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Serving leading biopharmaceutical companies globally:

US Department of Justice
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Generated: January 18, 2018

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Claims for Patent: 4,870,086

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Summary for Patent: 4,870,086
Title: Optically pure compound and a process for its preparation
Abstract:Optically pure S-(-)-1-propyl-2',6'-pipecoloxylidide hydrochloride monohydrate, with the structural formula ##STR1## a process for the preparation thereof and the use for inducing local anesthesia.
Inventor(s): Sandberg; Rune V. (Jarna, SE)
Assignee: Astra Lakemedel Aktiebolag (Sodertalje, SE)
Application Number:06/934,114
Patent Claims: 1. (S)-(-)-1-propyl-2',6'-pipecoloxylidide hydrochloride, wherein the compound is in the form of its monohydrate.

2. The compound according to claim 1, wherein it is substantially optically pure.

3. The compound according to claim 1, wherein it contains less than 0.5% by weight of the corresponding (R)-(+)-enantiomer.

4. A process for the preparation of substantially optically pure monohydrate of (S)-(-)-1-propyl-2',6'-pipecoloxylidide hydrochloride, which comprises:

dissolving (S)-(-)-1-propyl-2',6'-pipecoloxylidide hydrochloride in a volume of water which is 1 to 3 times its weight;

adding acetone to the dissolved mixture in an amount which is 5 to 15 times the volume of the water added, wherein the temperature of the acetone is between C. and its boiling point; and

isolating the monohydrate of (S)-(-)-1-propyl-2',6'-pipecoloxylidide hydrochloride.

5. The process according to claim 4, wherein the weight of the volume of water is equal to the weight of the (S)-(-)-1-propyl-2',6'-pipecoloxylidide hydrochloride and the volume of the acetone is 10 times the volume of the added water.

6. A method for inducing local anesthesia, which comprises adminstering to mammals including man needing local anesthesia an anesthetizing amount of the compound according to claim 1.

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Serving leading biopharmaceutical companies globally:

US Department of Justice
US Army
Daiichi Sankyo
Cantor Fitzgerald

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