Abbott Laboratories Corporation

Denton C Langridge

Hing L Sham

Daniel W Norbeck

Chen Zhao

Anthony Ralph Haight

Howard E Morton

Thomas J Sowin

Timothy L Stuk

Jien-Heh J Tien

M Robert Leanna

Michael S Allen

Daniel S Reno

Timothy A Robbins

Francis A Kerdesky

David Scarpetti

Linda M Lijewski

Laura Melcher

Arthur J Cooper

Patricia A Oliver

Jieh-Heh J Tien

Steven A Chamberlin

John J Hufnagel

John E Lallaman

Jufang Barkalow

Azad Hossain

Joseph B Paterson, Jr

This invention discloses a novel method for the conversion of carboxylic acids to carbothioic acids and application of the method to the preparation of androstane carbothiolates, such as fluticasone propionate, which avoids column chromatography.

Method for the preparation of fluticasone and related 17&#x3b2;-carbothioic esters using a novel carbothioic acid synthesis and novel purification methods

A process is disclosed for the preparation of N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)carbonyl)-amino acid derivatives.

Process for the preparation of a disubstituted thiazole

A process is disclosed for the preparation of an N-acylated activated derivative of an amino acid or a salt thereof.

Process for the preparation of an activated amino acid

The present invention relates to a process for the preparation of cabonate compounds useful for the preparation of compounds which are human immunodeficiency virus (HIV) protease inhibitors. The compounds have formula I: ##STR1## wherein R.sup.9 is hydrogen or lower alkyl, and the thiazolyl ring can be unsubituted or substituted with a lower alkyl group.

Process for the preparation of disubstituted carbonates

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

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

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

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Wildwood, IL, United States of America

Denton C Langridge