A kind of method of Michael addition synthesis benzhydryl quinuclidone

A technology of benzhydryl quinuclidine and benzylidene quinine, applied in the field of organic synthesis, can solve the problems of environmental protection pressure, unfriendly environment, undisclosed yield and the like in enlarged production, and achieves no environmental protection pressure, Low price and good purity
CN108822101BActive Publication Date: 2021-02-05SICHUAN QINGMU PHARMA CO LTD
3 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SICHUAN QINGMU PHARMA CO LTD
Publication Date
2021-02-05

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention discloses a method for synthesizing benzhydryl quinuclidine by Michael addition, and belongs to the field of organic synthesis. In the present invention, (Z)-2-benzylidenequinine-3-ketone is used as a raw material, and 2-(diphenylmethyl)quinuclidine-3- is obtained through Mike addition reaction in the presence of a cuprous catalyst. ketone product. Under the preferred reaction conditions, the yield can reach 85%, and the purity is higher than 99%. The preparation method of benzhydryl quinuclidine of the present invention solves the problems of low yield, low selectivity, unfriendly environment and the like existing in the prior method.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention relates to a synthesis method of benzhydryl quinuclidone, wherein the Michael addition synthesis method used belongs to the technical field of organic synthesis. Background technique

[0002] The benzhydrylquinuclidinone system is named 2-(benzhydryl)quinuclidin-3-one, the English name is 2-benzhydrylquinuclidin-3-one, which is the key intermediate of the veterinary drug Maropitant, and its structural formula is as follows :

[0003]

[0004] Currently on the market, Cerenia, whose active ingredient is maropitant citrate, is an antiemetic drug for large animals produced and sold by Pfizer. Maropitant is a type 1 neurokinin (NK1) receptor anti-blocking agent, which can act on the central nervous system by inhibiting substance P (the key neurotransmitter that causes vomiting), and can inhibit peripheral and central vomiting .

[0005] The synthetic report about benzhydryl quinuclidinone has following several methods at present: [00...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More