Abstract

SYNTHESIS, CHARACTERIZATION AND PROCESS VALIDATION OF OLANZAPINE INTERMEDIATES

Jawed I. Devlekar*, Sarang D. Kulkarni, Vikas B. Kandekar, Dr. Amol. A. Kulkarni

Abstract

N-Formyl compounds have been widely used in organic synthesis as Protecting of amines, precursor isocyanide preparation, an intermediate For mono methylated amines from primary amines, and catalyst for allylation or Reduction. Thus a number of formylating methods have been reported Acetic formic Anhydride continues to be the most widely used formylating reagent, but it is sensitive to atmospheric moisture and cannot be stored due to decomposition to acetic Acid and carbon monoxide. Many other useful formylation reagents have been Reported such as chloral, activated formaldehyde using DCC or EDCI, activated Formic ester and ammonium formate. Despite the usefulness of these reagents, such as high yields and mild conditions, they are less practical they are either toxic or Expensive and the preparation and use of these reagents require strictly anhydrous Conditions. We were reported a practical formylation procedure using aqueous 85% Formaldehyde. The documented evidence for the manufacturing process for the Olanzapine Intermediate was shown that the process has consistently produced the product within the Predetermined specifications.

Keywords: N-Formyl Piperazine, piperazine, formaldehyde.