Eli Lilly and Company

Richard E Holmes

Louis Nickolaus Jungheim

Robert J Ternansky

Charles J Barnett

Sandra K Sigmund

Charles David Jones

Thomas Edward Mabry

Ta-Sen Chou

Wayne A Spitzer

Larry W Hertel

Chafiq Hamdouchi

Cora Sue Grossman

Joseph Michael Gruber

Jesus Ezquerra-Carrera

Glen P Jourdan

Anti-viral compounds

A stereoselective anion glycosylation process for preparing beta- and alpha-anomer enriched 2', 2'-difluoro-2'-deoxynucleosides and 2'-deoxy-2'-fluoronucleosides by reacting an alpha- or beta-anomer enriched 2-deoxy-2-fluorocarbohydrate or 2-deoxy-2,2-difluorocarbohydrate with at least a molar equivalent of a salt of a nucleobase derivative in an inert solvent.

Stereoselective anion glycosylation process for preparing

7-Substituted bicyclic pyrazolidinone compounds as antimicrobials and the corresponding intermediates, are discussed or provided. The use of the antimicrobial compounds in pharmaceutical compositions and in methods for treating bacterial infections is set forth.

7-substituted bicyclic pyrazolidinones

7-substituted bicyclic pyrazolidinones, pharmaceutical compositions and

4-Substituted 1-(optionally substituted)diazolidinones are intermediates to 7-substituted bicyclic pyrazolidinone antimicrobials.

Substituted diazolidinones

4-(Protected amino)-3-oxo-1-(substituted and unsubstituted methylene)-1,2-pyrazolidinium ylides are intermediates to 7-substituted bicyclic pyrazolidione antimicrobials.

Pyrazolidinium ylides

1-(Alkylated)-2-(acylated)diazolidinones are intermediates to bicyclic pyrazolidinone antimicrobial compounds. The instant compounds have the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as defined in the specification.

1-(alkylated)-2-(acylated)diazolidinones

1-Alkylated diazolidinones are intermediates to bicyclic pyrazolidinone antimicrobial compounds. The instant compounds have the formula ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3, have the meanings as defined in the specification.

1-alkylated diazolidinones

Substituted pyrroloquinoxalinones and diones, useful as anti-inflammatory and anti-thrombotic agents.

Substituted pyrroloquinoxalinones and diones used in treating

7-Amino and 7-alkanoylamino-2-oxo-3-phenylindolines, useful as anti-inflammatory and anti-thrombotic agents.

7-Amino and 7-alkanoylamino 2-oxo-3-phenylindolines

Substituted pyrroloquinoxalinones and diones

Thio-substituted 2-oxoindolines have the formula ##SPC1## In which one of R or R.sub.1 is hydrogen and the other is R.sub.2 --S--, in which R.sub.2 is C.sub.1 -C.sub.3 alkyl, benzyl, halobenzyl, nitrobenzyl, C.sub.1 -C.sub.3 alkylbenzyl, or phenyl. These compounds are active in relieving a condition associated with anxiety, tension, or like emotional disturbances.

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Indianapolis, IN, United States of America

Richard E Holmes