Process of making isoprenoid phosphinylformic acid squalene synt

Details Process of making isoprenoid phosphinylformic acid squalene synt Process of making isoprenoid phosphinylformic acid squalene synt

1991-12-20

1992-11-24

Lee, Mary C.

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

Organic compounds

Phosphorus esters

558137, 558181, C07F 930, C07F 932

Patent

active

051663864

ABSTRACT:
Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents, are provided which have the structure ##STR1## wherein R.sup.2 is a metal ion, lower alkyl or H;

REFERENCES:
patent: 3943201 (1976-03-01), McIntosh
patent: 4018854 (1977-04-01), McIntosh
patent: 4386081 (1983-05-01), Helgstrand et al.
Issleib, K. et al., Synth. React. Inorg. Met.-Org. Chem. 1986, 16(9), 1253-; Chem. Abstr. 1988, 108, 37928h.
Kosolapoff, G. M. et al., Organic Phosphorus Compounds; vol. 4; Wiley-Interscience: New York, 1972; pp. 266-267.
Poulter, C. D., et al.,Biosynthesis of Isoprenoid Compounds, "Conversion of Farnesyl Pyrophosphate to Squalene", vol. 1, Chapter 8, pp. 413-441, J. Wiley and Sons, 1981.
Faust, J. R., et al., Proc. Nat. Acad. Sci., USA, "Squalene synthetase activity in human fibroblasts: Regulation via the low density lipoprotein receptor", 1979, 76, 5018-5022.
de Montellano, P. Ortiz, et al., J. Med. Chem., "Inhibition of Squalene Synthetase by Farnesyl Pyrophosphate Analogues", 1977, 20, 243-249.
Corey and Volante, J. Am. Chem. Soc., "Application of Unreactive Analogs of Terpenoid Pyrophosphates to Studies of Multistep Biosynthesis, Demonstration that `Presqualene Pyrophosphate`, is an Essential Intermediate on the Path to Squalene", 1976, 98, 1291-3.
Sandifer, R. M. et al., J. Am. Chem. Soc., 1982, 104, 7376-8, "Squalene Synthetase, Inhibition, by an Ammonium Analogue of a Carbocationic Intermediate in the Conversion of Presqualene Pyrophosphate to Squalene".
Bertolino, A., et al., Biochim. Biophys. Acta., 1978, 530, 17-23, "Polyisoprenoid Amphiphilic Compounds as Inhibitors of Squalene Synthesis and Other Microsomal Enzymes".
Davisson, F. J., et al., J. Org. Chem., 1986, 51, 4766-4779, "Phosphorylation of Isoprenoid Alcohols".
Stremler, K. E. et al., J.A.C.S., 1987, 109, 5542, "Methane and Difluoromethanediphosphonate Analogues of Geranyl Diphosphate: Hydrolysis-Inert Alternate Substrates".
McClard, R. W., et al., J. Am. Chem. Soc., 1987, 109, 5544-5545, "Novel Phosphonylphosphinyl (P-C-P-C) Analogues of Biochemically Interesting Diphosphates, Syntheses and Properties of P-C-P-C Analogues of Isopentenyl Diphosphate and Dimethylallyl Diphosphate".
Capson, T. L., PhD dissertation, Jun. 1987, Dept. of Medicinal Chemistry, the University of Utah, Abstract, Table of Contents, pp. 16, 17, 40-43, 48-51, Summary.
Biller, S. A., et al., J. Med. Chem., 1988, 31, 1869 "Isoprenoid(Phosphinylmethyl)phosphonates as Inhibitors of Squalene Synthetase".
Merck Index, Tenth Edition, p. 607, paragraph 4135, (1983).
Kosolapoff, G. M., "Organophosphorus Compounds", John Wiley and Sons, 1950, pp.146-147.

Affiliated with

Also associated with

Rating

Process of making isoprenoid phosphinylformic acid squalene synt does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Process of making isoprenoid phosphinylformic acid squalene synt, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Process of making isoprenoid phosphinylformic acid squalene synt will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-923050