Roche Palo Alto LLC

Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Gary R Lee

Keena Lynn Green

Charles Alois Dvorak

Keshab Sarma

Eric Roy Humphreys

Thomas Cleary

Thimma R Rawalpally

Yaohui Ji

Patrick Finbar McGarry

Anton Constantinescu

Anton Constantinescue

A method for preparing a compound of formula k  

Process for synthesis of phenoxy diaminopyrimidine derivatives

A method for preparing a compound of formula k or a salt or solvate thereof, or a salt or solvate thereof,with ammonia, to form the compound of formula k.

A method for preparing a compound of formula k or a salt or solvate thereof, or a salt or solvate thereof,

A method for preparing a compound of formula I the method comprising treating a compound of formula d with an iodination reagent, to form the compound of formula I, wherein R, Rand Rare as defined herein.

The present invention provides a novel method for preparing a key intermediate, 3-amino-pentan-1,5-diol (2), which is useful for the preparation of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)-propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidine-7-one (1) a MAP-kinase inhibitor useful in the treatment of rheumatoid arthritis.

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Belmont, CA, United States of America

Gary R Lee