公开(公告)号：US09018418B2

公开(公告)日：2015-04-28

申请号：US14003200

申请日：2012-01-17

Applicant: Che Jim Cheng ,  Fei Song ,  Yongmei Pan

Inventor： Che Jim Cheng ,  Fei Song ,  Yongmei Pan

IPC: C07C213/08 ,  C07C213/02 ,  C07C217/08 ,  C07C41/16

CPC classification number: C07C213/08 ,  C07C41/16 ,  C07C213/02 ,  C07C217/08 ,  C07C43/2055

Abstract: A method for preparation of an aryl poly(oxalkyl) quaternary ammonium compound is provided, said method comprising steps of: 1) reacting a phenol with a dihalopolyalkylene ether under the action of a phase transfer catalyst, to obtain an arylpoly(oxalkyl) halide; 2) reacting said arylpoly(oxalkyl) halide with an amination reagent under the action of a phase transfer catalyst, to obtain an arylpoly(oxalkyl) amine; 3) reacting said arylpoly(oxalkyl) amine with an alkylation reagent, to obtain an aryl poly(oxalkyl) quaternary ammonium compound; wherein R1 is H or a C1 to C16 alkyl group, located in the ortho, meta or para position; n is an integer of 2 to 6; R2 is H or a C1 to C16 alkyl group; R3 is H or a C1 to C16 alkyl group; R4 is a C1 to C16 alkyl group; X1 is Br or Cl; X is Cl, Br, or I. The preparation method according to the present invention requires low temperature and low pressure, the reaction time is short, and an overall yield can reach 75%. The operation is simple, the cost is low, and the product can be separated easily and have a purity of pharmaceutical grade, thereby facilitating the large-scale production.

Abstract translation: 提供了制备芳基聚（烷氧基）季铵化合物的方法，所述方法包括以下步骤：1）在相转移催化剂的作用下使苯酚与二卤代亚烷基醚反应，得到芳基聚（烷氧基）卤化物; 2）在相转移催化剂的作用下使所述芳基聚（氧烷基）卤化物与胺化试剂反应，得到芳基聚（氧烷基）胺; 3）使所述芳基聚（氧烷基）胺与烷基化试剂反应，得到芳基聚（烷氧基）季铵化合物; 其中R1是位于邻位，间位或对位的H或C1至C16烷基; n为2〜6的整数， R2是H或C1至C16烷基; R3是H或C1至C16烷基; R4是C1-C16烷基; X1是Br或Cl; X是Cl，Br或I.根据本发明的制备方法需要低温低压，反应时间短，总产率可达75％。 操作简单，成本低，产品分离容易，药品级纯度高，便于大规模生产。