PROCESS AND INTERMEDIATES FOR PREPARING PIRBUTEROL AND ANALOGS

A process for the preparation of a compound of the formula:; or a pharmaceutically acceptable acid addition salt thereof, wherein R is hydrogen, methyl or hydroxymethyl which comprises treating a compound of the formula:- wherein R is benzyl and R is hydrogen or methyl, or R and R are taken together...

Full description

Saved in:
Bibliographic Details
Main Authors CUE, BERKELEY WENDELL, JR, MASSETT, STEPHEN SARGENT
Format Patent
LanguageEnglish
Published 01.09.1982
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
Online AccessGet full text

Cover

More Information
Summary:A process for the preparation of a compound of the formula:; or a pharmaceutically acceptable acid addition salt thereof, wherein R is hydrogen, methyl or hydroxymethyl which comprises treating a compound of the formula:- wherein R is benzyl and R is hydrogen or methyl, or R and R are taken together and are with hydrogen; or, alternatively, to produce a compound in which R is methyl or hydroxymethyl, solvolyzing the compound of the formula (V) in which R and R are taken together, followed by treatment with hydrogen; followed by, optionally, conversion of the product (1) into a pharmaceutically acceptable acid addition salt by reaction with a suitable acid. Pirbuterol (R = hydroxymethyl) is a well known bronchodilator. Also claimed are certain novel intermediates, including those of the formula (V).
Bibliography:Application Number: EP19820300602