PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE INDOLINE DERIVATIVES OR SALTS THEREOF

摘要

The present invention relates to a synthesis method of optically active indoline derivatives or salts thereof, which are represented by general formula I and useful as a starting material for the production of drugs. By introducing terephthaloyl chloride as a starting material and using the same as a link in the synthesis of indoline derivatives or salts thereof, the present invention increases efficiency, greatly facilitates confirmation of intermediates, purification, and processes, and also increases the efficiency of reaction due to excellent stability. By using inexpensive and easy-to-handle zinc instead of expensive platinum catalyst, the present invention improves the yield thereof. By introducing a benzyl group into an amine group (general formula III, preferably chemical formula 23) to ensure optical purity in the final process, the present invention can produce, merely by means of recrystallization, optically pure indoline derivatives or salts thereof, represented by the general formula I.