SYNTHESIS OF BACE INHIBITORS

摘要

The present invention provides a one step carbonylation of a compound of formula II in the presence of water to afford a compound of formula (I), useful in processes to manufacture BACE inhibitors.;

主权项

1. A one step carbonylation of a compound of formula II in the presence of water to afford a compound of formula I, wherein hal is Cl or Br; X is —C—R2 or N; R1 is selected from the group consisting of
i) halo-C1-6alkyl,ii) C1-6alkyl,iii) halo-C1-6alkoxy,iv) C1-6alkoxy, andv) cyano, R2 is selected from the group consisting of
i) C1-6alkyl, andii) hydrogen.