公开(公告)号：US08524782B2

公开(公告)日：2013-09-03

申请号：US13011593

申请日：2011-01-21

申请人： Gottumukkala V. Subbaraju ,  Masna Mahesh ,  Hindupur R. Mohan ,  Thatipally Suresh ,  Igor Ivanisevic ,  Mark Andres ,  Kyle Stephens

发明人： Gottumukkala V. Subbaraju ,  Masna Mahesh ,  Hindupur R. Mohan ,  Thatipally Suresh ,  Igor Ivanisevic ,  Mark Andres ,  Kyle Stephens

IPC分类号： A01N31/14 ,  A61K31/075

CPC分类号： C07C37/055 ,  C07C41/26 ,  C07D309/12 ,  C07C39/21 ,  C07C43/23

摘要： The present invention provides a scalable process for the preparation of stilbenes by (i) condensing 3,5-dialkylbenzyl phosphonates with 4′-O-tetrahydropyranyl benzaldehyde to get 3,5-alkyl-4′-O-tetrahydropyranyl Stilbene and (ii) deprotecting the obtained 3,5-Dialkyl-4′-O-tetrahydropyranylstilbene to yield stilbenes. The present invention also provides a novel intermediate 3,5-Dialkyl-4′-O-tetrahydropyranyl stilbene, which is a key intermediate for the synthesis of stilbenes such as Pterostilbene and Resveratrol. The present invention also provides characteristics of various solid forms of Pterostilbene, methods for their preparation, as well as dosage forms containing the same for administration to or consumption by humans.

摘要翻译： 本发明提供了通过（i）将3,5-二烷基苄基膦酸酯与4'-O-四氢吡喃基苯甲醛缩合得到3,5-烷基-4'-O-四氢吡喃基二苯乙烯来制备二苯乙烯的可伸缩方法，和（ii） 将得到的3,5-二烷基-4'-O-四氢吡喃基芪脱保护，得到二苯乙烯。 本发明还提供了一种新型的中间体3,5-二烷基-4'-O-四氢吡喃基二苯乙烯，它是芪类和白藜芦醇合成二苯乙烯的关键中间体。 本发明还提供了各种固体形式的芪萜烯的特性，其制备方法，以及含有它们用于给予或消费人的剂型。

公开(公告)号：US20110144212A1

公开(公告)日：2011-06-16

申请号：US13011593

申请日：2011-01-21

申请人： Gottumukkala V. Subbaraju ,  Masna Mahesh ,  Hindupur R. Mohan ,  Thatipally Suresh ,  Igor Ivanisevic ,  Mark Andres ,  Kyle Stephens

发明人： Gottumukkala V. Subbaraju ,  Masna Mahesh ,  Hindupur R. Mohan ,  Thatipally Suresh ,  Igor Ivanisevic ,  Mark Andres ,  Kyle Stephens

IPC分类号： A61K31/09 ,  C07D309/12 ,  C07C41/30 ,  C07C37/11 ,  C07C43/23 ,  A61P35/00 ,  A61P29/00 ,  A61P39/06

CPC分类号： C07C37/055 ,  C07C41/26 ,  C07D309/12 ,  C07C39/21 ,  C07C43/23

摘要： The present invention provides a scalable process for the preparation of stilbenes by (i) condensing 3,5-dialkylbenzyl phosphonates with 4′-O-tetrahydropyranyl benzaldehyde to get 3,5-alkyl-4′-O-tetrahydropyranyl Stilbene and (ii) deprotecting the obtained 3,5-Dialkyl-4′-O-tetrahydropyranylstilbene to yield stilbenes. The present invention also provides a novel intermediate 3,5-Dialkyl-4′-O-tetrahydropyranyl stilbene, which is a key intermediate for the synthesis of stilbenes such as Pterostilbene and Resveratrol. The present invention also provides characteristics of various solid forms of Pterostilbene, methods for their preparation, as well as dosage forms containing the same for administration to or consumption by humans.

摘要翻译： 本发明提供了通过（i）将3,5-二烷基苄基膦酸酯与4'-O-四氢吡喃基苯甲醛缩合得到3,5-烷基-4'-O-四氢吡喃基二苯乙烯来制备二苯乙烯的可伸缩方法，和（ii） 将得到的3,5-二烷基-4'-O-四氢吡喃基芪脱保护，得到二苯乙烯。 本发明还提供了一种新型的中间体3,5-二烷基-4'-O-四氢吡喃基二苯乙烯，它是芪类和白藜芦醇合成二苯乙烯的关键中间体。 本发明还提供了各种固体形式的芪萜烯的特性，其制备方法，以及含有它们用于给予或消费人的剂型。