Furazanobenzimidazoles as prodrugs to treat neoplastic or autoimmune diseases

A process for the manufacture of a compound of formula (II-G):

• or a salt thereof,
• comprising the steps:
• (a) reacting a compound of formula
• with an alpha-amino acid derivative of the formula:
• in the presence of an activating agent and optionally in the presence of suitable bases, catalysts or co-reagents to yield the compound of formula:
• (b) reacting the product of Step (a) with a bromination agent to yield the bromo compound of formula:
• (c) reacting said bromo compound obtained in Step (b) with a compound of formula:
• to yield the compound of formula:
• (d) removing any protection groups being present from the group “protected Amino acid” to yield the compound of formula (II-G) and, optionally,
• (e) converting said compound of formula (II-G) to a salt thereof,
• in which formulae
• R1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl,
• represents 1,4-phenylene or a group of formula
• R2-G is a group of formula
• “Amino acid” represents a residue derived from a natural alpha-amino acid selected from glycine, alanine, and lysine by removing the carboxyl group from the alpha-carbon atom of said amino acid;
• and
• “protected Amino acid” means the same amino acid as “Amino acid”, primary amino groups and if required also other functional groups of said amino acid however being protected by a protecting group.