公开(公告)号：US20150126761A1

公开(公告)日：2015-05-07

申请号：US14401826

申请日：2013-05-22

申请人： SciPharm SàRL

发明人： Nareshkumar Jain ,  Michael Kirkup ,  Michael Marella ,  Sanjeevani Ghone

IPC分类号： C07C51/377 ,  C07C59/72 ,  C07F7/18

CPC分类号： C07C51/377 ,  C07C47/565 ,  C07C47/575 ,  C07C59/72 ,  C07C2603/14 ,  C07F7/18 ,  C07F7/1804 ,  C07F7/1892 ,  C12P31/00 ,  C12P41/002 ,  C12P41/004

摘要： A method for the preparation of treprostinil and its derivatives is described. In contrast to prior art, this method utilizes an easily scalable enzymatic resolution of a key intermediate for making these compounds. Another significant improvement of the described method over prior methods is the regioselective Claisen rearrangement of a 5-allyloxy-benzaldehyde precursor, which is facilitated by a bromo substituent in 2-position.

摘要翻译： 描述了曲前列素及其衍生物的制备方法。 与现有技术相反，该方法利用关键中间体易于扩展的酶分解来制备这些化合物。 所述方法与现有方法的另一重大改进是5-烯丙氧基 - 苯甲醛前体的区域选择性Claisen重排，其由2-位的溴取代基促进。

公开(公告)号：US09346738B2

公开(公告)日：2016-05-24

申请号：US14401826

申请日：2013-05-22

申请人： SciPharm SàRL

发明人： Nareshkumar Jain ,  Michael Kirkup ,  Michael Marella ,  Sanjeevani Ghone

IPC分类号： C07C59/115 ,  C07C51/377 ,  C07C47/565 ,  C07C47/575 ,  C07F7/18 ,  C07C59/72 ,  C12P31/00 ,  C12P41/00

CPC分类号： C07C51/377 ,  C07C47/565 ,  C07C47/575 ,  C07C59/72 ,  C07C2603/14 ,  C07F7/18 ,  C07F7/1804 ,  C07F7/1892 ,  C12P31/00 ,  C12P41/002 ,  C12P41/004

摘要： A method for the preparation of treprostinil and its derivatives is described. In contrast to prior art, this method utilizes an easily scalable enzymatic resolution of a key intermediate for making these compounds. Another significant improvement of the described method over prior methods is the regioselective Claisen rearrangement of a 5-allyloxy-benzaldehyde precursor, which is facilitated by a bromo substituent in 2-position.

摘要翻译： 描述了曲前列素及其衍生物的制备方法。 与现有技术相反，该方法利用关键中间体易于扩展的酶分解来制备这些化合物。 所述方法与现有方法的另一重大改进是5-烯丙氧基 - 苯甲醛前体的区域选择性Claisen重排，其由2-位的溴取代基促进。