Title: Process for preparing 6-chloro-2-chloromethyl-4-phenylquinazoline-3-oxide and intermediates therefor

Abstract: A process is described for the preparation of 6-chloro-2-chloromethyl-4-phenylquinazoline-3-oxide, a key intermediate in the synthesis of the known useful psychotherapeutic agents: chlorodiazepoxide and diazepam. This intermediate is prepared by the cyclization of 2-(1'-chloroimino-2'-chloromethyl)-5-chlorobenzophenone, itself a new compound. This compound in turn is prepared by the chloroacetylation of 2-amino-5-chlorobenzophenone to 2-chloroacetamido-5-chlorobenzophenone, another novel compound, and subsequent iminochloride formation.

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Inventors: Nakanishi, Susumu (Niantic, CT, US)
Barth, Wayne E. (East Lyme, CT, US)

Application Number: 508103
Filing Date: 1974-09-23
Publication_date: 1976-01-13
Assignee: Pfizer Inc. (New York, NY)
Primary Class(es): 544/283 564/212, 564/248
Other Classes:
US Patent Ref:

3340253

Sep, 1967

Reeder et al.

260/239.

Other Refs:
Primary Examiner: Rush, Raymond V.
Assistant Examiner:
Attorney: Connolly and Hutz