Process for the preparation of histamine H3 receptor modulators

摘要

The present invention is directed to novel processes for the preparation of histamine H3 receptor modulators, in the treatment of for example, cognitive disorders, sleep disorders and/or psychiatric disorders.

主权项

1. A process for the preparation of compound (I-C) or a pharmaceutically acceptable salt or a pharmaceutically active metabolite thereof; comprising reacting compound (V-S) with compound (VIII-S), neat or in an organic solvent; to yield the corresponding compound (IX-S); reacting compound (IX-S) with a reducing agent; neat, in water or in an organic solvent; to yield the corresponding compound (XI-S); reacting compound (XI-S) with compound (VI-S), wherein LG1 is a first leaving group and LG2 is a second leaving group; in an organic solvent; alternatively, reacting compound (XI-S) with compound (VI-S), wherein LG1 is a first leaving group and LG2 is a second leaving group; in the presence of a base; in a mixture of water and an organic solvent; to yield the corresponding compound (X-S); reacting compound (X-S) with compound (XIII-C); in the presence of a second inorganic base; in an organic solvent; to yield the corresponding compound (I-C).