- Chloromethyl chlorosulfate: A new, catalytic method of preparation and reactions with some nucleophiles
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A catalytic method of preparing chloromethyl chlorosulfate (CMCS) was described. The reaction of liquid SO3 with CH2Cl 2 at room temperature led to SO3 insertion into the C-Cl bonds, giving CMCS. The product mixtures consists entirely of CMCS and the product of further sulfation, methylene bis(chlorosulfate) (MBCS). The reaction was shown to be first order in the catalyst and third order in SO3 by measuring initial rates of CMCS formation or total CH2Cl2 consumption. The results show that the reaction between dichloromethane and SO3 at room temperature is accelerated by very low concentrations.
- Power, Nicholas P.,Bethell, Donald,Proctor, Lee,Latham, Elliot,Dawson, Paul
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- Development of a process for the preparation of chloromethyl chlorosulfate
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A new and efficient synthesis of chloromethyl chlorosulfate (CMCS) from chloroiodomethane and chlorosulfonic acid is described. This process leverages a chlorosulfonic acid-mediated iodide oxidation to drive the equilibrating displacement process to full conversion. The resulting iodine byproduct is further oxidized and removed as iodate, to prevent iodide-induced decomposition of CMCS. This new process provides an efficient and scalable protocol for the preparation of CMCS in 92% solution yield and high purity (>99 GC area %).
- Zheng, Bin,Sugiyama, Masano,Eastgate, Martin D.,Fritz, Alan,Murugesan, Saravanababu,Conlon, David A.
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- Method for the Recycling or Disposal of Halocarbons
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The present invention relates to a method for recycling and/or disposal of halocarbons, particularly fluorinated alkanes, such as trifluoromethane, by reacting said halocarbons with sulfur trioxide, particularly to form halide sulfonic acids and sulfur dioxide.
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- Preparation method of methyl bichlorosulfonate
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The invention discloses a preparation method of methyl bichlorosulfonate. The methyl bichlorosulfonate is prepared through the catalytic addition reaction of fuming sulphuric acid and dichloromethaneunder the condition that boron tribromide is taken as a catalyst. Compared with the prior art, the preparation method of the methyl bichlorosulfonate has the following advantages: (1) the novel catalyst of boron tribromide is cheap and easy to get, and the production cost is lowered; (2) due to the optimized catalyst and reaction condition, the MBCS (Methyl Bichlorosulfonate) yield is increased, and a byproduct CMCS is also reduced; (3) the use of the hazardous difficult-to-treat material sulfur trioxide is avoided, the operability is strong, and the industrial value is high; and (4) the problem of difficulties in storing and fusing the liquid sulfur trioxide in use is avoided.
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Paragraph 0011; 0024-0039
(2018/05/16)
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- COMPOSITION CONTAINING CHLOROMETHYL PHOSPHATE DERIVATIVE WITH IMPROVED STABILITY AND METHOD FOR PRODUCING THE SAME
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The present invention provides a process or the like which is employed for producing chloromethyl phosphate derivatives that are useful for producing water-soluble prodrugs, and which are excellent from the points of view of workability, operativity and energy saving. According to the present invention, there is provided a process for producing a composition containing a compound represented by the following formula (I) and a tertiary amine, (wherein R1 and R2 are identical or different from each other, and represent a C1-C6 alkyl group, a C2-C6 alkenyl group or a C6-C14 aryl C1-C6 alkyl group which may have a substituent, and R1 and R2 may together form a ring), the proces comprising the step of adding the tertiary amine having a boiling point at 1 atmosphere of 150°C or higher to the compound represented by formula (I).
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Page/Page column 11
(2009/12/27)
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- DC107 derivatives
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DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided: wherein R1 represents CO(CR4AR4B)n1(O(CH2)p1)n2OR5 {wherein n1 represents an integer of 1 or 2; R4A and R4B are the same or different, and each represents hydrogen or lower alkyl; p1 and n2 each represents an integer of 1 to 10; and R5 represents hydrogen, lower alkyl, or the like), or
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- DC107 derivatives
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DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided: STR1 wherein R1 represents hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR4, or the like; R2 represents hydrogen or COR6 ; R3 represents --CH2 OCOR7, phthalimidomethyl, or the like; and W represents oxygen or NR8 (wherein R8 represents hydroxy, lower alkoxy, lower alkenyloxy, aralkyloxy, substituted or unsubstituted arylsulfonylamino, or lower alkoxycarbonylamino).
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- Synthese et activite biologique de prodrogues de l'acide oxolinique
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Synthesis and biological activities of oxolinic acid pro-drugs.Antiseptic phenols, anti-inflammatory acids and polyethyleneglycol moieties have been attached by labile bonds to oxolinic acid giving pro-drugs with anti-bacterial activities.Some of them are more soluble in water, exhibit a more sustained action in the time and give higher plasma and tissue concentrations compared with the free drug.
- Loubinoux, B,Colin, JL,Thomas, V
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p. 461 - 467
(2007/10/02)
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