Process for preparation of benzo[B]thiophene glucuronides

Details Process for preparation of benzo[B]thiophene glucuronides Process for preparation of benzo[B]thiophene glucuronides

1995-03-31

1996-10-08

Rollins, John W.

Chemistry: molecular biology and microbiology

Micro-organism, tissue cell culture or enzyme using process...

Preparing compound containing at least three carbocyclic rings

4352521, 4352535, 4352536, C12N 112, C12N 120, C12P 1500

Patent

active

055630545

ABSTRACT:
The present invention provides a biotransformation process for preparing a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or a .beta.-glucuronide group of the formula ##STR2## provided at least one of R.sub.1 and R.sub.2 is a .beta.-glucuronide group.

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patent: 5217882 (1993-06-01), Chen
T. S. Chen et al., "Microbial Hydroxylation and Glucuronidation of the Angiotensin II (AII) Receptor Antagonist MK 954", J. Antibiot., 46(1), 131-134 (1993).
C. A. Frolik et al., "In Vivo and In Vitro Metabolism of Raloxifene", Am. Soc. Bone and Mineral Res., Tampa, FL, Sep. 18-22, 1993.
T. B. Lindstrom et al., "Disposition and Metabolism of New Benzthiophene Anteistrogen in Rats, Dogs, Monkeys", Xenobiotica, 14(11), 841-847 (1984).
L. J. Black et al., "The Relationship of the Antiestrogenic Efficacy of LY156758 to its Pharmacokinetics and Metabolism Following Oral Administration to Adult Ovariectomized Rats", 7th Int'l Congress of Endocrin., Quebec City, Canada, Jul. 1-7, 1984.

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