Title:
METHOD FOR LACTONIZATION OF MEVINIC ACID AND ANALOGS THEREOF
Document Type and Number:
Japanese Patent JP2718422
Kind Code:
B2
Abstract:
PURPOSE: To obtain a highly pure lactonized product containing an extremely small amount of impurities with a high productivity by lactonizing mevinic acid or analogs thereof by a new method.
CONSTITUTION: A compound represented by formula I, (wherein R is a 1-10C alkyl; R1 is CH3, CH2OH, or the like; Z is H, a metal cation, or the like; and a and b are each a single bond or double bond) is treated by a strong acid catalyst (preferably trifluoroacetic acid, or the like) in a water-miscible organic solvent so as to be lactonized. Then, a targeted compound represented by formula II with a 0.2% or less dimer impurity is obtained gradually adding water until the lactone is crystallized from the reaction catalyst. The lactonization is executed preferably at 20 to 25°C. Examples of compounds represented by formula II include 6(R)-[2-[(8(S)-(2,2-dimethylbutyryloxy)-2(S), 6(S)- dimethyl-1,2,6,7,8,8a(R)-hexahydronaphthyl-1(S)]ethyl]-4-(R)-hydroxy-3,4,5,6- tetrahydro-2H-pyran-2-one.
Inventors:
Laszlore. Tray bar
Application Number:
JP28993994A
Publication Date:
February 25, 1998
Filing Date:
November 24, 1994
Export Citation:
Assignee:
Merck End-Campany Inc.
International Classes:
A61K31/34; A61K31/35; A61K31/365; A61K31/366; A61P3/06; C07B63/00; C07C69/28; C07D309/30; (IPC1-7): A61K31/365
Domestic Patent References:
| JP56138181A | ||||
| JP568689A | ||||
| JP56122375A | ||||
| JP5948418A | ||||
| JP6097973A |
Other References:
【文献】欧州特許出願公開251625(EP,A)
Attorney, Agent or Firm:
Yoshio Kawaguchi (2 outside)
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