24424-99-5Relevant articles and documents
Modeling and spectroscopic studies of synthetic diazabicyclo analogs of the HIV-1 inhibitor BMS-378806 and evaluation of their antiviral activity
Legnani, Laura,Colombo, Diego,Cocchi, Elena,Solano, Lucrezia,Villa, Stefania,Lopalco, Lucia,Asti, Valeria,Diomede, Lorenzo,Marinone Albini, Franca,Toma, Lucio
, p. 287 - 294 (2011)
Three diazabicyclo analogs of BMS-378806, in which theaxial methyl group present on its piperazine ring is replaced by a carbon bridge, were synthesized and tested, through a viral neutralization assay, on a panel of six pseudoviruses. The diazabicyclooctane and-nonane derivatives maintained a significant infectivity reduction power, whereas the diazabicycloheptane derivative was much less effective. A modeling study allowed to relate the antiviral activity to the conformational preferences of the compounds. Moreover, similarly to BMS-378806, theoretical calculations predict the existence of different conformational families corresponding to the possible arrangements at the two planar amido functions of the compounds. High-field 1H NMR spectra confirm these results, as they show two distinct series of signals. A viral neutralization assay on a panel of six HIV-related pseudoviruses allowed the determination of the antiviral activity of three diazabicyclo analogs of BMS-378806, in which the axial methyl group on its piperazine ring is replaced by a carbon bridge. The diazabicyclooctane and-nonane derivatives show a significant infectivity reduction power that is related to their conformational preference. Copyright
Method for synthesizing di-tert-butyl dicarbonate ester by adopting phase transfer catalytic method
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Paragraph 0018-0041, (2018/12/02)
The invention discloses a method for synthesizing di-tert-butyl dicarbonate ester by adopting a phase transfer catalytic method, and belongs to the technical field of organic synthesis process. Di-tert-butyl decarbonate ester is synthesized from raw materials such as triphosgene and tert-butyl alcohol under the condition of adding alkali and a phase transfer catalyst, phosgene is prevented from being used as a raw material, the reaction condition is moderate, and meanwhile, the reaction time is greatly shortened, and the method has a great application value.
Preparation method of di-tert-butyl dicarbonate
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Paragraph 0025, (2017/07/19)
The invention relates to a preparation method of di-tert-butyl dicarbonate and belongs to the technical field of synthesis of pharmaceutical intermediates. The preparation method comprises the following steps: adding metal sodium into xylol; heating to obtain sodium sand; then dropwise adding tert-butyl alcohol and carrying out pumping filtration to obtain sodium tert-butoxide; dissolving the sodium tert-butoxide into petroleum ether; introducing carbon dioxide and reacting to obtain a monoester sodium salt solution; adding a catalyst and slowly dropwise adding diphosgene to react; after reacting, standing and carrying out the pumping filtration; and washing with water, drying, distilling, cooling and crystallizing to obtain the di-tert-butyl dicarbonate. According to the preparation method, the sodium tert-butoxide is prepared from the metal sodium and the di-tert-butyl dicarbonate is prepared from the sodium tert-butoxide; a pumping filtration method is used for replacing a previous distillation method, so that the process is simpler and more energy is saved; the petroleum ether is used for replacing n-hexane and toluene, so that the production cost is reduced and a product is easier to purify; and finally, after the reaction, the pumping filtration is carried out and then water washing is carried out, so that the amount of wastewater is reduced and the environment-friendly treatment cost is reduced.
Production technology of tert-butyl pyrocarbonate
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Paragraph 0002; 0003, (2017/07/12)
Tert-butyl pyrocarbonate is an important chemical engineering raw material. A production technology of the tert-butyl pyrocarbonate comprises the following steps: adding metered 98% sodium tert-butoxide and 99% 6# solvent oil to a reaction kettle, stirring and dissolving the 98% sodium tert-butoxide, controlling the temperature of the reaction kettle to be 5 DEG C, slowly introducing a proper amount of 99.99% carbon dioxide to increase the fluidity of a solution in the reaction kettle and reduce the density of the solution, slowing the stirring speed and accelerating the CO2 introduction speed until the solution does not absorb CO2, and carrying out a reaction for about 12 h to obtain sodium tert-butylcarbonate; controlling the temperature in the reaction kettle to be less than 5 DEG C after the reaction ends, slowly adding 99% trichloromethyl carbonate at a slow initial dropwise adding speed, controlling the temperature of the solution to be 0-5 DEG C, allowing the solution to be become thin and then become white, and dropwise adding all the 99% trichloromethyl carbonate in about 2 h; allowing a large amount of bubbles to be generated in the solution, and continuously keeping the temperature in a range of 0-5 DEG C for 1 h to generate bubbles (large CO2 release amount); heating the solution to 30 DEG C after low-temperature keeping ends, and continuously keeping the temperature for 3 h until no bubbles are generated and the reaction ends; and filtering a product obtained after a metathesis reaction ends, collecting the filtered product for external retail comprehensive utilization in order to obtain crude tert-butyl pyrocarbonate.
NOVEL THIOPHENE DERIVATIVES AS SPHINGOSINE-1-PHOSPHATE-1 RECEPTOR AGONISTS
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, (2011/10/01)
The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
VLA-4 INHIBITOR
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, (2008/06/13)
An object of the present invention is to provide a compound which selectively inhibits binding of a ligand and ±421 integrin (VLA-4), a process for producing the compound, and a medicament containing the compound. A compound represented by the formula (I) etc. orasaltthereof, a process for producing the compound or a salt thereof, a medicament containing the compound or a salt thereof, as well as a preventive and/or a therapeutic agent for a disease caused by cell adhesion, for example, inflammatory reaction, autoimmune disease, cancer metastasis, bronchial asthma, nasal obstruction, diabetes, arthritis, psoriasis, multiple sclerosis, inflammatory bowel disease and rejection reaction at transplantation, containing the compound or a salt thereof as a primary component. [wherein Y 1 represents a divalent aryl group etc. , V 1 represents an aryl group etc., and R 11 to R 14 represent H, OH or a halogen atom etc.]
BICYCLIC PYRROLE DERIVATIVES
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, (2008/06/13)
Compounds represented by the general formula (I), prodrugs thereof, or pharmaceutically acceptable salts of both are provided as compounds which have high DPP-IV inhibiting activity and are improved in safety, toxicity and so on: (I) wherein the solid line and dotted line between A1 and A2 represents a double bond (A1=A2) or the like; A1 is C(R4) or the like; A2 is nitrogen atom or the like; R1 is hydrogen atom, optionally substituted alkly group, or the like; R2 is hydrogen atom, optionally substituted alkyl group, or the like; R3 is hydrogen atom, halogen atom, or the like; R4 is hydrogen atom, hydroxyl, halogen atom, or the like; and Y is a group represented by the general formula (A) or the like; (A) [wherein m1 is 0, 1, 2 or 3; and the group (A) may be freed from R6 or substituted with one or two R6's which are each independently halogen atom or the like.]
Substituted γ-phenyl-Δ-lactams and uses related thereto
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, (2008/06/13)
γ-Phenyl-substituted Δ-lactams are disclosed. They may be formulated into pharmaceutical compositions, and/or used in the treatment or prevention of inflammation or other conditions or disease states.
Novel heterocyclic compounds, their preparation and their use as medicaments, in particular as antibacterials and beta-lactamase inhibitors
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, (2008/06/13)
The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a method for preparing these compounds, and to their use as medicaments, in particular as antibacterials and β-lactamase inhibitors.
β-lactam compounds and process for producing the same
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, (2008/06/13)
Novel β-lactam compound of the formula [1]: wherein R1is lower alkyl or hydroxy-substituted lower alkyl, R2is H or lower alkyl, X is O or, S, R3is H, metal or protecting group, W is a 6- or 7-membered nitrogen-containing heterocycle optionally being substituted at carbon atoms. Said β-lactam compound shows excellent antibacterial activity against Gram-positive bacteria, particularly against methicillin-resistantStaphylococcus aureusand methicillin-resistant and coagulase-negativeStaphylococcus aureus.
