90924-07-5Relevant articles and documents
Method for preparing indole-2,3-dione derivatives by catalytic oxidation of microwave copper/peroxyacetic acid
-
Paragraph 0024; 0055, (2018/09/08)
The invention discloses a method for preparing indole-2,3-dione derivatives by catalytic oxidation of microwave copper/peroxyacetic acid. The method comprises the following steps: a catalytic amount of catalyst copper iodide, indole, a derivative of the indole and peroxyacetic acid are added into a reaction vessel, wherein the indole, the derivative of the indole and the peroxyacetic acid are usedas raw materials, ethanol is used as a solvent, the reaction vessel is placed into a microwave reaction instrument, a reaction is performed at certain temperature and power, after a certain time, reduced-pressure concentration is performed, and a product is purified by column chromatography. The method provided by the invention is a method having novel raw materials, simple operation and high efficiency used for preparing a benzimidazole derivative; and compared with the prior art, the method provided by the invention has an obviously-accelerated reaction speed than that under conventional heating, mild reaction conditions, simple operation, a high yield, safety, low costs and environmental protection.
HUMAN LEUKOCYTE ELASTASE (HLE) INHIBITORS, AND RELATED PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE
-
, (2008/06/13)
Novel therapeutic agents useful as inhibitors of HLE are provided. The compounds have the structural formula (I) STR1 wherein R 1 through R 9, m, n and p are as defined herein. Methods of using the compounds of formula (I) to inhibit serine proteases and
2-OXY-4H-3,1-BENZOXAZIN-4-ONES AND PHARMACEUTICAL USE
-
, (2008/06/13)
2-Oxy-4H-3,1-benzoxazin-4-ones represented by the formula: STR1 and the pharmaceutically acceptable acid addition salts thereof, wherein: a is an integer of 0-4;A is a bond, or alkylene having one to eight carbon atoms;R is hydrogen, phenyl, imidazolyl or cycloalkyl having three to six carbon atoms, wherein the phenyl, imidazolyl or cycloalkyl ring is optionally substituted with 1-3 substituents independently selected from the group consisting of lower alkyl having one to four carbon atoms, lower alkoxy having one to four carbon atoms,--N(R 1) 2,--NO 2, halo or lower alkylthio having one to four carbon atoms, and, each R' is independently selected from the group consisting of lower alkyl having one to six atoms, lower alkenyl having two to six carbon atoms, lower alkoxy having one to six carbon atoms, lower alkylthio or halo-lower alkyl having one to four carbon atoms, halo,--NO 2,--N(R 1) 2, STR2--NR 1 COR 2, and STR3 in which each R 1 is independently hydrogen or lower alkyl having one to four carbon atoms, or together form a piperidine or a piperazine ring optionally substituted at the ring nitrogen by lower alkyl having one to four carbon atoms or--CH 2 CH 2 OH, each R 2 is independently lower alkyl having one to four carbon atoms, A is an alkylene group if R is hydrogen, and the pharmaceutically acceptable acid addition salts thereof are useful as serine protease inhibitors in humans and animals.