Reference

Preparation of optically pure (S)-(-)-1-propyl-2',6'-pipecoloxylidide hydrochloride monohydrate and pharmaceutical local anesthetic

Preparation of optically pure (S)-(-)-1-propyl-2',6'-pipecoloxylidide hydrochloride monohydrate and pharmaceutical local anesthetic. (Astra Laekemedel AB, Swed.). Israeli IL 82592 A1 10 Mar 1991, 10 pp. (Israel). CODEN: ISXXAQ. CLASS: ICM: C07D211-60. ICS: A61K031-445. APPLICATION: IL 87-82592 20 May 1987. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 1, 63 The title compd.-HCl (I) contg. (R)-(+)-enantiomer is dissolved in H2O corresponding to 1-3 times of its. wt., acetone 5-15 times of H2O vol. heated to a temp. 45° to its b.p. is added, the soln. filtered, and the end product is isolated as the title monohydrate II as a local anesthetic (no data). I 82 g contg. 10% of the (R)-(+)-enantiomer was dissolved in 85 mL H2O, whereupon acetone heated to its b.p. was added to a final vol. of 850 mL. The soln. 98717-15-8 and 132112-35-7 are cas registry numbers of chemicals which are used as reagents here. was filtered and left for crystn., whereby the 1st crystn. yield 71.7 g, which was dissolved in 72 mL H2O, whereupon boiling acetone to a final vol. of 750 mL was added, the soln. filtered and crystd. to give a final yield of 62.3 g (76%) of an optionally pure (399.5%) II contg. 5.4-5.6% H2O. Injectable solns. contg. II are given. .