Methods of preparing .alpha.-phosphonosulfinate squalene synthet

Details Methods of preparing .alpha.-phosphonosulfinate squalene synthet Methods of preparing .alpha.-phosphonosulfinate squalene synthet

1995-05-22

1996-08-06

Richter, Johann

Organic compounds -- part of the class 532-570 series

Organic compounds

Phosphorus esters

558131, 558177, 562 23, C07F 938, C07F 940

Patent

active

055435424

ABSTRACT:
.alpha.-Phosphonosulfinate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is alkyl, arylalkyl or aryl; R.sup.4 is H or a pharmaceutically acceptable cation; Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; including pharmaceutically acceptable salts.

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