Abbott Laboratories Corporation

Abbvie Inc.

Philip E Bauer

Sanjay R Chemburkar

Ketan M Patel

Bikshandarkoil A Narayanan

John F Bauer

Harry O Spiwek

Azita Saleki-Gerhardt

Kimberly A Allen

John E Hengeveld

Kimberly Ann Allen

David B Murphey

Richard R Copp, Jr

Rodney M Mittag

Brian S Moon

Dennis M Abad

Elise H Leese

Brian T Fohey

Greg S Lannoye

A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed.

Polymorph of a pharmaceutical

The present invention provides a simple, 1-step process for preparing a N-(aryl or heteroaryl)-hydroxyurea comprising reacting the corresponding alcohol, ester or ether with hydroxyurea and acid. This reaction is particularly useful for preparing a benzo[b]thienyl substituted N-hydroxyurea of formula: ##STR1## from compound 1: ##STR2## by reacting compound 1 with hydroxyurea and acid. R.sup.1 is selected from the group consisting of hydrogen, 1-6 carbon alkyl, 1-6 carbon alkoxy, and halogen; R.sup.2 is an 1-4 carbon alkyl; and R.sup.3 is selected from the group consisting of hydrogen, acyl, methyl, ethyl and mixtures thereof. Additional steps to isolate the pure bulk product follow.

Synthesis and isolation of N-(aryl or heteroaryl)-alkyl-N-hydroxyurea

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Chester Springs, PA, United States of America

Philip E Bauer