| 摘要 |
Process for industrial synthesis of (2S) indoline-2-carboxylic acid (I) by reacting racemic acid (III) with chiral amine to form salts (IV), separating crystals of (2S) salt from (2R) salt and then: (1) acidifying (2S) salt of (IV) to give (I); and (2) acidifying (2R) salt of (IV) to form a mixture having a majority of the (2R) acid, racemizing this to form (III) and repeating the process. Process for the industrial synthesis of (2S) indoline-2-carboxylic acid of formula (I) comprises: (1) reacting the racemic acid of formula (III) with a chiral amine to form the salts of formulae (IVa) and (IVb); (2) separating crystals of the (2S) salt (IVa) from the (2R) salt (IVb); (3) acidifying (IVa) with hydrochloric acid (HCl) to form (I); and (4) acidifying the residue containing the (2R) salt (IVb) with HCl to form a mixture having a majority of the (2R) acid; (5) racemizing this with the sodium hydroxide to form the racemic acid (III); and (6) repeating the process. An Independent claim is also included for preparation of perindopril using (I) prepared by the described process. |
