Details for Patent: 9,464,094
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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): | Inagaki; Masanao (Toyonaka, JP), Haga; Nobuhiro (Toyonaka, JP), Oda; Shinichi (Iwate-ken, JP) |
Assignee: | Shionogi & Co., Ltd. (Osaka, JP) |
Filing Date: | Mar 15, 2016 |
Application Number: | 15/071,147 |
Claims: | 1. A process for preparing a compound of the formula (I): ##STR00049## wherein R.sup.2 is optionally substituted lower alkyl, and R.sup.3 is optionally substituted lower alkyl, optionally substituted cycloalkyl, substituted or non-substituted aryl or substituted or non-substituted heteroaryl, characterized by treating with a base a compound of the formula (IIA): ##STR00050## wherein R.sup.2 and R.sup.3 are the same as defined above. 2. A process for preparing a compound of the formula (I): ##STR00051## characterized by treating with a base a compound of the formula (IIC): ##STR00052## wherein R.sup.1c is a hydroxy-protecting group deprotectable by a base, and R.sup.2 is optionally substituted lower alkyl, and R.sup.3 is optionally substituted lower alkyl, optionally substituted cycloalkyl, substituted or non-substituted aryl or substituted or non-substituted heteroaryl. 3. A process for preparing a compound of the formula (IB): ##STR00053## wherein R.sup.1d is a hydroxy-protecting group not deprotectable by a base or hydrogen; characterized by treating with a base a compound of the formula (IIB): ##STR00054## wherein R.sup.1b is a hydroxy-protecting group; R.sup.2 is optionally substituted lower alkyl, and R.sup.3 is optionally substituted lower alkyl optionally substituted cycloalkyl, substituted or non-substituted aryl or substituted or non-substituted heteroaryl. 4. The process according to claim 1, wherein the base is an inorganic base. 5. The process according to claim 1, wherein the base is potassium hydroxide, sodium hydroxide, lithium hydroxide, or cesium hydroxide. 6. The process according to claim 1, wherein the reaction temperature is about 30.degree. C.-about 100.degree. C. |