Abbott Laboratories Corporation

Medivir Ab

Eli Lilly and Company

Mediver Ab

M Robert Leanna

Howard E Morton

Jien-Heh J Tien

Anthony Ralph Haight

Timothy L Stuk

Michael S Allen

Hing L Sham

Thomas J Sowin

Daniel S Reno

Timothy A Robbins

Michael Rasmussen

Francis A Kerdesky

David Scarpetti

Linda M Lijewski

Laura Melcher

Daniel W Norbeck

Chen Zhao

Denton C Langridge

Bradley D Gates

Daniel J Plata

Steven M Hannick

Bikshandarkoil A Narayanan

Zhenping Tian

Michael J Martinelli

Rolf Wagner

John T Randolph

Dachun Liu

Todd Warren Rockway

David A Betebenner

Douglas K Hutchinson

Allan C Krueger

Larry L Klein

Kent D Stewart

Ming Clinton Yeung

Charles A Flentge

Keith F McDaniel

Thomas B Borchardt

William R Baker

Kirill A Lukin

Russell Drew Cink

Sou-Jen Chang

Darold L Madigan

Vincent S Stoll

Brian E Green

Peggy Huang

Thomas J Kress

Mira Hinman

Teresa A Rosenberg

Richard D Bishop

Bhadra Shelat

Daniel P Larson

Barry C Peterson

Todd D Bosse

John R Bellettini

Cynthia B Curty

John Bellettini

Tiffany Spitz

John K Pratt

Anthony K Fung

Daniel A Dickman

Lawrence Kolaczkowski

David A Riley

Xiao-Xiong Zhou

Bruce W Horrom

Nils-Gunnar Johansson

Bjorn G Lindborg

Stephen L Condon

Per Engelhardt

Hormoz Mazdiyasni

Marita Hogberg

Thomas M Zydowsky

Lakshmi Bhagavatula

Chi-nung W Hsiao

Pulla Reddy Singam

Weijiang Zhang

Ramesh R Patel

Greg Lannoye

Greg Wayne

Daniel Plata

Cheng-Xi Yang

Compounds having the formula are hepatitis C(HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C(HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.

Anti-infective agents

Compounds having the formula are hepatitis C (HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C (HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.

Novel processes towards the synthesis of the antiviral valomaciclovir stearate in which an esterified guanine acetal is reduced to the corresponding alcohol, reacted with an activated amino acid and N-deprotected. The esterified guanine acetal is prepared from a 9-guanine derivative bearing an acyclic hydroxymethylbutylacetal. The processes are amendable to one-pot reactions.

Synthesis of acyclic nucleoside derivatives

Methods and novel intermediates for the preparation of acyclic nucleoside derivatives of the formula:where one of Rand Ris an amino acid acyl group and the other of Rand Ris a &#x2014;C(O)C-Csaturated or monounsaturated, optionally substituted alkyl and Ris OH or H; or a pharmaceutically acceptable salt thereof.

Acyclic nucleoside derivatives

Methods and novel intermediates of the formula:

A process for the preparation of 5-hydroxymethylthiazole comprises reacting a compound of the formula, ##STR1## with a carboxylic acid salt (optimally in the presence of a quaternary ammonium salt) and hydrolyzing the resulting ester. Subsequent dechlorination gives 5-hydroxymethylthiazole.

Process for preparation of 5-hydroxymethylthiazole

Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl or benzyl; or R.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.8 is hydrogen or --C(O)R' wherein R' is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.

Process for the preparation of a substituted 2.5-diamino-3-hydroxyhexane

Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or

Process for the preparation of a substituted 2.5-diamono-3-hydroxy-hexane

New intermediates, and processes therefor, provide an efficient method for deriving 4-amino-1,2,2a,3,4,5-hexahydrobenz[cd]indoles, which are themselves intermediates to useful CNS agents, from the Kornfeld-Woodward ketone and like compounds. Preferred embodiments provide means for the preparation of substantially pure enantiomers of the desired 4-amino-1,2,2a,3,4,5-hexahydrobenz[cd]indole.

Intermediates to 4-amino- hexahydrobenz (cd) indoles and processes

Process for the prepartation of a substituted 2,5-diamino-3-hydroxyhexane

A substantially pure compound of formula: ##STR1## wherein R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or

Process for the preparation of a substituted 2,5-diamino-3-hydroxyhexane

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Grayslake, IL, United States of America

M Robert Leanna