公开(公告)号：US06806395B2

公开(公告)日：2004-10-19

申请号：US10380169

申请日：2003-03-18

申请人： Kimiyuki Shibuya ,  Tadaaki Ohgiya ,  Toru Miura ,  Kazuhiro Onogi

发明人： Kimiyuki Shibuya ,  Tadaaki Ohgiya ,  Toru Miura ,  Kazuhiro Onogi

IPC分类号： C07C3906

CPC分类号： C07C41/30 ,  C07C37/002 ,  C07C37/11 ,  C07C37/50 ,  C07C39/11 ,  C07C43/23 ,  Y02P20/55 ,  C07C39/06

摘要： A process for producing a 3,5-bisalkylphenol (2) according to the following reaction scheme: (wherein R1 represents a hydrogen atom, an alkali metal atom, an alkaline earth metal atom, or a hydroxyl-protecting group (other than methyl group); R2 represents a C1 to C5 lower alkyl group or an optionally substituted phenyl group; and each of R3 and R4, which may be identical to or different from each other, represents a lower alkyl group, an aralkyl group, or an aryl group); a carbinol compound (1); and a process for producing the carbinol compound. The production process of the present invention enables efficient and safe production of a variety of 3,5-bisalkylphenols including 3,5-diisopropylphenol, which are important as synthesis intermediates for drugs and agricultural chemicals, in shorter steps at high purity in high yield, thus contributing to consistent supply of drugs and agricultural chemicals.

摘要翻译： 根据以下反应方案制备3,5-双烷基苯酚（2）的方法：其中R 1表示氢原子，碱金属原子，碱土金属原子或羟基保护基（其他 比甲基）; R 2表示C1〜C5低级烷基或任选取代的苯基; R 3和R 4可以彼此相同或不同，表示 低级烷基，芳烷基或芳基）。 甲醇化合物（1）; 和甲醇化合物的制造方法。 本发明的制造方法能够高效安全地生产各种3,5-二异丙基苯酚，其中3,5-二异丙基苯酚作为药物和农用化学品的合成中间体是重要的，在高纯度，高收率的较短步骤中， 从而有助于持续供应毒品和农药。

公开(公告)号：US06204278B1

公开(公告)日：2001-03-20

申请号：US08858244

申请日：1997-05-19

申请人： Kimiyuki Shibuya ,  Katsumi Kawamine ,  Yukihiro Sato ,  Toshiyuki Edano ,  Souhei Tanabe ,  Masami Shiratsuchi

发明人： Kimiyuki Shibuya ,  Katsumi Kawamine ,  Yukihiro Sato ,  Toshiyuki Edano ,  Souhei Tanabe ,  Masami Shiratsuchi

IPC分类号： A61K31423

CPC分类号： C07D263/58 ,  C07D235/28 ,  C07D277/70

摘要： The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: where Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NH6—; R6 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.

摘要翻译： 本发明提供了新的酰苯胺化合物和包含它们的药物组合物。本发明涉及下式的化合物：其中Ar是任选取代的芳基; R 4和R 5相同或不同，并且各自是氢原子，低级烷基 ，或低级烷氧基; 并且R 4和R 5可以一起形成其中一个或多个亚甲基部分可以任选地被氧和/或硫原子取代的低级亚烷基; X是-NH-或氧或硫原子; Y是-NH-，氧 或硫原子，或亚砜或砜基; Z为单键或-NH6-; R6表示氢原子或低级亚烷基; 和n为0至15的整数;以及它们的盐和溶剂化物。本发明的化合物可用作药物组合物，特别是作为酰基辅酶A胆固醇酰基转移酶（ACAT）抑制剂。