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Last Updated: April 30, 2024

Details for Patent: 9,315,512


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Title:Crystal of 6,7-unsaturated-7-carbamoyl morphinan derivative and method for producing the same
Abstract: Stable crystalline forms of a compound represented by the formula (IA): ##STR00001## an acid addition salt, and/or a solvate thereof are provided by the present invention. Said crystalline forms are extremely useful as materials for preparing medicines. Novel processes for preparing 6,7-unsaturated-7-carbamoyl morphinan derivatives are also provided by the present invention.
Inventor(s): Tamura; Yoshinori (Toyonaka, JP), Noguchi; Kouichi (Amagasaki, JP), Inagaki; Masanao (Toyonaka, JP), Haga; Nobuhiro (Toyonaka, JP)
Assignee: Shionogi & Co., Ltd. (Osaka, JP)
Filing Date:Aug 04, 2015
Application Number:14/818,130
Claims:1. A process for preparing a crystal of an acid addition salt of a compound of the formula (IA): ##STR00049## comprising: adding an acid to the compound of the formula (IA), and optionally crystallizing the acid addition salt from a solvent.

2. A process for preparing a crystal of a p-toluenesulfonic acid salt of a compound of the formula (IA) ##STR00050## comprising: treating with a base a compound of the formula (IID): ##STR00051## wherein R.sup.1 is hydrogen or a hydroxyl-protecting group, 2) adding p-toluenesulfonic acid after deprotecting R.sup.1, and 3) optionally crystallizing the acid addition salt from a solvent.

3. A process according to claim 2, comprising treating with a base a compound of the formula (IIE): ##STR00052## wherein R.sup.1a is hydrogen or a hydroxy-protecting group deprotectable by a base, adding p-toluenesulfonic acid thereto, and optionally crystallizing the acid addition salt from a solvent.

4. The process according to any one of claims 1 to 3, wherein the salt is a non-solvate.

5. The process according to any one of claims 1 to 3, wherein the salt is a hydrate.

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