for the synthesis of (by machine translation)

The invention relates to a kind of the following formula (III) shown in the 3 […] aryl -2 the […] cyclopentene -1 the method for synthesizing compound of […], the method comprising: under a nitrogen atmosphere, in an organic solvent, the catalyst, in the presence of alkali and, the following formula (I) compounds and the following formula (II) compound in 40 the […] 50 C reaction under the 1 […] 2 hours, then raise the temperature, in the 70 […] 80 C reaction under the 4 […] 6 hours, so as to obtain the compound of said formula (III), wherein R 1 to C 1 ? C 6 alkyl or C 1 ? C 6 alkoxythiophene; R 2 to C 1 ? C 6 alkyl or halogenated C 1 ? C 6 alkyl; X is or S N; n is 1 or 2. The stated method, through catalyst, alkali, organic solvent, etc. of the auxiliary agent and combined and synergies, and through the control of reaction temperature, thus the objective product may be obtained in a high yield, in the field of organic synthesis technology has good prospects and research potential application of. (by machine translation)

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Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Combination regimens using progesterone receptor modulators

This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 allyl C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alknyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, NO2, amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aminoalkyl, CORF, or NRGCORF; or pharmaceutically acceptable salt thereof. These methods of treatment may be used for contraception or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or inmization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.

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Reference£º
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Synthesis and characterization of the arylomycin lipoglycopeptide antibiotics and the crystallographic analysis of their complex with signal peptidase

Glycosylation of natural products, including antibiotics, often plays an important role in determining their physical properties and their biological activity, and thus their potential as drug candidates. The arylomycin class of antibiotics inhibits bacterial type I signal peptidase and is comprised of three related series of natural products with a lipopeptide tail attached to a core macrocycle. Previously, we reported the total synthesis of several A series derivatives, which have unmodified core macrocycles, as well as B series derivatives, which have a nitrated macrocycle. We now report the synthesis and biological evaluation of lipoglycopeptide arylomycin variants whose macrocycles are glycosylated with a deoxy-alpha-mannose substituent, and also in some cases hydroxylated. The synthesis of the derivatives bearing each possible deoxy-alpha-mannose enantiomer allowed us to assign the absolute stereochemistry of the sugar in the natural product and also to show that while glycosylation does not alter antibacterial activity, it does appear to improve solubility. Crystallographic structural studies of a lipoglycopeptide arylomycin bound to its signal peptidase target reveal the molecular interactions that underlie inhibition and also that the mannose is directed away from the binding site into solvent which suggests that other modifications may be made at the same position to further increase solubility and thus reduce protein binding and possibly optimize the pharmacokinetics of the scaffold.

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Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

Extracurricular laboratory:new discovery of [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium(II)

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Electric Literature of 72287-26-4, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.72287-26-4, Name is [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium(II), molecular formula is C34H28Cl2FeP2Pd. In a Article£¬once mentioned of 72287-26-4

Palladium-catalyzed carbonylative synthesis of N-cyanobenzamides from aryl iodides/bromides and cyanamide

A novel and convenient protocol for the synthesis of N-cyanobenzamides starting from readily available aryl halides and cyanamide via palladium-catalyzed aminocarbonylation has been developed. The protocol utilizes Mo(CO)6 as the CO source or CO(gas) and affords the desired N-cyanobenzamides in moderate to good yields.

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Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Desulfonylative carbonylation of arylsulfonyl chlorides catalyzed by palladium complexes

Palladium complex-catalyzed carbonylation of arylsulfonyl chlorides in the presence of metal alkoxides M(OR)n (M = B, Al, and Ti) gives the corresponding esters along with diaryl disulfides. With metal carboxylates M(OCOR)n (M = Na, K, Ca, Mg, and Zn), the free acids are also obtained. Among the complexes tested as catalyst precursors, PdCl2(PPh3)2 and Pd(PPh3)4 showed good catalytic activity. The reaction could be also completed with Pd(PPh3)4 (0.02 mmol) and Ti(O-i-Pr)4 (2 mmol) at 160 C. However, decreasing the reaction temperature significantly reduced the product yield. While various solvents could be used, except N,N-dimethylformamide (DMF), acetonitrile appeared to be one of the most suitable solvents.

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Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

Top Picks: new discover of Bis(di-tert-butyl(4-dimethylaminophenyl)phosphine)dichloropalladium(II)

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Process for producing fluorine-containing biaryl compound

The present invention relates to a process comprising: reacting an aromatic boronic acid compound comprising a fluorine atom at the ortho position or a cyclic trimer thereof with an aromatic chloride represented by a specific formula in a water-containing solvent under heating, in the presence of a palladium catalyst and a tertiary amine compound; this process allows a fluorine-containing biaryl compound to be obtained in a high reaction yield.

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Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

Archives for Chemistry Experiments of [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium(II)

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Safety of [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium(II), At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 72287-26-4, name is [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium(II). In an article£¬Which mentioned a new discovery about 72287-26-4

Synthesis, structural characterization, and catalytic evaluation of palladium complexes with homologous ferrocene-based pyridylphosphine ligands

A ferrocene-based phosphinopyridine, Ph2PfcPy (1; fc = ferrocene-1,1′-diyl, Py = 2-pyridyl), was newly synthesized by Negishi coupling of Ph2PfcZnCl with PyBr. Its homologous compound Ph2PfcCH 2Py (2) was obtained by reductive dehydroxylation of Ph 2PfcCH(OH)Py (4), the latter resulting via reaction of in situ generated Ph2PfcLi with PyCHO. Depending on the stoichiometry, compounds 1 and 2 react with [PdCl2(cod)] (cod = eta2:eta2- cycloocta-1,5-diene) to give P,N-chelate and bis-phosphine complexes, [PdCl 2(L-?2P,N)] (5, L = 1;6, L = 2) and [PdCl 2(L-?P)2] (7, L = 1;8, L = 2), respectively. Analogously, [(LNC)PdCl]2 or [(LNC)Pd(MeCN) 2]ClO4 (LNC = [(2-dimethylamino-?N)methyl] phenyl-?C1) react with 1 and 2 to afford complexes featuring these compounds as P-monodentate ligands ([(LNC)PdCl(L-?P)]: 9, L = 1;10, L = 2) or P,N-chelating donors ([(LNC)Pd(L-?2P,N)]ClO 4: 11, L = 1;12, L = 2), respectively. With the exception of compound 9, which undergoes self-ionization in solution, all complexes are defined air-stable solids and were characterized by elemental analysis and conventional spectroscopic methods (multinuclear NMR, IR, and MS). The crystal structures of 4, 5, 7 3 CH2Cl2, 8, 11, and 12 were determined by X-ray crystallography, revealing structural differences resulting from a more flexible geometry of the methylene-spaced ligand 2. The catalytic potential of the Pd complexes 5 and 6 and their in situ generated counterparts (Pd(OAc) 2/L, L = 1, 2) was studied in Suzuki-Miyaura cross-coupling of 4-bromotoluene (13) with phenylboronic acid and in cyanation of the same substrate with K4[Fe-(CN)6]. The results were compared with those obtained under identical conditions with analogous catalysts based on the related donor-symmetric ligand 1,1′-bis(diphenylphosphino)ferrocene.

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Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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A concise asymmetric total synthesis of aspidophytine

An expedient asymmetric total synthesis of aspidophytine is reported. A highly convergent strategy involving the sequential annulation of vinyl iodide 5 with indole 6 exploits varying modes of indole reactivity to provide aspidophytine in 23% over six steps from 5. Copyright

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Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method