N-[2-Hydroxy-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-sulphonamide derivatives via N-[2-oxo-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-imine skeleton

摘要

A process, useful in the preparation of a class of sulphonamides which are aspartyl protease inhibitors and useful in the treatment of the human immunodeficiency virus (HIV), comprises the sequence: IV + [V or VI] --> III --> II --> I --> VIII where where each step is claimed individually and wherein:

R1

is a protecting group;

R2

is H, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl or alkyl-cycloalkyl;

R3, R4, R5 and R6

are H, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, alkyl-aryl, aryl-alkyl, alkyl-X-alkyl (where X is O, S or NH), "het", alkyl-"het" and "het"-alkyl;

M

is a group IA or IIA metal, or M is an optionally substituted alkyl, cycloalkyl or aryl group;

R7

is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, alkyl-aryl, aryl-alkyl, alkyl-X-alkyl (where X is O, S or NH), "het", alkyl-"het" and "het"-alkyl; each of R1-7 is independently optionally substituted by up to 5 substituents (as defined in the specification), including oxo (=O) and the divalent -O-(CH2)1-3-O-group which is attached to two points of attachment on one or more of the R1-7 substituents to form a ring;

R8

is a leaving group; and "het" is not defined.