QUINUCLIDINE DERIVATIVE HAVING SQUALENE SYNTHASE INHIBITORY ACTION

    公开(公告)号:JPH08269056A

    公开(公告)日:1996-10-15

    申请号:JP10893495

    申请日:1995-03-29

    Abstract: PURPOSE: To obtain a new quinuclidine derivative suppressing the biosynthesis of cholesterol by inhibiting squalene formation. CONSTITUTION: This derivative (salt) is shown by formula I [R1 is a (substituted) phenyl or a (substituted) pyridyl; R2 is a 5-9C alkylene, a 5-9C alkenylene or a 5-9C alkynylene; R3 to R5 are: (R3 , R4 , R5 )=(O, H, H), (O-CH2 , H, H) or R4 and R5 are bonded to form a double bond] such as 3- 5-[4-(3-methylphenoxy) phenyl]-2-pentenyloxy}-1-azabicyclo[2,2,2]octane. The derivative, for example, is obtained by reacting a compound of the formula R1 -R2 -X (X is a halogen, an alkylsulfonic acid ester, etc.) with a compound of formula II in an inert solvent in the presence of a base at 0-100 deg.C (preferably 0-25 deg.C) for 1-48 hours (preferably 12-24 hours) to give a compound of formula III and removing the amino-protecting group, borane.

    4,6-DI-TERT-BUTYL-2,3-DIHYDROBENZOTHIOPHENE DERIVATIVE

    公开(公告)号:JPH07330759A

    公开(公告)日:1995-12-19

    申请号:JP12033795

    申请日:1995-04-10

    Abstract: PURPOSE:To obtain the subject new compound excellent in antioxidation effect and lipid peroxidation inhibitory effect and useful as a therapeutic agent for ischemic organopathy such as arterial sclerosis or cardiac infarction. CONSTITUTION:A compound of formula I [R1 is H, a lower alkyl or an acyl; R2 and R3 are each H, a (substituted) alkyl or a (substituted) alkenyl; R4 is R3, etc.; (n) is 0 to 2] and its salts, e.g. 4,6-ditert-butyl-5-hydroxy-2, 2-dipentyl-2, 3-dihydrobenzothiophene. The compound of formula I is synthesized by converting a compound of formula II as the starting substance into a compound of formula III (R6 and R7 are each a lower alkyl; R8 is R4; R9 is R3), reacting the resultant compound in the presence of a Lewis acid such as boron trifluoride etherate in a solvent such as chloroform at room temperatures to synthesize a compound of formula IV and deprotecting it.

    2,3-DIHYDROBENZOFURAN DERIVATIVE
    3.
    发明专利

    公开(公告)号:JPH1135568A

    公开(公告)日:1999-02-09

    申请号:JP14085598

    申请日:1998-05-22

    Abstract: PROBLEM TO BE SOLVED: To obtain the subject novel compound that manifests strong cell- protecting action against the cytotoxicity caused by oxidized LDL in the kidney- originating cells and is useful for treatment or prevention of chronic renal failure and diabetic nephropathy and as an internal organ preservative. SOLUTION: This compound is represented by the formula (R1 is H, an acyl which may be substituted; R2 -R4 are each H, a lower alkyl, a lower alkenyl where both of them are not t-butyl, simultaneously; R and R are each H, an alkyl which may be substituted), typically 4,7-di -t-butyl-5 -hydroxy-2, 3- dihydrobenzofuran. This compound is prepared by adding dropwise methanesulfonic acid to a solution of 4-t -butyl-5 -hydroxy-2, 3-dihydrobenzofuran in a mixture of t-butyl alcohol with chloroform followed by extraction, washing and concentration of the product.

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