反应详情

(±)cis-1-(3,4-Dichlorobenzyl)-2-methylaminoindane (7.49 g) was prepared from (±)cis-1-(3,4-dichlorobenzyl)-2-aminoindane (Preparation 2, Method B, 13.95 g) as described in Preparations 3-5 , and then converted into the single enantiomers (+)cis-1-(3,4-dichlorobenzyl)-2-methylaminoindane hydrochloride(E1) and (-)cis-1-(3,4-dichlorobenzyl)-2-methylaminoindane hydrochloride(E2) as described above. In each case chiral purity was greater than 99.5% as judged by chiral HPLC analysis (Column: CHIRALPAK AD; Eluent: 99/1 hexane/ethanol+0.1% DEA). The level of other impurities was<0.3% as judged by HPLC (Column: Merck RP--Select B. Eluent A: 0.1% TFA in water; Eluent B 0.1% TFA in acetonitrile; Eluent composition increased linearly from 5%B to 80% B over 40min. and then held at 80% B for a further 10 min).

1. temperatureEluent composition increased linearly from 5%B to 80% B over 40min.