PROCESSES AND INTERMEDIATES FOR PREPARING A MEDICAMENT

摘要

Disclosed is a process for the preparation of the following compounds:;;where R1, R1a and R2a have the definitions in the description, as well as a process to prepare other intermediates that may be useful to synthesise downstream products, especially compounds that are useful as medicaments, for instance Bruton's tyrosine kinase (Btk) inhibitors such as ibrutinib. Also disclosed are other processes, other intermediates and compounds per se.

主权项

1. A process for the preparation of a compound of formula I, or a derivative thereof, wherein R1 represents a nitrogen protecting group; R1a represents —CN, —C(O)OR1b or —C(O)N(R1c)(R1d); R1b, R1c and R1d each independently represent C1-6 alkyl, aryl or heteroaryl; R2a represents:
(i) phenyl substituted at the 4-position with halo or —O—R2b; or(ii) hydrogen; R2b represents hydrogen or phenyl; which process comprises reaction of a compound of formula II, or a derivative thereof, wherein R1a and R2a are as defined above; X1 represents a suitable leaving group, with a compound of formula III, or a derivative thereof, wherein R1 is as defined above.