18217-00-0Relevant articles and documents
Organocatalytic Chlorination of Alcohols by P(III)/P(V) Redox Cycling
Longwitz, Lars,Jopp, Stefan,Werner, Thomas
, p. 7863 - 7870 (2019/06/27)
A catalytic system for the chlorination of alcohols under Appel conditions was developed. Benzotrichloride is used as a cheap and readily available chlorinating agent in combination with trioctylphosphane as the catalyst and phenylsilane as the terminal reductant. The reaction has several advantages over other variants of the Appel reaction, e.g., no additional solvent is required and the phosphane reagent is used only in catalytic amounts. In total, 27 different primary, secondary, and tertiary alkyl chlorides were synthesized in yields up to 95%. Under optimized conditions, it was also possible to convert epoxides and an oxetane to the dichlorinated products.
Preparation method of chloroethyl-substituted aromatic compound
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Paragraph 0187; 0189; 0191, (2019/02/06)
The invention belongs to the technical field of preparation of organic chloride products and particularly relates to a preparation method of a beta-chloroethyl-substituted aromatic compound. The method comprises the following steps: by taking 1-bromine-2-chloroethane and arylboronic acid as raw materials in the atmosphere of a reaction solution and nitrogen gas, heating under the action of a catalytic system with a nickel catalyst and a dipyridyl ligand, and weak base additives and pyridine additives, separating and purifying after reaching a reaction endpoint to obtain the beta-chloroethyl-substituted aromatic compound. According to the preparation method, the nickel catalyst and the dipyridyl ligand which are cheap and easily available are commercially available are used as the catalyticsystem; the directional introduction from beta-chloroethyl to aromatic group is achieved, so that the beta-chloroethyl-substituted aromatic compound can be efficiently prepared. The method is mild inreaction condition and low in raw material cost; the reaction steps are simple and are easy to operate; meanwhile, the reaction scale is easy to enlarge; the product is simple and convenient to separate; the method is suitable for industrial production.
OXADIAZOLONES AS TRANSIENT RECEPTOR POTENTIAL CHANNEL INHIBITORS
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Paragraph 0255-0258, (2018/06/12)
The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.